0<< DBOBJSDEFFORMFLDNAMESINDEX0INDEX57WANTSKSWSFIELDS0!1!1X !1!1 D HQDNNQ"Z^$Z"&42}.e&o(*.`6e#,{,#*;Y]22(jV [F8pL& %$b |F"g{*|6Vy FF9y0*(rCtNnF}:<O~o.HLf\0Btx'xW { y |]a]a9%}# zZt#J ; :%%۷$ E =Vt ٻUt W,v$p%$ $|$n%&/&k&s&&&( zWt( ִXt*, k\t,x%,q%,Όr%,Όs%, ,,.4Lt.dMt.Nt.PE~%.PE%../.s#.s.2[2* 2* 4 {%4 |%4ut%4uu%44|4}4#6G(Ot6Qt6fm%8Yt:kx%:y%:O:WH<3s}%<^z%^` hb s0RU!1!1uu>C:\TudorData\SunsetMolecular\Wombat2004\wb2004_histH1GPCRs.dbRootIDSMDL.ID SMDL.IDx SMDL.SIDmol.ref mol.name mol.gnamemol.str *Structuremol.smimol.kwkw est.logkow est.logwsol exp.logkow exp.logwsol act.listidtypevalueminmaxinhib target.type target.name bio.speciesbio.tissuetypebio.tissuesource bio.cellbio.intracellstr bio.stimulus bio.effect swissp.idswissp.species enz.family enz.name enz.typeenz.ecenz.substrate enz.reactant enz.cofactorenz.radiosubstrate enz.actdet rec.family rec.name rec.type pro.family pro.name pro.typebind.endogenligandbind.radioligandbind.nonspecificother*fmla_mol.str*mol.weight_mol.str*ctab_mol.str*keys_mol.str*exact_mol.str antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine + D' [ffr@333333@rh|SMDL-00000472-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482a!-x8G}&D˖ ,??LFp " v  @0 LxQx $< = > ? @ABCDEFGHIJKLMNOPQRSTUVWXYZ[\]^_`abcd e f!g!h"i"j#k#nsotp u        l qmr      ( 0 8!"@#$$$%&'()*+,-./0123456 7 8 9 : ; dm     $CN(C)CC1CC2N(O1)c3ccccc3Cc4ccccc24oes TPF"X !JĂEC&S UuH`\ċ`$`aY^T^YY5^3NF|eFPc6ޭʃdd$2X& y=DtQ: b B %p K%jF'lI1|[8 b F""%$p$&L&&*(o(X*,,}.S0622~4\6F8::6<~<>^>>F@@0BxBD\DDDFF2HzHJ_JJHLL;NN'PoPBRyPLT'VoVXVXXAZZ\f\^O^^;``!bhbdHdd8ffhahjHjj;ll'nrnp_plKrrrstuvwxyz{|}0EtU!1!1dm +  IC508.72008.72008.7200 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150  !"#$%&'()*+  IC508.42008.42008.4200 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine ,./0123456789:;<=  -?D%(@t@Q@|?5SMDL-00000470 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 1 R-95292 (CN(C)CC1CC2N(O1)c3cc(Cl)ccc3Oc4ccccc24wuu TPN ,HJԠC)p/$ZBʩJ<!Q"d(ŚK sMo:X QLbVc R:VoBFȟR1-+ͱqÅü]۠;H1V-{` ! -x8G}'D . ,     ? abs  IC506.99006.99006.9900 receptorH1human cloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine>@ABCDEFGHIJKLMNO gIC507.98007.98007.9800 receptor5-HT2Ahuman:cloned L929 cell antagonistP28223humanxGPCRserotonergic receptor@[125I]R-91150[^_`abcdefghijklm IC508.13008.13008.1300 receptor5-HT2Chuman cloned CHO cell antagonistP28335humanGPCRserotonergic receptor3[3H]mesulergineenpqrstuvwxyz{|}~  \o D%"p@ @\(\]SMDL-00000471-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2483 mianserin CN1CCN2C(C1)c3ccccc3Cc4ccccc24eEo T(Q ZUJԩAP2İH'*5ʇR,%Ҝ6u6̧R"$'ht/}/t:&L!N 8;8!/m?,X8*MD /m,PRSTUVZXWY7IC508.47008.47008.4700 receptorH1humancloned CHO cell vnh"  | 6 z p f \ P F < 2 * $ t ~ , p j : ( 4bt Z R H > 0 $     \B:0& pvld^:@J$P*4~Ztb IC507.64007.64007.6400 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150        IC507.91007.91007.9100 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine  !"#$%&  (abs IC508.17008.17008.1700 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine')*+,-./012345678  dmCF + GI DHKIC507.04007.04007.0400 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 MPQRSTUVWXYZ[\]^_  IC507.43007.43007.4300 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor[3H]mesulergine`bcdefghijklmnopq  NasD)ĠiQFs@E)\(@~jtOSMDL-00000473-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482b%CN(C)CCC1CC2N(O1)c3ccccc3Cc4ccccc24suu TPe+:d+QJ ><`!>(>خhHyyēgǙ'rFs&ҕ99)yؾ @!-X8oG}&Ò nt,9;<=>B@?A??oabs1JL N@IC507.08007.08007.0800 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilaminertuvwxyz{|}~ dmrF+@8o IC508.41008.41008.4100 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150 IC507.73007.73007.7300 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCR    D+Ԡ0 GD't@Q@&\SMDL-00000474-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482c&CN(C)CCCC1CC2N(O1)c3ccccc3Cc4ccccc24ww TPeAƊ ZN!Smx B\kskN1VOSR|z/h}h=N9ь׳CS|!h̶̏L*) 2 RoS.k!-X8oG}&Ò ,??abs    $ x l b X N F @ X`j " ,  2  V ~ P  $RV < 4 *   h P6.$ d~tj`XR .4>D(`<hVhhNF<2$zzpf^X|rdVLB8,"P pserotonergic receptor [3H]mesulergine  IC506.17006.17006.1700 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine              dm #  + $ &  ! % ( IC507.37007.37007.3700 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 * - . / 0 1 2 3 4 5 6 7 8 9 : ; <   IC507.84007.84007.8400 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine = ? @ A B C D E F G H I J K L M N   + > P D+Ԡ0 GD't@" Q@&\, SMDL-00000475 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2e&CCN(CC)CC1CC2N(O1)c3ccccc3Cc4ccccc24ww TPF"X !JĂEC2bPTL%T}x B \crepU /Ny}g5z /Sْ{rgwgɌ{8BϬ{j(r2e-e !-x8G}&ؠD˖  ,         ?? abs ' )  IC507.87007.87007.8700 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamineO Q R S T U V W X Y Z [ \ ] ^ _ `   dmk n C50+eo q C l p s IC50 <6.0000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150u x y z { | } ~   IC506.49006.49006.4900 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor[3H]mesulergine@   v D/3"u@m yGz@ETw SMDL-00000476-Bioorg. Med. Chem. Lett. 12(2)-2002 243-248a2f,CC(C)N(CC1CC2N(O1)c3ccccc3Cc4ccccc24)C(C)C{ TPFE`*'N*HQ.\*DWN -O0FO;޸n<'姡 șHMM!-x8G}&ؠD˖ 3,a c d e f j h g i ??0absr t ed.IC506.82006.82006.8200 receptorH1humanccloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine  .D)(*w@ RQ@K SMDL-00000477-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482g!8/8g&L˖ ,    ?? antagonistP28223humanGPCRvlbT n N z n d Z T H > 4 * "  f z p b V L B 8 , "    P P6.$ X b   " f vlfZPF<4.xvlbXLB8.& ppVND:, x(<zth^TJB<. ~dm   +    IC50 <6.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150                  IC506.16006.16006.1600 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine  ! " # $ % & ' ( ) * + , - . / 0    2 0CN(CC1CC2N(O1)c3ccccc3Cc4ccccc24)C(=O)C(F)(F)F} T$BBP)Q-81u.a<ε;c56Z4X¬W>..7Vn6n۶wjx=;T=s 6%6 D8 abs   IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine1 3 4 5 6 7 8 9 : ; < = > ? @   dmK N  + O Q  L P S IC507.88007.88007.8800 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 U X Y Z [ \ ] ^ _ ` a b c d e f g   IC508.15008.15008.1500 receptor5-HT2Chuman cloned CHO cell antagonistP28335humanGPCRserotonergic receptor[3H]mesulergineh j k l m n o p q r s t u v w x y   V i { D%ۊeq@M \(\@\(\W SMDL-00000478-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482h!CNCC1CC2N(O1)c3ccccc3Cc4ccccc24kUq TPejT B* :!I)dj:PA0b*22b^v/_F/rug%,r%V(}}汜4D%Dep:tp!j,x9G}&D˖ @j,A C D E F J H G I ??abscR T oniIC507.97007.97007.9700 receptorH1human5cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilaminez | } ~   dm MDL+. 43- IC507.80007.80007.8000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanCGPCRserotonergic receptor[125I]R-91150  A 9 D# pp@ (\ @\(\ SMDL-000004799-Bioorg. Med. Chem. Lett. 12(2)-2002 243-248P2j NCC1CC2N(O1)c3ccccc3Cc4ccccc24gEo TPej BT:İH25ʇ( 1Ut x1u//vV9}ˆc}*>>"m":828!3,x9G}&D˖ e., ??abs 9, ??humancloned L929 cell h^T Nx v l b X L B 8 . & p     >  6   H <"Pvj`VLD>|  *0 @  TBH v T:2(f& :~tj`TH@:x&, vIC508.25008.25008.2500 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine      IC506.70006.70006.7000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine !"#  + .1 abs 24 /36IC507.24007.24007.2400 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 8;<=>?@ABCDEFGHIJ  IC507.86007.86007.8600 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine KMNOPQRSTUVWXYZ[\  9L^D)ĠiQFs@0@ r:SMDL-00000480 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2k'CN(C)CC1(C)CC2N(O1)c3ccccc3Cc4ccccc24 uuu$TQD*h$ J+Q ><`!"pU}<%8=FFF腼LK˝%E4&.pE4WD0 RF/TnȡlHMM!~-x]8g}&ȝd˖ ~,$&'()-+*,??easu@57anIC508.78008.78008.7800 receptorH1humanecloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine]_`abcdefghijklmn +oy|orabs}S z~IC50 <6.0000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor [125I]R-91150 IC506.03006.03006.0300 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptor@[3H]mesulergine@ 0 D)ĠiQFs@{@ rSMDL-00000481-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482l'CN(C)CC1(C)CC2N(O1)c3ccccc3Cc4ccccc24uuu$TQD*h$ J+Q ><`!"pU}<%8=FFF腼LK˝%E4&.pE4WD0 RF/TnȡlHMM!~-x]8g}&ȝd˖ ~,oqrstxvuw??asuIC507.21007.21007.2100 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine  x n d ^ R H > 4 , & p z n d Z P D : 0 &   h h N F < 2 $   p z     6  ~  |pf\RJDxnbXND<6ldZPB4*  .,4>*T$&|rh^VPzpbVLB8," xdm   +   IC507.60007.60007.6000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150  !"#$%  IC507.79007.79007.7900 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine &()*+,-./01234567  '9D+Ġut@ Gz@Q8SMDL-00000482 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2m(C(C1CC2N(O1)c3ccccc3Cc4ccccc24)N5CCCC5yy TPF"X  !JjUCbQTL%T}Hk`W\\Ë_$_َԷ^33D|EPcc,{߬JibdK !s,x8G}&ؠD  abs  IC508.52008.52008.5200 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine8:;<=>?@ABCDEFGHI  dmTW + XZ UY\IC506.85006.85006.8500 receptor5-HT2Ahuman)cloned L929 cellC antagonistP28223humanbGPCRserotonergic receptor_[125I]R-91150^abcdefghijklmnop eIC50 <6.0000 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptor[3H]mesulergineqstuvwxyz{|}~  _rD+Ġ(Pu@VGzG@1Zd`SMDL-00000483-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482n)C(C1CC2N(O1)c3ccccc3Cc4ccccc24)N5CCOCC5-{ TPF"X Z*X:dJE:@!5/WW }V2--wv7|*:_9̸=/<؟$f: 2 R6Z6!$ s,x8G}&ؠD $,JLMNOSQPR??abs[]IC507.58007.58007.5800 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine dm@[3+ IC506.55006.55006.5500 receptor5-HT2A  D- u@Q@VSMDL-00000484-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482q*CN1CCN(CC2CC3N(O2)c4ccccc4Cc5ccccc35)CC1} TPF"XU X&VzPDXHR1Pьxu0ZA0k v *)/*/Y}*[o[n/mtV-/V?a1'"r"1zvhyv@%e@t@Jlʥl!R,x8G}&D <R,??abs@  * nv \ 2 V &  :h ~ t j b \  znbZTxn`RH>4( LD L V 6  b 0  > ~vp$8 L|rf\RH@:X`j&,P,P> serotonergic receptor [125I]R-91150 IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine        IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine !"#  dm.1 + 24 /36IC50 <6.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 8;<=>?@ABCDEFGH  IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine IKLMNOPQRSTUVWX  9JZD-=u@0Gz@qh|:SMDL-00000485 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2d'CN(C)CCCCC1CC2N(O1)c3ccccc3Cc4ccccc24 {y TPeTARAcŊ02d)BE@^a.ʣң2\ %OWU:`;ei%(KOvKJV0'b4&>ޤ&$!ߊ-X8oG}&Ò ߊ,$&'()-+*,??abs570IC50 <6.0000@ receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamineY[\]^_`abcdefgh  dmsv@I+wy tx{IC50 <6.0000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150C} IC50 <6.0000 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptor[3H]mesulergine0 e ~D38V-2x@uGz@5^I B SMDL-00000486@-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482i4O=C1N(CC2CC3N(O2)c4ccccc4Cc5ccccc35)C(=O)c6ccccc16捁 TPM ERBDK%S rA )CNhamdHe4Yxqx p@bȪcS#[``Fڲv#ږ#ΤZO3GT zhze_m03!>d&$!=<G&ѽ٢E 0,iklmnrpoq??abs8z|IC50 <6.00001 receptorH1human@cloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine y??3 antagonist67vp | p f \ V J > 6 0 h | t j ` R F < 2 (     @ R 8 0 &   H d  *   V  xnh\PHBzzpfZNF@~vndZL>4* 8*2<"L$"|pf\RF:2,rj dm   +  IC50 <6.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150  !"#$  IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine %'()*+,-./01234  &6D'(lw"Fs@ RQ @X9vSMDL-00000487 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2o(CN(C)C(=O)C1CC2N(O1)c3ccccc3Cc4ccccc24uuu`TPD"ua*F!R+Q T ><`!~5Xt.vus w5tvy5'6Fa,/,׼h&9& !U /8G&٢Eϖ U , abs  IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine5789:;<=>?@ABCD  dmOR + SU PTWIC50 <6.0000 receptor5-HT2Ahuman.cloned L929 cell4 antagonistP28223human3GPCRserotonergic receptor[125I]R-91150TY\]^_`abcdefghi IC50 <6.0000 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptor[3H]mesulergine@jlmnopqrstuvwxy  Zk{D+?t@Q\(\ @%C[SMDL-00000488-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482p)C(C1CC2N(O1)c3ccccc3Cc4ccccc24)N5CCNCC5{ TPF"X Z*X:dJE:@1 t.vX Ҡ4y&ְ.RaXWV7,/,(9hq%%@!s,x9G}& e4n,EGHIJNLKM??cabsoVXuleIC50 <6.0000 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilaminez|}~ dm+ IC50 <6.0000 receptor5-HT2Ahumancloned L929 cellP28223 D7]hӸy@Gz@$SMDL-00000489-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482r3C(C1CC2N(O1)c3ccccc3Cc4ccccc24)N5CCN(CC5)c6ccccc6TPB95PTGHL1EPA )!DRQF^ԑqVa B 0ܩih j 1Q+-6ƭ6F+Jm^Ut2_A0!m15umeToU2)d#&3GGw z!(s,x8G&ؠD \(,??abs  ~ ~ F B| @  Jx ~ t j d X L D > v zpf\PD<6tldZPB4*  |.& . 8  D   |v(~tj`TH@:x^fp&,b(\,0 human GPCRserotonergic receptor [125I]R-91150 IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine        IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine !"#$%  dm03 + 46 158IC50 <6.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 :=>?@ABCDEFGHIJ  IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine KMNOPQRSTUVWXYZ  ;L\D7Y/{@2p= ף@Cl{ <SMDL-00000490 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2s5Clc1cccc(c1)N2CCN(CC3CC4N(O3)c5ccccc5Cc6ccccc46)CC2TPBE5PhDRO,xTS5ՔCTTB -F^QGQKR؇ޅSۄP0P y5yHolLۊhnKo8zQF؊zWL:]WFl]z[L.G%LdYLl[)Q;6; T!>K s,x8G'ؠD >Ka,&()*+/-,.??rabs79115IC50 <6.0000 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine[]^_`abcdefghij dmux+y{ vz}IC50 <6.0000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150 IC50 <6.0000 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptor[3H]mesulergine @ D3Ġq8w@w@}?5^ISMDL-00000491-Bioorg. Med. Chem. Lett. 12(2)-2002 243-2482t.C(C1CC2N(O1)c3ccccc3Cc4ccccc24)N5Cc6ccccc6C5ƅTPP5PTQE5PB9$a]daQJRNF@ B&nj6DKfaoց]RokaA^y}]:s^yx]"0Nܟ'~ў &vj!s,x8G}&ؠD ,kmnoptrqs??abs|~?IC50 <6.0000 receptorH1humancloned CHO cell antagonistP35367humanGPCR 1 x r ~ | r f Z R L z p f X J @ 6 ,   D Z b l .  ^ ( & T .xl`XRvl^PF<2& Jt|48l.@n"4xndXLD>|, histaminergic receptor[3H]pyrilamine+   abs  IC50 <6.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150  !"#$%&'  IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine (*+,-./01234567  )9D' [ffr@333333@rh|SMDL-00000492 -Bioorg. Med. Chem. Lett. 12(2)-2002 243-248 2u$CN(C)CC1CC2N(O1)c3ccccc3Cc4ccccc24qes$TPF"X %BĂÆ&S }XEaSEݩ]xGלOwaxwԟS{.w;! !-x8G}&D˖  ,    ?? asu  IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine8:;<=>?@ABCDEFG  dmRU + VX SWZIC507.64007.64007.6400 receptor5-HT2Ahuman0cloned L929 cellC antagonistP28223human@GPCRserotonergic receptorX[125I]R-91150\_`abcdefghijklmn  IC507.91007.91007.9100 receptor5-HT2Chumancloned CHO cell antagonistP28335human@GPCRserotonergic receptor[3H]mesulergine@oqrstuvwxyz{|}~ @ ]pD' [ffr@T333333@rh|^SMDL-00000493C-Bioorg. Med. Chem. Lett. 12(2)-2002 249-253@2C$CN(C)CC1CC2N(O1)c3ccccc3Cc4ccccc24oes TPF"X !JĂÆ(S UuH`PџWIkZ#TIO=,Y=$Td$TٌzH_KzLz1]cdD`_!-x8G}&D˖ ,HJKLMQONP??absY[IC508.17008.17008.1700 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine dmoni+tept IC507.32007.32007.3200 receptor   D)ĠiQFs@ffffff@S㥛SMDL-00000494-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533a'CN(C)CC1CC2N(O1)c3ccccc3Cc4cccc(C)c24suu TP E0U, J$i-Z2Rg6<!?>7״WzH(v&zHȈGt%Xt%cĈX!)-x8G&D˖ ),??abs 0 &    < nv n 2 h 8 & :h ~ x , zt.rh^TH>4*"l` h r h $ b 2 , Z 2DB(  VvnhBJT,Z2<N*ZHV 5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 IC507.52007.52007.5200 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine     IC507.93007.93007.9300 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine !"#$%&'()*+,-./  dm:= + >@ ;?BIC507.98007.98007.9800 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 DGHIJKLMNOPQRSTUV  IC508.20008.20008.2000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine WYZ[\]^_`abcdefgh  EXjD)ĠiQFs@<ffffff@S㥛FSMDL-00000495-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533b'CN(C)CC1CC2N(O1)c3ccccc3Cc4cc(C)ccc24@suu T(QU0!C'Z,|T( 0"Z2Rh-<!BGBw̗+Ʊv}x˸׺we8Ghh$w=2!-x8G}&D˖ co,023459768??absACIC507.80007.80007.8000 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamineiklmnopqrstuvwxyz dm+ IC508.16008.16008.1600 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150 IC508.33008.33008.3300 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptor@[3H]mesulergine @ D'E )?s@@V-SMDL-00000496-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533c'CN(C)CC1CC2N(O1)c3ccc(F)cc3Cc4ccccc24uuu TPEeԠB' XP/$Z2J<!  ݶ ]m>{^wa>_^"6BfVc,cv!R %ncUǢS`#!-x8G}'D˖ &,{}~??absIC50       nb H @ 6 ,    v | r j d   @ F P * V 0 : v R z h " ~ z`XND6* " rXPF<."zt$.PV`:f@J`x2ph^TF:0&  2(<pVND:, v8.89008.89008.8900 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilaminedm +  !IC508.46008.46008.4600 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 #&'()*+,-./012345  IC508.98008.98008.9800 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine 689:;<=>?@ABCDEFG  $7ID't3t@@x&%SMDL-00000497 -Bioorg. Med. Chem. Lett. 12(2)-2002 249-253 3d(CN(C)CC1CC2N(O1)c3cc(Cl)ccc3Cc4ccccc24uuu TPU C'pP/$Z2J<! @\k.zN2vអNꡞ"#AZ^Uҕ Bf*"mZŎC# !s -x8G}'D˖ .s ,?? abs  " IC508.63008.63008.6300 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamineHJKLMNOPQRSTUVWXY  dmdg +hj eilIC508.51008.51008.5100 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptore[125I]R-91150(nqrstuvwxyz{|}~ IC508.52008.52008.5200 receptor5-HT2Chumancloned CHO cell antagonistP28335human GPCRserotonergic receptor[3H]mesulergine@  oD)ĠiQFs@fffffff@S㥛pSMDL-00000498e-Bioorg. Med. Chem. Lett. 12(2)-2002 249-253l3e'CN(C)CC1CC2N(O1)c3cc(C)ccc3Cc4ccccc24esuu TPU C'Z,|T( /"Z2F<!0?>'˷F̗zا(ֱzxwاt5؊cdtU}7!-x8G}&D˖ ,Z\]^_ca`b??abskmIC508.23008.23008.2300 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine dm.+u0  D't3t@@x&SMDL-00000499-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533g(CN(C)CC1CC2N(O1)c3c(Cl)cccc3Cc4ccccc24uuu TPEeԠ,V2h- Z2*B<!n.|Nxa2NZ!"CZҕf9X#Z^c-"#BҕȎC`#!/$-x8G'L˖ ./,??abs Zbl X  R "  &T ~ t n b X N D < 6 vlbVLB80*z z`XND6(  " & 0  H   ~rh^TLFzpdZPF>8nf\RD6," 0.6@,V&(zrh^PD:0* rIC507.49007.49007.4900 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150      IC507.99007.99007.9900 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine  !"#$  &IC507.81007.81007.8100 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine%'()*+,-./0123456  dmAD + EG BFIIC507.17007.17007.1700 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 KNOPQRSTUVWXYZ[\]  IC508.12008.12008.1200 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine^`abcdefghijklmno  L_qD)R8_v@C ףp= @(\MSMDL-00000500-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533i.CN(C)CC1CC2N(O1)c3ccccc3Cc4cccc(c24)C(F)(F)F{ P(B DJU)J(BC&ňA1JLь5!cxџ#WZI#sKY=_KTI+O=,79:;<@>=???absHJIC507.32007.32007.3200 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamineprstuvwxyz{|}~ dm+}8 IC506.52006.52006.5200 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150 IC507.71007.71007.7100 receptor5-HT2Chumancloned CHO cell antagonistP28335human      D)Ġ(_FFt@Q@p= ףSMDL-00000501-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533j&COc1ccc2Cc3ccccc3N4OC(CN(C)C)CC4c2c1yw PU0 C'Z,|TE".dDdNR[x @C#2Ͻq-%ɬN*ŧJ*2n=N*]lF-2q0z%=6/]vj" /!g -x8G}&D˖ g,??abs   $ t j ` V N H  bjt$ * 4  :   ^ & X (  .\^ D < 2 (    p  @& TzndZPHB$.4hDXFpX>6,"j|rh^VP |rdVLB8," zGPCRserotonergic receptor [3H]mesulergine IC507.84007.84007.8400 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine              dm #  + $ &  ! % ( IC507.27007.27007.2700 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 * - . / 0 1 2 3 4 5 6 7 8 9 : ; <   IC507.97007.97007.9700 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine = ? @ A B C D E F G H I J K L M N   + > P D'E )?s@" @V-, SMDL-00000502 -Bioorg. Med. Chem. Lett. 12(2)-2002 249-253 3k'CN(C)CC1CC2N(O1)c3ccccc3Cc4ccc(F)cc24 uuu PU0 C'pP/$Z2R)i-<! ܹ\2~NZp.aNz!"#[cU!C`fT#LoEZYUʎ%B /" !k-x8G}'D˖ &k ,         ?? abs ' )  IC508.42008.42008.4200 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamineO Q R S T U V W X Y Z [ \ ] ^ _ `   dmk n +.o q 0 l p s IC507.50007.50007.5000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor[125I]R-91150u x y z { | } ~   0IC507.93007.93007.9300 receptor5-HT2ChumanHcloned CHO cell antagonistP28335humantGPCRserotonergic receptori[3H]mesulergine   v D'E )?s@m @V-w SMDL-00000503.-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533l'CN(C)CC1CC2N(O1)c3ccccc3Cc4c(F)cccc24@uuu T(QCePT!,V2衤- Z: )hQ*<!""|rZV_nRF#ƘxrZ#Ȋ&~C~X#k`+Ȳ#j`-"#!-x8G'D˖ &),a c d e f j h g i ??0absr t ed.IC508.64008.64008.6400 receptorH1humanFcloned CHO cell antagonistP35367humangGPCRhistaminergic receptor[3H]pyrilamine  .D)R8_v@" ףp= @(\"SMDL-00000504-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533n!0/}8g&D˖ , "" "??histaminergic receptorclonedGPCRvlR l L x l b X R F < 2 (  d | n b X N D 8 . $   \ \B:0& d n   z * r zpf`TJ@6.(r|pf\RF<2( jjPH>4&r|"8 ~tnbXND<6" ~dm"" + " " " " "IC506.00006.00006.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 """""""""""""""" "  IC506.36006.36006.3600 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine !"#"$"%"&"'"(")"*"+","-"."/"0"1"2"  """4".CN(C)CC1CC2N(O1)c3ccccc3Cc4c(cccc24)C(F)(F)F{ AQPAQ*L0тC$ƈA1SZDь!cPѨW+YFlZQ\K݃$Tm$TOFQ#’4\6ٕ_ԫi|HKc:bDh >0 abs  " " IC507.43007.43007.4300 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine3"5"6"7"8"9":";"<"=">"?"@"A"B"C"D"  dmO"R" + S"U" P"T"W"IC507.62007.62007.6200 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 Y"\"]"^"_"`"a"b"c"d"e"f"g"h"i"j"k" *IC508.30008.30008.3000 receptor5-HT2Chumancloned CHO cell antagonistP28335human@GPCRserotonergic receptor[3H]mesulerginel"n"o"p"q"r"s"t"u"v"w"x"y"z"{"|"}"  Z"m""D'E )?s@Q"@V-["SMDL-00000505-Bioorg. Med. Chem. Lett. 12(2)-2002 249-253@3q'CN(C)CC1CC2N(O1)c3cccc(F)c3Cc4ccccc24uuu TD*eP!,V 2衤- Z: *%B<!"nRx|rZVF#XrX#ȊbC~~^##j`-"Ȳk`+#!-x8G'D˖ &0,E"G"H"I"J"N"L"K"M"??absnV"X"llIC508.76008.76008.7600 receptorH1human@cloned CHO cell antagonistP35367human"GPCRhistaminergic receptor[3H]pyrilamine~""""""""""""""""" dm""|+#""k` """IC507.04007.04007.0400 receptor5-HT2Ahuman0cloned L929 cell antagonistP28223human@GPCRserotonergic receptor[125I]R-911502""""""""""""""""" ] @ "$$D)ĠiQFs@"ffffff@S㥛"SMDL-00000506@-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533r'CN(C)CC1CC2N(O1)c3cccc(C)c3Cc4ccccc24suu TPE"ePT!,J0Ҋ-Z: *><!GG7&شGH1VxH|% ȈXȈ|%lX!-x8G&D˖ 0,"""""""""??abs0"""??human@""f` x n d Z R L  HPZ( . 8  >  " H r B  Bb H @ 6 ,    t X>6,"l|rh`Z  6<F L&0l H p^t pVND:,  8 L|rf\RH@:&,( pIC508.41008.41008.4100 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine "$$$$$$$ $ $ $ $ $$$$$IC508.22008.22008.2200 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine$$$$$$$$$$$$$ $!$"$#$  dm.$1$ + 2$4$ /$3$6$IC508.94008.94008.9400 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 8$;$<$=$>$?$@$A$B$C$D$E$F$G$H$I$J$  IC508.94008.94008.9400 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine K$M$N$O$P$Q$R$S$T$U$V$W$X$Y$Z$[$\$  9$L$^$D'E )?s@0$@V-:$SMDL-00000507 -Bioorg. Med. Chem. Lett. 12(2)-2002 249-253 3s'CN(C)CC1CC2N(O1)c3cc(F)ccc3Cc4ccccc24 uuu TPU C'pP/$Z2J<! l.zN2_vaNZ"AZUc BfT+bmZ^֣ҕƎC #!s-x8G}'D˖ &s ,$$&$'$($)$-$+$*$,$??tabs-5$7$ IC508.59008.59008.5900 receptorH1humanocloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine]$_$`$a$b$c$d$e$f$g$h$i$j$k$l$m$n$ dmy$|$]me+}$$$ z$~$$IC507.97007.97007.9700 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor [125I]R-91150e$$$$$$$$$$$$$$$$$ IC508.21008.21008.2100 receptor5-HT2Chumancloned CHO cell antagonistP28335humanGPCRserotonergic receptorC[3H]mesulergine7$$$$$$$$$$$$$$$$$  $$$D'@j+t@{$@ r$SMDL-00000508-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533t*CN(C)CC1CC2N(O1)c3cc(F)ccc3Cc4ccc(F)cc24{w T(Q,% BXH0bȐqP%SLlx @D$A?>״7&zXzH(vFHtň(UX}ۗ'ct!-x8G}'D˖ ,o$q$r$s$t$x$v$u$w$??abs$$$IC507.77007.77007.7700 receptorH1humancloned CHO cell antagonistP35367humanGPCR[3H]pyrilamine$$$$$$$$$$$$$$$ $  z t h ^ T J B < l | r h ^ R H > 4 , & v v \ T J @ 2 $    ~  $ , 6  F   zndZPHBvl`VLB:4jbXN@2(,*2<(R"$|rh^VPzpbVLB8," tdm & & + && &&&IC507.65007.65007.6500 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 &&&&&&&&&& &!&"&#&$&%&&&  IC507.95007.95007.9500 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine '&)&*&+&,&-&.&/&0&1&2&3&4&5&6&7&8&  &(&:&D3Ԡc@'w@ &= ףp=@Zd&SMDL-00000509 -Bioorg. Med. Chem. Lett. 12(2)-2002 249-253 3u.CN(C)CC1CC2N(O1)c3cc(ccc3Cc4ccccc24)c5ccccc5ƁTPB 8QBhԁ1PЃEUHFRJRL!h._vNZ2r=ZؿN"BQ&mҕfZ^֣穜YҕŽC`` !-x8G&D  ,"&&&& &&&&abs && IC508.10008.10008.1000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine9&;&<&=&>&?&@&A&B&C&D&E&F&G&H&I&J&  dmU&X& + Y&[& V&Z&]&IC50 <6.0000L receptor5-HT2Ahuman.cloned L929 cell5 antagonistP28223humancGPCRserotonergic receptorT[125I]R-91150_&b&c&d&e&f&g&h&i&j&k&l&m&n&o& IC50 <6.0000 receptor5-HT2Chuman&cloned CHO cell antagonistP28335humanGPCRserotonergic receptor[3H]mesulerginep&r&s&t&u&v&w&x&y&z&{&|&}&~&&  `&q&&D'E )?s@W&@V-a&SMDL-00000510-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533h'CN(C)CC1CC2N(O1)c3ccccc3Cc4cccc(F)c24@uuu PU0ՠ,V*h- Z2R)h1:<!^9 /gZ,ަ#$d.'Vn_P%`e{$U.S$e!/-x8G'D˖ &/&,K&M&N&O&P&T&R&Q&S&??abs\&^&}&IC50 <6.0000 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine&&&&&&&&&&&&&&& @dm&&+&&& &&&IC50 <6.0000 receptor5-HT2A&&&&&&" (((((((  (D)R8_v@& ףp= @(\&SMDL-00000511-Bioorg. Med. Chem. Lett. 12(2)-2002 249-2533m.CN(C)CC1CC2N(O1)c3ccccc3Cc4ccc(cc24)C(F)(F)F{ PT D )Ja„ ѠQ1RLՌ!d^Cd׳܁v%lutL+q@ [tlᜌjtj l{YSĺDXTfj2Q@R!8/}8g&D˖ >8,&&&&&&&&&??abs&&&(     2 z d > ^ .  Ft * 4vl`TLFp x "(2 8n 4  h 8 & < j \B:0& n8 L|rf\RH@:&,lHP>t  L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine ( ( ( ((((((((((((  & ((IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor[3H]pyrilamine(((((( (!("(#($(%(&('(((  dm3(6( + 7(9( 4(8(;(IC50 <6.0000 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor [125I]R-91150 =(@(A(B(C(D(E(F(G(H(I(J(K(L(M(  IC50 <6.0000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine N(P(Q(R(S(T(U(V(W(X(Y(Z([(\(](  >(O(_(D't3t@5(@x&?(SMDL-00000512 -Bioorg. Med. Chem. Lett. 12(2)-2002 249-253 3p(CN(C)CC1CC2N(O1)c3ccccc3Cc4c(Cl)cccc24uuu T(QCePT!,V2衤- Z: )hQ*<!2\9/! c,3P.KF{(dC :`%'b{U.w&$ ! -x8G'D˖ r.T,)(+(,(-(.(2(0(/(1(??abs3:(<(@GPIC50 <6.0000o receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor[3H]pyrilamine^(`(a(b(c(d(e(f(g(h(i(j(k(l(m( y(Ki8.69908.69908.6990 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine@|((((((((((((((GKi8.39798.39798.3979 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor[3H]prazosin(((((((((((((((G Ki7.00007.00007.0000 receptor5-HT2Arat@ membranehippocampus; brain antagonistP14842rat@GPCRserotonergic receptor[3H]-8-OH-DPAT((((((((((((((((( 2 r }(((**#*5*G*Drrd+ĠS" v@z(@~(SMDL-00002162p/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-11526L*Cn1c(=O)sc2cc(CCN3CCC(CC3)c4ccccc4)ccc12}y TQ` Bh+W*L YtiV@B8 tk}HznL9itL,[̐͐+[,z#+zIzn`/.ΐ/!Ҹ=,1.߳T Ҹ0,n(p(q(r(s(w(u(t(v(??ncx({((7.52297.5229~t | r f \ R H B < t l ^ L @ 8 . "    4 F &     Z ^dnR "~ L   *Xzt ~x vlbXL@82p\dn$Z T$(VH.&Z~rjd R80& Ki4.69904.69904.6990 receptor5-HT3 rat membranecortex; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]ketanserin(******* * * * * *****Ki6.00006.00006.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]raclopride************* *!*G  Ki7.69907.69907.6990 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor[3H]pyrilamine"*$*%*&*'*(*)***+*,*-*.*/*0*1*2*3*  Ki6.00006.00006.0000 receptorm1rat membranebrain antagonistP08482rat GPCR; ion channel #muscarinic acetylcholine receptor [3H]telenzepine 4*6*7*8*9*:*;*<*=*>*?*@*A*B*C*D*E*  Ki7.69907.69907.6990 receptorsigma1rat membranebrain antagonistQ9R0C9rat [3H]-(+)-pentazocineG-protein sensibleF*H*I*J*K*L*M*N*O*P*Q*R*S*T*U*V* b*Ki8.52298.52298.5229 receptorsigma2ratr membranebrainz antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocinee*h*i*j*k*l*m*n*o*p*q*r*s*t*GKi8.00008.00008.0000 receptor5-HT1Arat( membranecortex; braine antagonistGPCRserotonergic receptor*[3H]prazosinu*w*x*y*z*{*|*}*~*******G Ki6.39796.39796.3979 receptor5-HT2Arat membranehippocampus; brain antagonistP14842ratGPCRserotonergic receptor[3H]-8-OH-DPAT***************** Ki5.00005.00005.0000 receptor5-HT3rat membranecortex; brain antagonistP35563ratligand-gated ion channelserotonergic receptor[3H]ketanserin***************** nKi7.5229****((,,,,,,,, ,G f*v**** ,Dssd/,w@c*@#~jg*SMDL-00002163/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-11527,Cn1c(=O)sc2cc(CCCCN3CCC(CC3)c4ccccc4)ccc12} TQf Bh+W*Lq0ፆdAA0BZ D4@=J' }~E4iJ'"Ѧv IO>5&z]p{Rd{*$ !=,1.߳T ,W*Y*Z*[*\*`*^*]*_*??nca*d**  F ,   X v n d X N D : 4 . f^P>2*  & 8  LrxT 6 N  >l|rhb\nf\ND80* TD*"Vzpjd ~tfTH@6*    receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]racloprideKi5.22185.22185.2218 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor[3H]pyrilamine , , ,,,,,,,,,,,,,,,  ',Ki8.30108.30108.3010 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine *,-,.,/,0,1,2,3,4,5,6,7,8,9,G Ki8.39798.39798.3979 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor [3H]prazosin:,<,=,>,?,@,A,B,C,D,E,F,G,H,I,G  Ki6.39796.39796.3979 receptor5-HT2Arat membranehippocampus; brain antagonistP14842rat GPCRserotonergic receptor [3H]-8-OH-DPATJ,L,M,N,O,P,Q,R,S,T,U,V,W,X,Y,Z,[,  Ki5.69905.69905.6990 receptor5-HT3 rat membranecortex; brain antagonistP35563ratligand-gated ion channelserotonergic receptor.[3H]ketanserin\,^,_,`,a,b,c,d,e,f,g,h,i,j,k,l,m, ,Ki <7.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor[3H]raclopriden,p,q,r,s,t,u,v,w,x,y,z,{,G eKi8.52298.52298.5229 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor[3H]pyrilamine|,~,,,,,,,,,,,,,,,, @+,;,K,],o,},,Dttd-Ԡ?xv@(,(\@S,,SMDL-00002164/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-11528+Cn1c(=O)sc2cc(CCN3CCC(Cc4ccccc4)CC3)ccc12{ TQT B(FBSV&Nh X"pJ vrQܐVøSܪ/2k¸k۞!H=,1.߳T eH@,,,, ,!,%,#,",$,??nc&,),Ki7.00007.00007.0000 receptorm1rat membranebrain antagonistP08482ratoGPCR; ion channel1#muscarinic acetylcholine receptor)[3H]telenzepinec,,,,,,,,,,,,,,,,, Duud1uVx@.(\@m.SMDL-00002165/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-11529-Cn1c(=O)sc2cc(CCCCN3CCC(Cc4ccccc4)CC3)ccc12}PBQQP e&TO,NDQU\hF CSBP@Bp4=>|AFơh1K"fyOPF@Yp){Tɟ Y" yh!! =,1.߳T  ,,,,,,,,,,??$,f T 0` .  \$ z t n 8 tj`VPJ xjVJB<0$BhN2* zzpf\VPr`TLB6," HZ:," nX ^ h D  r > $ R |*jPH:& .Ki8.30108.30108.3010 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine ... . . . . .......G Ki7.52297.52297.5229 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor [3H]prazosin........... .!.".#.G  Ki6.15496.15496.1549 receptor5-HT2Arat membranehippocampus; brain antagonistP14842rat GPCRserotonergic receptor [3H]-8-OH-DPAT$.&.'.(.).*.+.,.-.../.0.1.2.3.4.5.  Ki5.69905.69905.6990 receptor5-HT3 rat membranecortex; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]ketanserin6.8.9.:.;.<.=.>.?.@.A.B.C.D.E.F.G.  Ki7.00007.00007.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]racloprideH.J.K.L.M.N.O.P.Q.R.S.T.U.V.W.G  Ki8.04588.04588.0458 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor[3H]pyrilamineX.Z.[.\.].^._.`.a.b.c.d.e.f.g.h.i. ..%.7.I.Y.k.nc.Ki6.69906.69906.6990 receptorm1rat membranebrain antagonistP08482ratGPCR; ion channel#muscarinic acetylcholine receptor[3H]telenzepinej.l.m.n.o.p.q.r.s.t.u.v.w.x.y.z.{. .Ki8.52298.52298.5229 receptorsigma2rat membranebrain@ antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine..............GKi7.52297.52297.5229 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor@[3H]prazosin...............G @Ki5.52295.5229.....00000000 0 0 0 0 !0Dvvd+48Ev@.Q @ +.SMDL-00002166/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-115210+Cn1c(=O)sc2cc(CCN3CCN(Cc4ccccc4)CC3)ccc12{ TQ\( `:+*Vh #R@k#h#A-Ne,N)_-u%+u-1e,81_-08^,e,) &00^-!=,1.߳T D@,|.~........??nc..?13@nc|   P 6 .   `  |  fv lvR * L   2`vh^RJD8.$n 0Bzpf\VPjbXJ8,$H4 FzndZPJDrdZNF<0& < 5.5229 receptor5-HT2Arat membranehippocampus; brain antagonistP14842rat GPCRserotonergic receptor [3H]-8-OH-DPATKi4.69904.69904.6990 receptor5-HT3 rat membranecortex; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]ketanserin 00000000000000000  Ki <5.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]raclopride0"0#0$0%0&0'0(0)0*0+0,0-0G  Ki8.15498.15498.1549 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor[3H]pyrilamine.000102030405060708090:0;0<0=0>0?0  ...0 0/0A0Ki6.30106.30106.3010 receptorm1rat membranebrain antagonistP08482rat GPCR; ion channel #muscarinic acetylcholine receptor [3H]telenzepine @0B0C0D0E0F0G0H0I0J0K0L0M0N0O0P0Q0  ]0Ki8.69908.69908.6990 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine`0c0d0e0f0g0h0i0j0k0l0m0n0o0GKi7.39797.39797.3979 receptor5-HT1Arat membranecortex; brain0 antagonistGPCRserotonergic receptor[3H]prazosinp0r0s0t0u0v0w0x0y0z0{0|0}0~00G Ki6.04586.04586.0458 receptor5-HT2Arat@ membranehippocampus; brain antagonistP14842ratTGPCRserotonergic receptor [3H]-8-OH-DPAT00000000000000000 Ki5.09695.09695.0969 receptor5-HT38rat4 membranecortex; brain antagonistP35563ratligand-gated ion channelserotonergic receptor[3H]ketanserin00000000000000000 Ki5.00005.00005.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor000000000000002G  a0q000022%2Dwwd/f6$#x@^0@B`"[b0SMDL-00002167/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-115211-Cn1c(=O)sc2cc(CCCCN3CCN(Cc4ccccc4)CC3)ccc12}PB5EEAdSOu*RL8QU\hFDKQCP h@=edy!rȡh1K$"'P?Bm"`P9y<{$v塅bZ!=,1.߳T T,R0T0U0V0W0[0Y0X0Z0??nc\0_00 ~ t j d ^ x p f X F : 2 (    V B (   T |rh^XRrh\TJ>4*  Jnt~B 2r < :h\6 pxrf\RHB<rj\H<4." 4Z@$lrjbXJ4(  [3H]racloprideKi >7.0000 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor[3H]pyrilamine222222 2 2 2 2 22222  Ki5.00005.00005.0000 receptorm1rat membranebrain antagonistP08482rat GPCR; ion channel #muscarinic acetylcholine receptor [3H]telenzepine 2222222222222 2!2"2#2  Ki7.42957.42957.4295 receptorsigma1rat membranebrain antagonistQ9R0C9rat [3H]-(+)-pentazocineG-protein sensible$2&2'2(2)2*2+2,2-2.2/20212223242 @2Ki8.09698.09698.0969 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine C2F2G2H2I2J2K2L2M2N2O2P2Q2R2G Ki7.00007.00007.0000 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor [3H]prazosinS2U2V2W2X2Y2Z2[2\2]2^2_2`2a2b2G  Ki6.00006.00006.0000 receptor5-HT2Arat membranehippocampus; brain antagonistP14842ratGPCRserotonergic receptor[3H]-8-OH-DPATc2e2f2g2h2i2j2k2l2m2n2o2p2q2r2s2t2 .Ki4.69904.69904.6990 receptor5-HT3rat membranecortex; brain antagonistP35563ratligand-gated ion channelserotonergic receptor[3H]ketanserinu2w2x2y2z2{2|2}2~222222222 oKi7.00007.00007.0000 receptorD2rat@ membranestriatum; brain@ antagonistGPCRdopaminergic receptor@[3H]raclopride222222222222222G D2T2d2v222Dxxd+ |,}F{@A2Q@tE2SMDL-00002168/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-1152121Cn1c(=O)sc2cc(CCN3CCN(Cc4ccc(Cl)cc4Cl)CC3)ccc12@}PB11QdF\PUURI9B<EQʃC` 01ZRZUUj f j>avWfņ vbo^Ʀf6a YƆ٘v`o GV!5 ,1.T d5t,52728292:2>2<2;2=2??gnc?2B212(Ki8.00008.00008.0000 receptorH1ratC membranebrain antagonistP31390ratGPCRhistaminergic receptor[3H]pyrilamine22222222222222222 oDyyd/  .V`}@4(\@S㥛 4SMDL-00002169/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-1152,2222.4444??mbrane" T ~ , x n d Z T N h`VH6*" F 2DxlbXNHB~pbXLD:.$  :h n x < , p  6  4 b J2* `vlbXRLzrhZPD<6*D 4Ki8.04588.04588.0458 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine 4 4 444444444444G Ki6.69906.69906.6990 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor [3H]prazosin444444 4!4"4#4$4%4&4'4(4G  Ki6.04586.04586.0458 receptor5-HT2Arat membranehippocampus; brain antagonistP14842rat GPCRserotonergic receptor [3H]-8-OH-DPAT)4+4,4-4.4/404142434445464748494:4  Ki5.69905.69905.6990 receptor5-HT3 rat membranecortex; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]ketanserin;4=4>4?4@4A4B4C4D4E4F4G4H4I4J4K4L4  Ki7.00007.00007.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]racloprideM4O4P4Q4R4S4T4U4V4W4X4Y4Z4[4\4G  Ki >7.0000 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor[3H]pyrilamine]4_4`4a4b4c4d4e4f4g4h4i4j4k4l4  44*4<4N4^4n43Cn1c(=O)sc2cc(CCCCN3CCN(Cc4ccc(Cl)cc4Cl)CC3)ccc12PB1![dPFSQTRHB^p1xYd@5.0000 receptorm1rat membranebrain antagonistP08482ratGPCR; ion channel.#muscarinic acetylcholine receptor[3H]telenzepinebm4o4p4q4r4s4t4u4v4w4x4y4z4{4|4 4Ki8.30108.30108.3010 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine44444444444444G@Ki7.52297.52297.5229 receptor5-HT1Arat membranecortex; brain antagonist444444444444 66G 6Dzzd+ |,}F{@4Q@t4SMDL-00002170/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-1152143Cn1c(=O)sc2cc(CCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)ccc12}PBMEA BD>a\PUQG-B8ĄEQQȂCP$1ZRZUUf ?avWf vojj o ^Ʀf6a Yf٘v`bGV!* =,1.߷\ d* ,}444444444??nc44???  ~ t n h  |b N @ H   Hv t l b T J > 6 0 $   Z 0zpf\VPjbXJ8,$H4 FzndZPJDrdZNF<0& < " serotonergic receptor [3H]prazosinKi5.30105.30105.3010 receptor5-HT2Arat membranehippocampus; brain antagonistP14842rat GPCRserotonergic receptor [3H]-8-OH-DPAT66666 6 6 6 6 66666666  Ki5.52295.52295.5229 receptor5-HT3 rat membranecortex; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]ketanserin666666666 6!6"6#6$6%6&6'6  Ki6.69906.69906.6990 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]raclopride(6*6+6,6-6.6/60616263646566676G  Ki7.39797.39797.3979 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor[3H]pyrilamine86:6;6<6=6>6?6@6A6B6C6D6E6F6G6H6I6  4466)696K6Ki6.00006.00006.0000 receptorm1rat membranebrain antagonistP08482rat GPCR; ion channel #muscarinic acetylcholine receptor [3H]telenzepine J6L6M6N6O6P6Q6R6S6T6U6V6W6X6Y6Z6[6  f6Ki8.69908.69908.6990 receptorsigma2ratR membranebraine antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocinei6l6m6n6o6p6q6r6s6t6u6v6w6x6GKi6.52296.52296.5229 receptor5-HT1Arat1 membranecortex; brain antagonistGPCRserotonergic receptorh[3H]prazosiny6{6|6}6~66666666666G Ki5.00005.00005.0000 receptor5-HT2Arat membranehippocampus; brain antagonistP14842ratGPCRserotonergic receptor[3H]-8-OH-DPAT66666666666666666 Ki4.52294.52294.5229 receptor5-HT3rat membranecortex; brain@ antagonistP35563ratligand-gated ion channelserotonergic receptor@[3H]ketanserin66666666666666666 dG c j6z66688#858D{{d/  .V`}@g6(\@S㥛k6SMDL-00002171/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-1152155Cn1c(=O)sc2cc(CCCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)ccc12PBIEA BD>aDSQuQI1^p1xYT@,x0A!PYsLAAgYh$n)h-!yyKŸ' )Jw&'b?mHnOYPfAYcT! =,1.߷\ 3t,4]6^6_6`6d6b6a6c6nce6h6GPCRhistaminergic receptor3ptjbX r j ` R @ 4 , "   P < "    N vlbXRL zlbVND8.$` DLR\ J V0jzrl`VLB<6zldVB6.(.B( T~rj`TJ@60*~ Ki7.00007.00007.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]raclopride68888888 8 8 8 8 888Ki8.04588.04588.0458 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor[3H]pyrilamine888888888888888 8!8  Ki6.30106.30106.3010 receptorm1rat membranebrain antagonistP08482rat GPCR; ion channel #muscarinic acetylcholine receptor [3H]telenzepine "8$8%8&8'8(8)8*8+8,8-8.8/808182838  Ki6.85706.85706.8570 receptorsigma1rat membranebrain antagonistQ9R0C9rat [3H]-(+)-pentazocineG-protein sensible4868788898:8;8<8=8>8?8@8A8B8C8D8 + O8R8 P8T8Ki5.69905.69905.6990 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine V8Y8Z8[8\8]8^8_8`8a8b8c8d8e8G Ki <5.0000 receptor5-HT1Arate membranecortex; brain antagonistGPCRserotonergic receptor[3H]prazosinf8h8i8j8k8l8m8n8o8p8q8r8s8G Ki <5.0000 receptor5-HT2Arat membranehippocampus; brain antagonistP14842ratGPCRserotonergic receptor[3H]-8-OH-DPATt8v8w8x8y8z8{8|8}8~888888 Ki <5.0000 receptor5-HT3cratb membranecortex; brain antagonistP35563ratrligand-gated ion channelserotonergic receptor[3H]ketanserin888888888888888 Ki <5.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor[3H]raclopride8888888888888G Ki4.69904.69904.6990 receptorH1rat membranebrain antagonistP31390rat8888888888888866: W8g8u8888:D||d!]s@Q8GzG@EX8SMDL-00002172/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-115216/C[C@H]1CN(CCc2ccc3n(C)c(=O)sc3c2)C[C@@H](C)N1qUo$TQ^*P+WLPP +I: k>\jEyE*PPkYy3]Yl›*wccAim+ !=,1.߳Կ $,E8G8H8I8J8N8L8K8M8??absS8U88   z t n  v h V J B 8 ,   f dJB:0" v ,zpf`Z lt~:P@Jf 0 ` .  8fnf\ND80&2>Rxrf\RHB<zrdPD<6*   [3H]pyrilamineKi <5.0000 receptorm1rat membranebrain antagonistP08482rat GPCR; ion channel #muscarinic acetylcholine receptor [3H]telenzepine :::::: : : : : :::::  + :: :!:Ki7.00007.00007.0000 receptorsigma2rat membranebrain antagonist[3H]-1,3-di-o-tolylguanidine(+)-pentazocine #:&:':(:):*:+:,:-:.:/:0:1:2:G Ki <4.0000 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor [3H]prazosin3:5:6:7:8:9:::;:<:=:>:?:@:G  Ki <4.0000 receptor5-HT2Arat membranehippocampus; brain antagonistP14842rat GPCRserotonergic receptor [3H]-8-OH-DPATA:C:D:E:F:G:H:I:J:K:L:M:N:O:P:  Ki <4.0000 receptor5-HT3 rat membranecortex; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]ketanserinQ:S:T:U:V:W:X:Y:Z:[:\:]:^:_:`:  Ki <4.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor[3H]raclopridea:c:d:e:f:g:h:i:j:k:l:m:n:G Ki <4.0000 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor[3H]pyrilamineo:q:r:s:t:u:v:w:x:y:z:{:|:}:~: $:4:B:R:b:p::D}}d%1_^t@:(\ @V- %:SMDL-00002173@/Bioorg. Med. Chem. Lett. 12(8)-2002 1149-1152171C[C@H]1CN(CCCCc2ccc3n(C)c(=O)sc3c2)C[C@@H](C)N1:yus$TQd*P+WL@ 1n#e`b @H(k Mr+yA2 AR#y+!RshhrwR㥠wݏڞ޶r!=,1.߳Կ 4,:::::::::??abs :":Ki <4.0000 receptorm1rat membranebrain antagonistP08482ratGPCR; ion channel@#muscarinic acetylcholine receptor[3H]telenzepine::::::::::::::: :Ki7.57007.5700:::::<<<<<<<< < < < < < #<D'(Hris@:> ףp= @I + :SMDL-000045030Bioorg. Med. Chem. Lett. 12(15)-2002 2031-20344"CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1quq`ġXB)lQ3BrJ 6hx DD{1/D1ey eK /%H&JFDFdHX/XkkQfm!m D0@ 1 Sqm,:::::::::??nc:::<eP F @ : Z 4  J & V D R \ F > 4 &     , X>6.$ j 0xpfZNHBxph^P:.&:J0(Z ( h~nx f ~ l & zrhZPD<6*` 7.5700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi5.22005.22005.2200 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide<<<<<<<<<<<<<<<<< <  :<"<Ki4.84004.84004.8400 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide!<$<%<&<'<(<)<*<+<,<-<.</<0<1<2<3<4<  @<Ki8.52008.52008.5200 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideC<F<G<H<I<J<K<L<M<N<O<P<Q<R<S<T<U<V<  Ki5.97005.97005.9700 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideW<Y<Z<[<\<]<^<_<`<a<b<c<d<e<f<g<h<i<  D<X<k<D+H:w@A<(\@nE<SMDL-000045040Bioorg. Med. Chem. Lett. 12(15)-2002 2031-20345+CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OC)cc1@y  E$DTDxp $fG&(:@ dPKxʟPKkF㘤h) BjBFqiQ3=U1iUkyژa e!AL&󀴇Q 1 DSqmA@,5<7<8<9<:<><<<;<=<??nc?<B<Ki4.92004.92004.9200 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidej<l<m<n<o<p<q<r<s<t<u<v<w<x<y<z<{<|< <Ki8.86008.86008.8600 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide<<<<<<<<<<<<<<<<<< Ki6.56006.56006.5600 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine<<<<<<<<<<<<<<<<<>  <<>D-H\='ohx@<= ףp=@zG<SMDL-000045050Bioorg. Med. Chem. Lett. 12(15)-2002 2031-20346A-923,CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OCC)cc1{  E$DTDxp $fǍLQt @ ?S58* |X>6," "jbZPB0$ thioperamideKi4.90004.90004.9000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide>>>>>> > > > > >>>>>>>>   >Ki7.69007.69007.6900 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide#>&>'>(>)>*>+>,>->.>/>0>1>2>3>4>5>6>  Ki6.24006.24006.2400 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide7>9>:>;><>=>>>?>@>A>B>C>D>E>F>G>H>I>  $>8>K>D14H>M)z@!>)\(@Zd;O %>SMDL-00004506 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-20347 .CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OCCCC)cc1}T TPD!RG AC!DLDWpZlE(t Q >4<$R-ơ 4dH;>-ҌaH"R+# Ҍ0[Ӳe.Sy.S o+-CB!3!1ӽAt !IL&󀴇Q 1 DSq I ,>>>>>>>>>?? nc>"> Ki5.73005.73005.7300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideJ>L>M>N>O>P>Q>R>S>T>U>V>W>X>Y>Z>[>\> h>Ki8.30008.30008.3000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidek>n>o>p>q>r>s>t>u>v>w>x>y>z>{>|>}>~> LKi6.51006.51006.5100 receptorH1humanu membranecloned antagonistP35367humanuGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminemthioperamide>>>>>>>>>>>>>>>>>>  l>>>D/$H#Hy@i>Q@ʡEm>SMDL-00004507@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-20348@/CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OC(C)C)cc1} DAN0%HPxp$L̰Q;D+@@Ijx(~'ZWħjAc.A$~ZvA%C.%ħAa渦e\\WZfUAeUECjhhc|!\\+&󀴗Q|1 Dsqe\.,]>_>`>a>b>f>d>c>e>??Cncg>j>)C)Ki4.75004.75004.7500 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine5thioperamide>>>>>>>>>>>>>>>>>> D14H>M)z@ @zG@ @SMDL-000045080,>>>@@@@@@??L membrane@~8 JxD  T v p d Z P F @ :  hNF>4& 2 j p z J . | D  6 d vlbXRL |rhZPD:4( hP, p`6<F>~0zlbVLF:0&z @Ki8.00008.00008.0000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide @@@@@@@@@@@@@@@@@@  Ki6.56006.56006.5600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide@!@"@#@$@%@&@'@(@)@*@+@,@-@.@/@0@1@  @ @3@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-20349 0CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OCC(C)C)cc1}TPB"aDI!U>4WAVlXh!4x 1 4<>#R-+4ơ >-cH;ьơ"RcH"+-ӌ0 [Ӳe.Sy.S oB!B13!r-ӽA ![L&󀴇Q 1 DSq [ nc@ @ Ki5.43005.43005.4300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide2@4@5@6@7@8@9@:@;@<@=@>@?@@@A@B@C@D@  P@Ki8.02008.02008.0200 receptorH3rat membranecortex; brain antagonistQ9QYN8rat)GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideS@V@W@X@Y@Z@[@\@]@^@_@`@a@b@c@d@e@f@ @Ki5.92005.92005.9200 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideg@i@j@k@l@m@n@o@p@q@r@s@t@u@v@w@x@y@  T@h@{@D/,8'>9y@Q@@(\U@SMDL-0000450900Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203410/CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)NC(C)C)cc1N} DVAN0%HPx7Lа1c;F+`1Ijx(~W'ZjAc.A$~ZvA%C.%ħAa渦WZf\\fUAeUECjhhc|!a\+&󀼗q1 Dsq\a,E@G@H@I@J@N@L@K@M@??ncO@R@Ki4.95004.95004.9500 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidez@|@}@~@@@@@@@@@@@@@@@ @Ki7.67007.67007.6700 receptorH3rat@@@@@@@@@>BBBBBBBB 0 @ BBD-8HXx@@= ףp= @MbX9@SMDL-000045100Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203411,CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)NCC)cc1{ +AHPxp $fǍLTQt0@P5<?R-Q54 H;?-+A!֒RHтԂ B0s\2f.y. pӂ+-rs1!RA!.IL&󀼇q1 DSqT .I,@@@@@@@@@??nc@@@@( "   0  l H $f 4 " P~8  z t H tjdXND:4.\B:2(&^ d n > " p 8  * X |vj`VLF@@|PvhVJB<0& t*0:4"f. cortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi5.80005.80005.8000 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide B B B BBBBBBBBBBBBBBB  Ki4.63004.63004.6300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideBBB B!B"B#B$B%B&B'B(B)B*B+B,B-B.B  :BKi8.13008.13008.1300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide=B@BABBBCBDBEBFBGBHBIBJBKBLBMBNBOBPB  Ki5.98005.98005.9800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideQBSBTBUBVBWBXBYBZB[B\B]B^B_B`BaBbBcB  >BRBeBD1,8}tJy@;ByGz@?BSMDL-000045110Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034120CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)N3CCCC3)cc1恁DSPBQI!eŃ1PR`aDWlTTiq x0€0I4<>#+3R-4і rH;>-qH2RC0# \2+-S e.cy.s oR31S A! s\&󀴇ь9 D[qb s,/B1B2B3B4B8B6B5B7B??nc9B+#R-4dơ >-cH;q+ҌaH"R#Ҍ0 ++C!<[Ӳe.Sy.sC!R roB1ӽA!1\&󀴇ь9D{yj1,wByBzB{B|BB~B}BB??ncBB? Ki z n d ^ R H > 4 . ( z V < 4 , "   j pz8 .l 2 6dvpdZPF@: nf\RD:.$R:~xrZJ$l*4*hxndVL@60$dL(\xT:2*  Ki4.75004.75004.7500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideBDDDDDDD D D D D DDDDDDDKi7.67007.67007.6700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide!D$D%D&D'D(D)D*D+D,D-D.D/D0D1D2D3D4D  Ki4.58004.58004.5800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide5D7D8D9D:D;DD?D@DADBDCDDDEDFDGD  "D6DIDD)Hx@x@D{Gz@%C #DSMDL-00004513 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203414.CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)S(=O)(=O)C)cc1y *QII)R$҈7PаG%!@@I`kv('Vr(Vv)`B#/AB#%'/W']?ĹEZ\VAeVija} !zǝ̿ÃtQ 1)DSq) z ,DDDDDDDDD?? ncD D Ki4.08004.08004.0800 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideHDJDKDLDMDNDODPDQDRDSDTDUDVDWDXDYDZD  fDKi7.90007.90007.9000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideiDlDmDnDoDpDqDrDsDtDuDvDwDxDyDzD{D|D gKi4.95004.95004.9500 receptorH1humano membranecloned antagonistP35367humantGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide}DDDDDDDDDDDDDDDDDD C jD~DDD-$HQ,z@gD(\@V-kDSMDL-00004514o0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034152CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)S(=O)(=O)C(C)C)cc1} D D QS"IR7R@;"CQ١ |&׹ZFʡY\ 5F j,jt㊖1ksU\Y ١U-!2!ǝܿvь9)D[q)lh,[D]D^D_D`DdDbDaDcD??nceDhDRKi4.68004.68004.6800 receptorH2human, membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideDDDDDDDDDDDDDDDDDD rD5 Ho\':~@F333333@K7 FSMDL-000045150Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203416,DDDDDFFFF??ineX& ^ | r h b \ 0 | n d X N H < 2 (    | d@&  t F L V " V   @ vj`ZND:0*$ldZPB8,"P8|vpXHj&f~tj\RF<6*   FKi7.43007.43007.4300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide F F FFFFFFFFFFFFFFFF  Ki4.87004.87004.8700 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideFF F!F"F#F$F%F&F'F(F)F*F+F,F-F.F/F  FF1F:CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)S(=O)(=O)c3ccc(C#N)cc3)cc1&2PBQ ԀeE\DQEKlE_aMHC0Q0cԊaF?F@FAFBF  NFKi7.44007.44007.4400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideQFTFUFVFWFXFYFZF[F\F]F^F_F`FaFbFcFdF Ki6.54006.54006.5400 receptorH1human membranecloned antagonistP35367human@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideeFgFhFiFjFkFlFmFnFoFpFqFrFsFtFuFvFwF  RFfFyFD58(iz@OFQ@ rhSFSMDL-00004516@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034171CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3ccccc3)cc1rT "PAaDHEC!DLPUl]ءTЁCL %S=Mu7BX+k1e^=6BSuMX +4.(@|PvhVJB<0& t" 8  membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi7.13007.13007.1300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide H HHHHHHHHHHHHHHHHH  F HHKi4.83004.83004.8300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideH H!H"H#H$H%H&H'H(H)H*H+H,H-H.H/H0H  AHSMDL-000045180Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034193CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3ccc(C)s3)cc13 UQ,!QD)BaEM1DaF(q^pQD 0 OմY2EucO!>{v#EYż2sc#$m1%b2v$mdzʣc&s$$D3}3ʳsؔ$42@!=|+06ў9T[q=,1H3H4H5H6H:H8H7H9H??nc;H>HKi5.09005.09005.0900 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidefHhHiHjHkHlHmHnHoHpHqHrHsHtHuHvHwHxH HKi7.53007.53007.5300 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideHHHHHHHHHHHHHHHHHH Ki7.10007.10007.1000 receptorH1human0 membranecloned antagonistP35367humanGPCRhistaminergic receptorHHHHHHHHHHHHHHHHJJ  HHJD18^.;|@H@y&1,HSMDL-000045190Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034202CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3sccc3Cl)cc1!D`AUQ,PC)baEM1EDRt[(^pEqգ 0 H <(1~q z2ߦ-a"w27zr%5q rɖlF<l(c &ARqYw &htl 9|' ! 0Ѿ;]{qXv0,yH{H|H}H~HHHHH??ncHH?5.0500Ki| v l b X R L z ` X P F 8 &   D f lv( *\ " 2`" ~tjd^2 vl^TH>8,"lT0tdHNX H B~pfZPJ>4* ~X4h`F>6, ![3H]-(R)-Nalpha-methylhistamine thioperamideKi4.71004.71004.7100 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideJJJJJ J J J J JJJJJJJJJ  !JKi7.98007.98007.9800 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide$J'J(J)J*J+J,J-J.J/J0J1J2J3J4J5J6J7J  Ki6.40006.40006.4000 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide8J:J;JJ?J@JAJBJCJDJEJFJGJHJIJJJ  %J9JLJD1Hfʉy@"Jffffff @V-&JSMDL-00004520 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034210CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3ccco3)cc1恁DTC! %TQIBaEK)DaF\E[p,6Dt A@Z2dTPՄw#EżBZŻsP!d#m1?{E»̃wشmC3&D$t$dÔC$$2 !\6ю9D{}  ,JJJJJJJJJ?? nc J#J Ki4.70004.70004.7000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKJMJNJOJPJQJRJSJTJUJVJWJXJYJZJ[J\J]J iJKi8.07008.07008.0700 receptorH3rat membranecortex; brainJ antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidelJoJpJqJrJsJtJuJvJwJxJyJzJ{J|J}J~JJ Ki6.98006.98006.9800 receptorH1human membranecloned antagonistP35367humanaGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideJJJJJJJJJJJJJJJJJJ  mJJJD3H->z@jJ@1ZdnJSMDL-000045210Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034221CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3occc3C)cc1`BEUT D-PC)BaEM1DaD(q^pEbЁ q4iTAUaA9ލPi Z ж# 2aӶ*ϠZǚ",yf=[ S*=+dcd!|6Ѿ9D{}HCc,^J`JaJbJcJgJeJdJfJ??nchJkJKi4.89004.89004.8900 receptorH2human membranecloned antagonistP25021humaniGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineethioperamideJJJJJJJJJJJJJJJJJJ ,JLLLLLLLL??0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034L`,Z~ Z @ 8 . $  $&  x n h b 6 vnf\N<0("  Z  r h D l : ( p 8ztH~th^XLB8.("tP6.&^dn2"d,*Xzpj^TJ@:4$  LKi8.39008.39008.3900 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide LLLLLLLLLLLLLLLLL L  Ki7.25007.25007.2500 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide!L#L$L%L&L'L(L)L*L+L,L-L.L/L0L1L2L3L  L"L5LD38K7z@ L ףp= @nLSMDL-00004522 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034231CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3cccn3C)cc1 PQ FQ,PC)BaEM1DQ[(^pa €4X̃ Aq 1/r|Ílm ahd?h%|Qc5q (JPTiq] Z&| ) !R|6Ѿ9D{y fR nc L L Ki4.93004.93004.9300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide4L6L7L8L9L:L;LL?L@LALBLCLDLELFL  RLKi7.35007.35007.3500 receptorH3rat2 membranecortex; brain@ antagonistQ9QYN8ratQGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideULXLYLZL[L\L]L^L_L`LaLbLcLdLeLfLgLhL eKi5.37005.37005.3700 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideiLkLlLmLnLoLpLqLrLsLtLuLvLwLxLyLzL{L  VLjL}LD/HW`Vy@SLHzG@Q8WLSMDL-000045230Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034240CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3cnco3)cc1恁!QAUQ,PC)BaEM1DaJ\E[p1fD(t0@Hs57'|̷y2`q̋<͖`jƁF&&[b[iK<lXh'ARqYw &htl 9|' !?Ѯ9E{}^,GLILJLKLLLPLNLMLOL??ncQLTLKi4.56004.56004.5600 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide|L~LLLLLLLLLLLLLLLLL QL .D/!9ʉvy@LQ@33333NSMDL-0000452460Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034253CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3cnc[nH]3)cc16恁!QAUQ,PC)BaEM1DaJ\E[p1fD(t@a Hs57'|̷y2`q̋<͖`jƁF&&[b[iK<lXh'ARqYw &htl 9|' 6!??9[y0?-,LLLLLLLLL??6ncLL!.5L&Q 1 DSq F,NATNBTNETDTCTLrzNh 8b >H 6 p 2 v n d Z L B 6 , &    Z Z6 j pd\VJ@6,&    z n \  lH.&|@|PvhVJB<0& tfTB Ki8.35008.35008.3500 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideLNNNNNN N N N N NNNNNNNKi6.28006.28006.2800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideNNNNNNNNNNN N!N"N#N$N%N&N  NN(NKi4.71004.71004.7100 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide'N)N*N+N,N-N.N/N0N1N2N3N4N5N6N7N8N9N  ENKi7.74007.74007.7400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideHNKNLNMNNNONPNQNRNSNTNUNVNWNXNYNZN[N  Ki5.69005.69005.6900 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide\N^N_N`NaNbNcNdNeNfNgNhNiNjNkNlNmNnN  IN]NpND1!9)"Èz@FNGzG@A`"JNSMDL-00004525i0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034261CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3cnccn3)cc1@TDCB !NR^!DDTE a^pх3ԅQs 0 | QK˘ Ílm  q̮irDlqFF\;l$Ʊc @Qq .'Tt`|Aw=·q@` @!Hь9E[y H,:NN?NCNAN@NBN??ncDNGNKi4.33004.33004.3300 receptorH2human@ membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideoNqNrNsNtNuNvNwNxNyNzN{N|N}N~NNNN NNKi7.28007.28007.2800 receptorH3rat membranecortex; brain0 antagonistQ9QYN8ratnGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideNNNNNNNNNNNNNNNNNN m ( NPPD3 8|yxz@NQ @OnNSMDL-000045260Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034271CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3ccccn3)cc1TP B eHD*TB4YhT\n#Tbp(T˃dQKG0.clm p#gddir&[QQKǎqX1PFTiq Iw F\l]!|ϧmRq@` 2!g\&ь9D[yCdgc,NNNNNNNNN??ncNN26D/$8.9(Hx@T@;v TSMDL-00004530NSMDL-0000453132??xf * | X > 6 . $   2 "    @  x r f \ R H B <  |bZPF8."F. |rlfN>& `, 6  \ tlbXJ@4*$X2ztnBzpbPD<6*   Ki6.38006.38006.3800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideNPPPPPPP P P P P PPPPPPKi4.73004.73004.7300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidePPPPPPPPPPPP P!P"P#P$P%P  1PKi7.69007.69007.6900 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide4P7P8P9P:P;PP?P@PAPBPCPDPEPFPGP  Ki6.14006.14006.1400 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideHPJPKPLPMPNPOPPPQPRPSPTPUPVPWPXPYPZP  5PIP\PD3 8|yxz@2PQ@K7A`6PSMDL-00004527@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034281CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3cccnc3)cc1iSPBAhD"@VD!Th1 FTE^lTr @(U˃d7G-aÍlm Fagd ir&[QQĶ˘ ;lXh@Qq7'Tt`|Aw| )!x&ь9E[qdx,&P(P)P*P+P/P-P,P.P??nc0P3PKi4.22004.22004.2200 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide[P]P^P_P`PaPbPcPdPePfPgPhPiPjPkPlPmP QDC/Q+lKr 644:1%p["n : p$^KCG%*-8URO^o(b Fd`edl,X&Hd5s AZBRhb6<X*xZ\_J[oVah';`2HDlHjzz c[iA[  U)~~[&mΗg+R 9$GItHtJtߊ-O= Q *3WR <ҸrKt  iqRX.?Htr2pRT+3T/3 m32{WAspȌpʌNT© o}&=Z˕>KLs/=Ϧ)  D3 8|yxz@RQ@K7A` RSMDL-000045280Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203429T "PA\DHDTB4[d! &D^pEB P(T˃dQK͖`,7A||Kir&[QQKǎqX1PFTiq̮ .'5}sq Y| )!Wg\&ь9 D[q0dWg-,nPpPqPrPsPRuPtPvP??31,xPNNJzPTTLT???* v R t b  ~|X>6," " xnd^X,ld\RD2& PhfBb0n. vpj>~tj\RF<6*   {{QDN/wP<^z%b sTRKi8.20008.20008.2000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideR R R R RRRRRRRRRRRRRR  Ki6.32006.32006.3200 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideRRRR R!R"R#R$R%R&R'R(R)R*R+R,R-R  RR/R1CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)c3ccncc3)cc1 ncRR Ki4.65004.65004.6500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide.R0R1R2R3R4R5R6R7R8R9R:R;RR?R@R  LRKi8.50008.50008.5000 receptorH3rat membranecortex; braina antagonistQ9QYN8ratPGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminehthioperamideORRRSRTRURVRWRXRYRZR[R\R]R^R_R`RaRbR Ki5.72005.72005.7200 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidecReRfRgRhRiRjRkRlRmRnRoRpRqRrRsRtRuR  PRdRwRD-8gL2rhw@MRGz @ ףp=QRSMDL-000045290Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203430+CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)CC)cc1y D CB!$Sf8r8" $dA%*:@ d!|J K` Bp#/OBlmf/1nkY)d &m kbI_'0|`w=sq(Ɓ)!2L&Q 1 DSq2,ARCRDRERFRJRHRGRIR??ncKRNRRKi4.50004.50004.5000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidevRxRyRzR{R|R}R~RRRRRRRRRRR * | r l f : x l b \ P F < 2 , & x T : 2 *    P V ` 6  d 0  J ~tnbXND>8 2ztnBzrhZH<4."f"(2 TKi8.19008.19008.1900 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideT T T T TTTTTTTTTTTTTT  Ki6.06006.06006.0600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideTTTT T!T"T#T$T%T&T'T(T)T*T+T,T-T  TT/T,CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)CCC)cc1{ D CB!$Sf8r8" $dШGKT"t @;|40N-\#0FVh4rۂ\b>ר`F8׬*36a>-`3p.λ 60sSЙ5  .5 nc{PTKi4.64004.64004.6400 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide.T0T1T2T3T4T5T6T7T8T9T:T;TT?T@T  GTKi8.35008.35008.3500 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideJTMTNTOTPTQTRTSTTTUTVTWTXTYTZT[T\T]T  Ki5.40005.40005.4000 receptorH1humanT membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide^T`TaTbTcTdTeTfTgThTiTjTkTlTmTnToTpT  KT_TrTD/$8.9(Hx@HT ףp= @K7A`LT0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034.CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)C(C)C)cc1{ D EDHNxp $fPQcG"t @;|40N-|n052AVdm 6sX^ǂk0m<(_48-`3p.)A.,6 LAn!F\&ь9 D[qncFTITeptKi4.53004.53004.5300 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineTthioperamideqTsTtTuTvTwTxTyTzT{T|T}T~TTTTTT TKi8.67008.67008.6700 receptorH3rat@ membranecortex; brain antagonistQ9QYN8rateGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideTTTTTTTTTTTTTTTTTT (  TVVD/8ݟ(x@TGz@=OTSMDL-000045320Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203433.CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)C3CC3)cc1} DQ^P#'Re#RD4pqcGdTyPYAA:cj^Βa>r Lymk0:P#4 F--%Cz 6|`| 8k㼻cͻ 6,sS!\&ь9 D[q0,TTTTTTTTT??ncTT5.05005.0500@~ z n f ` T J @ 6 0 *  h$ nxF ,v @  4bv R 8 0 &     `F>4**tj`VPJ2" D x @rXPF<.$<@|PvhVJB<0& t* Ki5.75005.75005.7500 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideTVVVVVVV V V V V VVVVVVKi4.50004.50004.5000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideVVVVVVVVVVVV V!V"V#V$V%V  1VKi8.50008.50008.5000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide4V7V8V9V:V;VV?V@VAVBVCVDVEVFVGV  Ki6.45006.45006.4500 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideHVJVKVLVMVNVOVPVQVRVSVTVUVVVWVXVYVZV  5VIV\VD1$8Y y@2V ףp= @Q6VSMDL-00004533@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203434/CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)C3CCC3)cc1@}T "PAaDHEC!EXTRSX[XT5B)0 |ƙr5ÍtơF&,)O0lmF.1jkXc mkP_g`w`a2hwlY| !Q\&ь9 D[qVQ,&V(V)V*V+V/V-V,V.V??nc0V3VKi4.99004.99004.9900 receptorH2human membranecloned antagonistP25021humanVGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide[V]V^V_V`VaVbVcVdVeVfVgVhViVjVkVlVmV 0yVKi8.00008.00008.0000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide|VVVVVVVVVVVVVVVVVV Ki7.25007.25007.2500 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideVVVVVVVVVVVVVVVVVV  }VVVD7$8Z֗I{@zVQ@/$~VSMDL-000045340Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034352CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)Cc3ccccc3)cc1єF,$HPA"aDI!U>4WAY[dGBSއK FB5XA񬠱q!rAV9F)V[PK76lL Zh=l6UǙ^G=5lv 2 '},hФb:6!=Z\8&<1 Dsq=Z,nVpVqVrVsVwVuVtVvV??ncxV{VVV>BHTTXXXXXXXX X X X X  ^ :    n  t h ` Z N D : 0 * $  r `  pL2*  xnd^X,ld\RD2& PhZ6b0b. vpj>~tj\RF<6*    receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideXKi7.96007.96007.9600 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideXXX X!X"X#X$X%X&X'X(X)X*X+X,X-X.X  Ki5.96005.96005.9600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide/X1X2X3X4X5X6X7X8X9X:X;XX?X@XAX  X0XCXD/$8I3MIz@X@ffffffXSMDL-00004535 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203436-CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)CSCC)cc1 } D CB!$Sj8r(CĈ7HЈacG:(@06XA񠠱qlAm q72rdl9F6`Ʃ2&(0k6ƙ^G5lvw=q>J €) ! AL&Q 1TSq  A , XXXXXXXXX?? ncXX Ki4.64004.64004.6400 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideBXDXEXFXGXHXIXJXKXLXMXNXOXPXQXRXSXTX  `XKi7.24007.24007.2400 receptorH3rat membranecortex; brain$ antagonistQ9QYN8ratfGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine(thioperamidecXfXgXhXiXjXkXlXmXnXoXpXqXrXsXtXuXvX 6Ki4.67004.67004.6700 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidewXyXzX{X|X}X~XXXXXXXXXXXX  dXxXXD/$H#Hy@aX\(\ @o= ףpeXSMDL-000045360Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034371CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)C(C)(C)O)cc1h} DW',%HR9F(A;بe@@Jr@@Y[-M3R4Y8oL3YsH$>Gd/7$Ysοb8˘5.|?2/!_\&={}_ ,UXWXXXYXZX^X\X[X]X??nc_XbX$HKi4.61004.61004.6100 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideXXXXXXXXXXXXXXXXXX  D-$(v@ZzG@ rhZSMDL-000045370Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203438w CC9 * xAC2fqFPU Açʝ6`Z?Z  KZKi7.80007.80007.8000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideNZQZRZSZTZUZVZWZXZYZZZ[Z\Z]Z^Z_Z`ZaZ  Ki5.65005.65005.6500 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidebZdZeZfZgZhZiZjZkZlZmZnZoZpZqZrZsZtZ @ OZcZvZD/$(9J^Hw@LZQ@(\PZSMDL-000045380Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203439*CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1{QN, a$PX7LаGJ:h%p!9KFLr @Sn6\Nr8ԈQ#Y#5Mh z8Ἳcjͻ5,s?!m3 \809 DSq m3,@ZBZCZDZEZIZGZFZHZ??ncJZMZKi4.73004.73004.7300 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamideuZwZxZyZzZ{Z|Z}Z~ZZZZZZZZZZ ZZKi7.87007.87007.8700 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamideZZZZZZZZZZZZZZZZZZ Ki6.18006.18006.1800 receptorH1human membranecloned  \D/4(eu$iw@ZzG@xZSMDL-000045390Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203440(CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1y CC9 * xAC2fa < %O;-mXyrpF;-si sd5@h4̃5ጯy:P 0Gj+>0s?Й5!N L0@ 1 DSqN,ZZZZZZZZZ??ncZZZ go v l b \ V j b Z P B 0 $   N d jtP (z J   0^,  ~ t n h < |pf`TJ@60*|X>6.$"R X b : f4 L xrf\RHB<@|PvhVJB<0& t&,6 z antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideZZZZZZZZZZZ\\\\\\\ Z\ \Ki5.12005.12005.1200 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide \ \ \\\\\\\\\\\\\\\\  (\Ki8.03008.03008.0300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide+\.\/\0\1\2\3\4\5\6\7\8\9\:\;\<\=\>\  Ki6.34006.34006.3400 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide?\A\B\C\D\E\F\G\H\I\J\K\L\M\N\O\P\Q\  ,\@\S\D/4(eu$iw@)\(\@ffffff-\SMDL-00004540 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203441*CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1yCC= *T*U261fA  < 3N;-mXyrpF;- c855siZ$ 0֬#N 0Zj+>/cf4 @i!T \809 DSqtTi,\\ \!\"\&\$\#\%\??hnc'\*\\Ki5.02005.02005.0200 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideR\T\U\V\W\X\Y\Z\[\\\]\^\_\`\a\b\c\d\ p\Ki7.78007.78007.7800 receptorH3rat membranecortex; brain( antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamides\v\w\x\y\z\{\|\}\~\\\\\\\\\ Ki7.22007.22007.2200 receptorH1human membranecloned antagonistP35367human.GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide\\\\\\\\\\\\\\\\\\  t\\\D/ (F=Dy@q\Q@jtu\SMDL-000045410Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203442,CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1}PQDC qD5SO]!DETV`[ CO- @@X 7 (ڒÉ2ɝ6`Ћ<͓؆k(iAq h$kcI<`)U{=u`VIwqB!h\04ծ9 TSq` h,e\g\h\i\j\n\l\k\m\??nco\r\\Ki5.15005.15005.1500 receptorH2human membranecloned antagonistP25021\\\\\\\\\\\\\^^^^^ @  z p j ^ T J @ : 4  b H @ 8 .    , p v D 4 r  > < j |pf\RLF~tf\PF@4*  t\8|l06@F*xnbXRF<2("hD*"x human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide^Ki8.30008.30008.3000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide^^^^^^^^^^ ^!^"^#^$^%^&^'^  Ki5.65005.65005.6500 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide(^*^+^,^-^.^/^0^1^2^3^4^5^6^7^8^9^:^  ^)^<^D%ԠH?:ut@^@On^SMDL-00004542 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203448(CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C)CC1us  E$"$TDxh $f!X)RP xKڕQ@L*/\x@wQ V;*+;K:@K*;V@/L:@@-/;QK !9L&󀴇Q  DSq  9 ,^^ ^ ^ ^^ ^ ^^?? nc^^ Ki4.40004.40004.4000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide;^=^>^?^@^A^B^C^D^E^F^G^H^I^J^K^L^M^  Y^Ki8.27008.27008.2700 receptorH3rat@ membranecortex; brain antagonistQ9QYN8ratiGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineCthioperamide\^_^`^a^b^c^d^e^f^g^h^i^j^k^l^m^n^o^ Ki5.78005.78005.7800 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidep^r^s^t^u^v^w^x^y^z^{^|^}^~^^^^^  ]^q^^D'Ha"u@Z^Q@= ףp= ^^SMDL-000045430Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203449)CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)CC)CC1h{u  E$"$TDxh $fqCR61ow<<>r=}ƺv3>ז.9tVt>w^ms&,!<L&󀴇Q  DSq <^,N^P^Q^R^S^W^U^T^V^??ncX^[^Ki4.25004.25004.2500 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide^^^^^^^^^^^^^^^^^^ ^ rD14H>M)z@^)\(@Zd;O `SMDL-00004544@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203450.CCCCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OCC)cc1}T TPDRG AŃ !DLDZlWd!0x Q p~ɷt#'e tx~7#(ṱU־7kɷ½v ֛v 66a#齦Wf W'!IL&󀴇Q 1 DSqeIn,^^^^^^^^^??nc^^ D5.85005.85005.8500.8500zp Z `j2 b , &T ~ t h ^ X L B 8 . ( " xpf\ND8.(\ D |d T v   . r  xn`VJ@:.$ n|bZPF8."F. |rlfN>`\P, Ki8.43008.43008.4300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide^`````` ` ` ` ` ```````Ki6.25006.25006.2500 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide``````````` `!`"`#`$`%`&`  ``(`Ki5.67005.67005.6700 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide'`)`*`+`,`-`.`/`0`1`2`3`4`5`6`7`8`9`  E`Ki8.10008.10008.1000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideH`K`L`M`N`O`P`Q`R`S`T`U`V`W`X`Y`Z`[`  Ki6.30006.30006.3000 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide\`^`_```a`b`c`d`e`f`g`h`i`j`k`l`m`n`  I`]`p`D3DH잼 {@F`Q@A`"J`SMDL-00004545i0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203451/CCCCCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OCC)cc1 T TPDRG AŃ !DLDZpX\#BD4S|^DǬd`^5Z: OVXk9ff%k&Ly\faǕ`>ҮMg^]`Ԯ+#ӽwq`~E&`Iy!LL&󀴇Q 1 DSqL,:`<`=`>`?`C`A`@`B`??ncD`G`Ki5.57005.57005.5700 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamideo`q`r`s`t`u`v`w`x`y`z`{`|`}`~```` ``Ki8.33008.33008.3300 receptorH3rat@ membranecortex; braine antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide`````````````````` mKi```^^^bbbbbbbb b b b b  ``bD)HPv@`Q @/$ `SMDL-000045460Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203452,CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1y  Fj($T("&R%$'j#3R )|7`DZ:?j`aYq`w8)XqDOk Zňka||mkm` qkZq{q5kU6|!\&󀴇  D[q,`````````??nc```  re, & 2 x T : 2 *   ~ n B h 6 $ Jx ~ t n b X N D > 8 |bZPF8."F. |rlfN>" `( 2 \ tlbXJ@4*$X2ztnBzpbPD<6*    receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi4.10004.10004.1000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide bbbbbbbbbbbbbbbbbb  *bKi7.60007.60007.6000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide-b0b1b2b3b4b5b6b7b8b9b:b;bb?b@b  Ki6.22006.22006.2200 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideAbCbDbEbFbGbHbIbJbKbLbMbNbObPbQbRbSb  .bBbUbD/Hh(y@+byGz@ʡE/bSMDL-00004547 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203453/CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CCCCC3)CC1 }QS TP !QG!%DAHVPROdU[ L m\@C1_- k}dřu-5_  >yzsk "}dZpp3]i=yz|kMUUM ![\&󀴇  D[q [ , b"b#b$b%b)b'b&b(b??enc^,bKi5.10005.10005.1000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideTbVbWbXbYbZb[b\b]b^b_b`babbbcbdbebfb rbKi8.14008.14008.1400 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine1thioperamideubxbybzb{b|b}b~bbbbbbbbbbb  Ki6.03006.03006.0300 receptorH1humana membranecloned antagonistP35367human8GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineithioperamidebbbbbbbbbbbbbbbbbb  vbbbD+H:w@sb@ ףp=wbSMDL-000045480Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203454-CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)CC(C)C)CC1y D W 5bP "7Rxa,:` e8[Ȋ3[k<}*k_;D\{[^[;f]Ҋ{܋֚]|˫!{W\8&󀴗Q1 Dsq{W,gbibjbkblbpbnbmbob??Wncqbtb?WKi4.16004.16004.1600 receptorH2human membranecloned antagonistP25021humaniGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidebbbbbbbbbbbbbbbbbb ??t??t| ~ t f \ P F @ 4 *   t n T L B 8 *   8 xnd^X@ 0 R   N f^TJ<2& J\8 lrf^XLB8.(" pp^nJ0(~v\TJ@2(  dKi8.44008.44008.4400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidedddddddddddddddd d!d  Ki6.13006.13006.1300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide"d$d%d&d'd(d)d*d+d,d-d.d/d0d1d2d3d4d  d#d6dD)H;Nёv@ dp= ף @"~j dSMDL-00004549 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203455*CCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)OCC)cc1w  E$"$TDxh $fq` HAm2_-~d ku-5_  >sk}d "Zp3ƭp]i=yzM|kUU !.?L&󀴇Q 1 DSq .? ,bdddd ddddnc d d Ki4.65004.65004.6500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide5d7d8d9d:d;dd?d@dAdBdCdDdEdFdGd  RdKi7.41007.41007.4100 receptorH3rat- membranecortex; brainC antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideUdXdYdZd[d\d]d^d_d`dadbdcdddedfdgdhd @Ki6.45006.45006.4500 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideidkdldmdndodpdqdrdsdtdudvdwdxdydzd{d  Vdjd}dD+Hh|gw@SdHzG @x&1WdSMDL-000045500Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203456.CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C=C(C)C)CC1y   *Ta#b4r@Q< ^e8[Ȋ3[k:}:*k_D\{[^;f[]Ҋ{܋|]̫!r\&󀴗Q Dsqdr@,bIdJdKdLdPdNdMdOdncQdTdKi4.66004.66004.6600 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide|d~ddddddddddddddddd dddHffffffff f f f f fff fD)HPv@d @X9v dSMDL-000045510Bioorg. Med. Chem. Lett. 12(15)-2002 2031-203457-CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C(=C)C)CC1w  jPa#b4p#G# @I2`eBk{eve5F`A>!~kUtkͶeE#[qU4q-讕juű{ W!i\&󀴇 D[qi,ddddddddd??ncdddF L @  V 2z H 6 ^ n T L B 8 *   8 \8 l rf^XLB8.("   ^ p ^  nJ0(~@|PvhVJB<0& t^:TBf 7.26007.26007.2600 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi6.01006.01006.0100 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideffffffffffffff f!f"f#f  df%fKi4.65004.65004.6500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide$f&f'f(f)f*f+f,f-f.f/f0f1f2f3f4f5f6f  BfKi7.16007.16007.1600 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideEfHfIfJfKfLfMfNfOfPfQfRfSfTfUfVfWfXf  Ki6.03006.03006.0300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideYf[f\f]f^f_f`fafbfcfdfefffgfhfifjfkf  FfZfmfD1H:Hy@Cf333333@/$GfSMDL-000045520Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034580CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)Cc3ccccc3)CC1恁QS TPC "фG!%I@T\QEEu80ut Q$Npɗy#ՖG yx# 4۾Vѭ֖oɗǽV V׽7f#w\ɇ%t!=d\8&󀴗 Dsqn=dh,7f9f:f;ff=f?f??fncAfDfKi4.90004.90004.9000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidelfnfofpfqfrfsftfufvfwfxfyfzf{f|f}f~f fKi7.17007.17007.1700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideffffffffffffffffff @Ki6.68006.68006.6800 receptorH1human membranecloned antagonistP35367humanGPCRfffffffffffffffhhh hD/ܠHVy@fGz@/$fSMDL-000045530Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034592CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)c3ccc(F)cc3)CC1QS !HPA rRBTCN8DdQt1<8Ex a$\ 2O7#hTq0Zr \Sqjm$(k.Yw%%kLA|{vWq c{%HqҮIP'h]RkZ)!\&  D[q\,fffffffff??ncfff io z ~ t f T H @ : . $    r l r|4 0h . 8fP ,  ` vpdZPF@:hNF>4&2v|J:|DBpvlbXRL lRJ@6(>6~vndVD80* histaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide ffhKi4.37004.37004.3700 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidehhh h h h h hhhhhhhhhhh  #hKi7.60007.60007.6000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide&h)h*h+h,h-h.h/h0h1h2h3h4h5h6h7h8h9h  Ki5.99005.99005.9900 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide:hh?h@hAhBhChDhEhFhGhHhIhJhKhLh  'h;hNhD/ԠH@p ${@$hzG@n(hSMDL-00004554 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034603CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)c3cccc(F)c3F)CC1 0a1!ThQE`:`]T1цZHņEQԁđDYM \<ɇ3]kF%smSqXkhf%k]>3ZWc{%kT ZUķkNծ9.#h$ !&L{q  ,hhhhh!hhh h?? nc"h%h Ki4.76004.76004.7600 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideMhOhPhQhRhShThUhVhWhXhYhZh[h\h]h^h_h khKi7.23007.23007.2300 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine1thioperamidenhqhrhshthuhvhwhxhyhzh{h|h}h~hhhh Ki6.35006.35006.3500 receptorH1humani membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidehhhhhhhhhhhhhhhhhh  ohhhD1HUN{@lhGz@S㥛phSMDL-000045550Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034613CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)c3ccc(SC)cc3)CC1QS !HPA rRBT$2DDdSDBP @D 5X:Ռ ZQIf F%WsN9?#ȬZ  jKi7.40007.40007.4000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidejjjjjjjjjjjjjjjj j!j  Ki6.09006.09006.0900 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide"j$j%j&j'j(j)j*j+j,j-j.j/j0j1j2j3j4j  j#j6jD1X0L Fz@ j333333@/$jSMDL-00004556 0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034623CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)c3ccc(OC)cc3)CC1 QS !HPA rRBP M8Xp!EQlC  @`$W3kD'%`^5Z: OVXkpNZQ9?f$kWyUqWHf7UyuqŹR殌 9kI !\&󀴇  D[q  ,hjjjj jjjjnc j j Ki5.08005.08005.0800 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide5j7j8j9j:j;jj?j@jAjBjCjDjEjFjGj  QjKi7.88007.88007.8800 receptorH3rat2 membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminepthioperamideTjWjXjYjZj[j\j]j^j_j`jajbjcjdjejfjgj @Ki6.25006.25006.2500 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidehjjjkjljmjnjojpjqjrjsjtjujvjwjxjyjzj  Ujij|jD7$HaI|@RjQ@x&1Vj0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034639CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)c3ccc(cc3)C(C)(C)C)CC1eaTCDC `C]RBlaDdGE`LCE=@ 5X:Ռ ZQp &%Gqtޮy5Sq>pӵg`<]9ffkQ0qǕ`VHf7Uyuq򑃸F+k&!\_&  D[q,hIjhJjKjOjMjLjNjncPjSjKi5.81005.81005.8100 receptorH2humanj membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine.thioperamide{j}j~jjjjjjjjjjjjjjjj j .D1H:Hy@j{Gz@xlSMDL-00004558.0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034642CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)c3cccc(C)c3)CC1恁aN1$HPA4%X(aDETAY!RpA8Et a(`$3hkr fU`5< vZl>ci|j3{g`^ -Uq\ ZUSk߮9.#h|!g|8&󀴇1D[qg@,jjjjjjjjj??ncjjD+jjDjDlljz d jt. (b ( 0^ z p d Z T H > 4 * $  fLD:0" 0 zpf\VP8 ( J  F x^VLB4*B@|PvhVJB<0& thTB Ki6.54006.54006.5400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidejllllll l l l l lllllllKi6.42006.42006.4200 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidelllllllllll l!l"l#l$l%l&l  ll(lKi5.43005.43005.4300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide'l)l*l+l,l-l.l/l0l1l2l3l4l5l6l7l8l9l  Ki8.20008.20008.2000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideFlIlJlKlLlMlNlOlPlQlRlSlTlUlVlWlXlYl  Ki6.37006.37006.3700 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideZl\l]l^l_l`lalblcldlelflglhliljlklll  Gl[lnlD1HƊLCxz@jQ @㥛 HlSMDL-00004559x0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034654CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)/C=C/c3cccnc3)CC1QTG Ҡ Aa!QRBDayxEvą3Tc q,$X3\)DǬOZY5רT3`Ak$Z)Dɧ$g`"Wy\ fakzSřWg8xkԮ+#H'qI!hL&󀴇Q DSqbh,:ll?lClAl@lBl??absjElKi4.60004.60004.6000 receptorH2human membranecloned antagonistP25021human@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidemlolplqlrlsltlulvlwlxlylzl{l|l}l~ll +5ll1CCllKi8.14008.14008.1400 receptorH3rat@ membranecortex; brain antagonistQ9QYN8rat@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidellllllllllllllllll e @ lnnD5X"2H|@lp= ף@I +lSMDL-00004560@0Bioorg. Med. Chem. Lett. 12(15)-2002 2031-2034668CCOC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)/C=C/c3ccc(OC)cc3)CC1QSG Ҡ AU)BpDBхSlE_ N aP q M3#(%Tq*kir%%0sMű<#Z𘯡Atg`KZ`IwF` āF-UQuqzAP_8|I!L&󀴇Q DSqe.,lllllllll??absllDS,prrrrrrrr2* SMDL-000045683??3@zrD< j P H @ 6 (   D 4 ,4>  R & z p j ^ T J @ : 4  v\TJ@2( @(vlf`H8" * V tlbXJ@4*$X2ztnBzpbPD<6*   Ki6.21006.21006.2100 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidelnnnnnnn n n n n nnnnnnKi5.17005.17005.1700 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidennnnnnnnnnnn n!n"n#n$n%n  + 0n3n 1n5nKi8.91008.91008.9100 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide7n:n;nn?n@nAnBnCnDnEnFnGnHnInJn  Ki5.17005.17005.1700 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKnMnNnOnPnQnRnSnTnUnVnWnXnYnZn[n\n]n  8nLn_nD7\Xsᒚ~@2n(\@L9nSMDL-00004561a0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20372@ACCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](C)NC(=O)OC(C)(C)C)cc1 6ADAH5D4PB!rDE6TRd\O<bTԓ Ba JDf frǚŚe9ƚfd=yզ~ XrmOar!+򀼿={y0,qnsntnunvnznxnwnyn??abs6nn? 64.3300ratx | t j ` R H < 2 ,   ` H $  h X `hr` v f p  $J  v ,ZtlbXJ@4*$X 6~xrF~vl^L@82&jv|J8. vpj>~tj\RF<6*   Ki4.64004.64004.6400 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidenppppppp p p p p pppppp+ p p p"pKi7.83007.83007.8300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide$p'p(p)p*p+p,p-p.p/p0p1p2p3p4p5p6p7p  Ki5.48005.48005.4800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide8p:p;pp?p@pApBpCpDpEpFpGpHpIpJp  %p9pLpD;|X:f-@pQ@Q8&pSMDL-00004563 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20374 DCCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)cc1VQDDH5D J@8PB%rE6ZTTXpDO<TlAcHEA  Q ơ4Y0LgqĶJ6^ĖT7@g'ӫtJv{q637fɹt{56^&uu- 77V,gTܹǦF! !r|+_&򀼷={y r ,ppppppppp?? abs !p#p Ki4.87004.87004.8700 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideKpMpNpOpPpQpRpSpTpUpVpWpXpYpZp[p\p]p +hpkppipmpKi7.01007.01007.0100 receptorH3rat membranecortex; brain6 antagonistQ9QYN8rat1GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine]thioperamideoprpsptpupvpwpxpypzp{p|p}p~ppppp Ki4.97004.97004.9700 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamidepppppppppppppppppp  ppppD;|X:f-@jpQ@Q8qpSMDL-000045640Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20375ECCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)cc1VQDDH5D J@8PB%rE6ZTTXpDO<TlAcHEA  Q ơ4Y0LgqĶJ6^ĖT7@g'ӫtJv{q637fɹt{56^&uu- 77V,gTܹǦF!!r|+_&򀼷={yr,^p`papbpcpgpepdpfp??abslpnpKi4.90004.90004.9000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidepppppppppppppppppp ??  v l ` V P D : 0 &  T 0    d |j^VPD:0&       h V  L(\~tj\RF<6*  jR. rbpxjpz4V <j~tj\RF<6*   +  r r  rrKi7.84007.84007.8400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamiderrrrrrrrrrrrrr r!r"r#r  Ki5.33005.33005.3300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide$r&r'r(r)r*r+r,r-r.r/r0r1r2r3r4r5r6r  r%r8rD=X {@ rGz@+NrSMDL-00004565 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20376 FCCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)cc1fQDDL5D JH4B ]TSZTXXtDY@\a1%x0DPdy\*x[RyByܟIL%*Ax=u=L%J;bBJŕsԉHXXڵsx]ŕO !|+_9&򀼿={y  abs  rr Ki5.35005.35005.3500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide7r9r:r;rr?r@rArBrCrDrErFrGrHrIr  + TrWr UrYrKi6.95006.95006.9500 receptorH3rat@ membranecortex; brainZ antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide[r^r_r`rarbrcrdrerfrgrhrirjrkrlrmrnr tKi5.09005.09005.0900 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideorqrrrsrtrurvrwrxryrzr{r|r}r~rrrr  \rprrD=X {@VrGz@+N]rSMDL-000045660Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20377iECCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)cc1rfQDDL5D JH4B ]TSZTXXtDY@\a1%x0DPdy\*x[RyByܟIL%*Ax=u=L%J;bBJŕsԉHXXڵsx]ŕO!|+_9&򀼿={y ,JrLrMrNrOrSrQrPrRr??@absXrZrKi5.46005.46005.4600 receptorH2human7 membranecloned antagonistP25021human)GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamiderrrrrrrrrrrrrrrrrr DAt!YVzN@t(\@Q tSMDL-000045670Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20378QDDP5,! B "GdSMqE$QDŅ}gPEq*Q8, 1Z-աUݡPZvNse%Өm=\2u!ENmnyneU権먭]Yi3we9) EΨKI\ZU]ɼ! |+_9&򀼿={y,rrrrrtrrl??@ V P > zJ &  Z ~vlbTJ>4."b J& j Zn v bxhr 2 P   x : h vndZLB6,&ZZ6 jpd\VJ@6,& n\ + tt ttKi7.63007.63007.6300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide t t tttttttttttttttt  Ki4.77004.77004.7700 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidett t!t"t#t$t%t&t't(t)t*t+t,t-t.t/t  tt1tICCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)cc1 abs tt Ki4.92004.92004.9200 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide0t2t3t4t5t6t7t8t9t:t;tt?t@tAtBt  y=F@@0BxBD\DDDFF2HzHJ_JJHLL;NN'PoPBRyPLT'VoVXVXXAZZ\f\^O^^;``!bhbdHdd8ffhahjHjj;ll'nrnp_plKrrCt;vVt#xnx zTzzz|2~~~bLD-xcPF-xaG;'s;jOp6Vy>^~.Nnm%n%o%p%q%r%s%t%u%v%w%x%y%z%{%|%}%yDt%X+ MtPt NtRt  DAt!YVzN@Ot(\@Qv0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20379 HCCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)cc1QDDT5,! B "GdQSNq$QDŅ}gLEqJ Q8, G0YmܱұױUM-PȁY*urA҄^i[M*qnMݞmmn]omA#n5]5UwAhn̈́JE ɹ[\u6Un9Ź5! |+_9&򀼿={y02* -,lFtlGtHtLtJtItKtabsQtSt11,UtvvvWtvvvv??4  v  p > >zNZ6 jpd\VJ@6,& bjt WW:Ki7.27007.27007.2700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideTtvvvvvv v v v v vvvvvvvKi5.03005.03005.0300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidevvvvvvvvvvv v!v"v#v$v%v&v  vv(vKi4.83004.83004.8300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide'v)v*v+v,v-v.v/v0v1v2v3v4v5v6v7v8v9v  + DvGv EvIvKi8.72008.72008.7200 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKvNvOvPvQvRvSvTvUvVvWvXvYvZv[v\v]v^v  Ki4.45004.45004.4500 receptorH1human@ membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide_vavbvcvdvevfvgvhvivjvkvlvmvnvovpvqv @ Lv`vsvD-8HXx@Fv(\@ rhMvSMDL-000045690Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037103CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](C)N)cc1N{$D %NH7HHacGMYt0x$5Qk;4ީ]Q [>$]N2֩;5j=,,s%54N2F:G5=!?N\&9[yT ?Nv,:vv?vCvAv@vBv??absHvJvKi4.39004.39004.3900 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidervtvuvvvwvxvyvzv{v|v}v~vvvvvvv v+@vvvvKi8.15008.15008.1500 receptorH3rat membranecortex; brain0 antagonistQ9QYN8ratnGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidevvvvvvvvvvvvvvvvvv (Kivvvnxxxxxxxx x x x x xx  vvxD-HaӫXy@v?S vSMDL-000045700Bioorg. Med. Chem. Lett. 12(15)-2002 2035-20373CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](N)CO)cc1}$DV'0%H$P3r(Q;(e`HI1`Z/?ͪwjp+kV:ĨujnZop̃EMp)k":5A\AmԆl+kILѯGMc!gܿ9{y\gabsvvvN H T v \ T L B 4 "    @ | t PX F  | v j ` V L F @  |tj`RH<2,  `H$ hX( 0 : `vfp<v" tlbXJ@4*$X2ztnBzpbPD<6*   4.33004.3300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi4.46004.46004.4600 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidexxxxxxxxxxxxxxxx x!x  + ,x/x -x1xKi7.77007.77007.7700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide3x6x7x8x9x:x;xx?x@xAxBxCxDxExFx  Ki4.78004.78004.7800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideGxIxJxKxLxMxNxOxPxQxRxSxTxUxVxWxXxYx  4xHx[xD1<84z@.x(\ @rh5xSMDL-00004571 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037126CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](N)C(C)C)cc1}DSPB2I!5VD!T`aDP@qE[p e,t00I1Z᧍ZZNrem\]!ryNmߐԭUX .eyMd&+we-ڐՐw19|t!r|&9{yndrh,"x$x%x&x'x+x)x(x*x??xabsx0x2x@xKi4.50004.50004.5000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideZx\x]x^x_x`xaxbxcxdxexfxgxhxixjxkxlx +xwxzxxx|xKi7.10007.10007.1000 receptorH3rat2 membranecortex; brain) antagonistQ9QYN8ratNGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide~xxxxxxxxxxxxxxxxxx Ki4.72004.72004.7200 receptorH1humano membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidexxxxxxxxxxxxxxxxxx e xxxD1<84z@yx(\ @rhxSMDL-000045720Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037137CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](N)C(C)C)cc1}DSPB2I!5VD!T`aDP@qE[p e,t00IO0Z᧍ZZNrem\]!ryNmߐԭUX .eyMd&+we-ڐՐw19|!r|&9{ydr,mxoxpxqxrxvxtxsxux??rabs{x}x?rKi4.42004.42004.4200 receptorH2human membraneclonedxxxxxxxxxxxzzzzzzz ?? ~ v z n d ^ R H > 4 . ( z V < 4 , "    l t ~ 8 0 r 2 8 f |rf\VJ@6,& fLD:0" 0zpf\VP8(0F6@F^D<2((ph^TF<0&   antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide+ zz zzKi7.21007.21007.2100 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamidezzzzz z!z"z#z$z%z&z'z(z)z*z+z,z  Ki4.84004.84004.8400 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide-z/z0z1z2z3z4z5z6z7z8z9z:z;zz?z  z.zAzD3L8t)*z@zGz @~jtzSMDL-00004573 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037147CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](N)CC(C)C)cc1 SGҐPB QD&VDTdDU`Wh3b P(U $pqG{gܶyuq7{޶g҇w^wvх6޶]vV]5T6 !Br|9&9[y lBr ,z z z z zzzzz?? abs zz Ki4.85004.85004.8500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide@zBzCzDzEzFzGzHzIzJzKzLzMzNzOzPzQzRz  +]z`z>z^zbzKi6.77006.77006.7700 receptorH3rat0 membranecortex; brainL antagonistQ9QYN8rat4GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidedzgzhzizjzkzlzmznzozpzqzrzsztzuzvzwz Ki5.01005.01005.0100 receptorH1humanz membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidexzzz{z|z}z~zzzzzzzzzzzzz  ezyzzD3L8t)*z@_zGz @~jtfzSMDL-00004574@0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037158CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](N)CC(C)C)cc1SGҐPB QD&VDTdDU`Wh3b P(U $0jtSg`Twf;5jb˕}sf`vՇI:}CvSV7F&5EvVF6ߕF&IWVL裦!Br|9&9[y8lBr*,SzUzVzWzXz\zZzYz[z??0absazczed.Ki4.78004.78004.7800 receptorH2human( membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamidezzzzzzzzzzzzzzzzzz D74!9 *}@|p= ף@- |SMDL-00004575i0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203716!|9&9[y,zzzzz||z|??SMDL-0000457617 ,zE|zF|zI|H|G|z?? receptorHB0P~ H * v \ T J @ 2 (   @ :  |vJ zpbPD<6*   n  ^ N < 2ztnBxj`TJD8.$x`<"pV^hx~X"PhD*" + || | |Ki8.04008.04008.0400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide ||||||||||||||||||  Ki5.48005.48005.4800 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide|!|"|#|$|%|&|'|(|)|*|+|,|-|.|/|0|1|  | |3|:CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@H](N)Cc3ccncc3)cc1&SGҠPB Q!QRC`DayXNE_ )t@! rBb r97m6mnaNK~LQr8aa-PPm@\KG\n8mdrz{\dE\zKQ,b Y\abDK-D\MQDZ\ePa\mNb"/s  abs | | Ki4.43004.43004.4300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide2|4|5|6|7|8|9|:|;|<|=|>|?|@|A|B|C|D|  + J|M| K|O|Ki7.99007.99007.9900 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamideQ|T|U|V|W|X|Y|Z|[|\|]|^|_|`|a|b|c|d| eKi5.64005.64005.6400 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidee|g|h|i|j|k|l|m|n|o|p|q|r|s|t|u|v|w|  R|f|y|D74!9 *}@L|p= ף@- S|0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037;CCCCCC(=O)c1ccc(OCCCN2CCN(CC2)C(=O)[C@@H](N)Cc3ccncc3)cc19&SGҠPB Q!QRC`DayXNE_ )t@! rB r97m6mnaNK~LQr8aa-PPm@\KG\n8mdrz{\dE\zKQ,b Y\abDK-D\MQDZ\ePa\mNb"/s!|9&9[yabsN|P||Ki4.46004.46004.4600 receptorH2human| membranecloned antagonistP25021human@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidex|z|{|||}|~||||||||||||| +||||Ki8.68008.68008.6800||||||zXn~~~~~~~~ ~ ~D3,XGɫs|@|@;On|SMDL-000045770Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203723AC[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1QG0QDY5 "P,aFOAE*Gl!RPII !G   @[`p`i-7sLFU-Ժ_㰅fB-eiL|,s8ȅ|EE"F!_ƣŅ8!-.0!~|+_&{yx~,|||||||||??abs||| ~   8 J| &2 R ~ r h ^ T N H  znd^RH>4.(zV<4," 0 8 B  ^ |rf\VJ@6,& Z6 jpd\VJ@6,& R  membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi5.09005.09005.0900 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide ~ ~ ~~~~~~~~~~~~~~~~  | ~~Ki4.08004.08004.0800 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide~ ~!~"~#~$~%~&~'~(~)~*~+~,~-~.~/~0~  + <~?~ =~A~Ki8.90008.90008.9000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideC~F~G~H~I~J~K~L~M~N~O~P~Q~R~S~T~U~V~  Ki4.16004.16004.1600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideW~Y~Z~[~\~]~^~_~`~a~b~c~d~e~f~g~h~i~  D~X~k~D)8dzwv@>~gfffff?ffffffE~SMDL-000045780Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203724 A-3041213C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1ry$ Fz($T(""(VR G IOq3uR0кeci#oBj]qtBcec>9Cj¯i{`]beBic>򪖣[z`#/h!Z|&[yBZ,1~3~4~5~6~7~;~9~8~:~?abs@~B~Ki4.15004.15004.1500 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidej~l~m~n~o~p~q~r~s~t~u~v~w~x~y~z~{~|~ +@~~l@~~Ki7.69007.69007.6900 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide~~~~~~~~~~~~~~~~~~ Ki4.27004.27004.2700 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor~~~~~~~~~~~~~~~~  ~~D)8dzwv@~gfffff?ffffff~SMDL-000045790Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037252C[C@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1y$ Fz($T(""(VR G IOq3uR0к`i#oBj]qtBcec>9Cj¯i{`]beBic>򪖣[z`#/!Z|&[yBZ,}~~~~~~~~~??abs~~~ z t  x n ` N B : 4 (    l jr| P . J   6d0 xrl@ xnbXRF<2("nJ0( ~T\f8n,& N~pfZPJ>4* ~X4h`F>6, ![3H]-(R)-Nalpha-methylhistamine thioperamideKi4.38004.38004.3800 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide   +  # !%Ki6.92006.92006.9200 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide'*+,-./0123456789:  Ki4.33004.33004.3300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide;=>?@ABCDEFGHIJKLM  (<OD74uEa4a=EvV[#yrV +/+@uP?$F @4 E=%F?EEt?L?ܱPyaɁY !re|+_&"d{y re ,?? abs $& Ki4.30004.30004.3000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideNPQRSTUVWXYZ[\]^_` +knlpKi7.52007.52007.5200 receptorH3ratL membranecortex; braine antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine)thioperamideruvwxyz{|}~ Ki4.43004.43004.4300 receptorH1human membranecloned antagonistP35367human3GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide  sD-8PN+x@mףp= ?㥛 tSMDL-000045810Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037274O=C(C1CC1)c2ccc(OCCCN3CCN(CC3)C(=O)[C@H]4CCCN4)cc2}AC DA$PBBQM1ńaJ]VVQ΁QC`$\MySR뒏S~+S~MQMyR+#NRAh~CWh!|&[yP,acdefjhgi??absoqKi4.27004.27004.2700 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide @ v l ` V P D : 0 &   f L D : 0 "   0  zpf\VP8 (   0F6@ F ^D<2((xrf\RHB<jPH@6( 4LjFFrzpj^TJ@:4$ +    Ki8.40008.40008.4000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$  Ki5.26005.26005.2600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide%'()*+,-./01234567  &9D?LX#@ p= ף@Cl{SMDL-00004582 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203728HCC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2vQDDQFY5DED2PBFFM`\|SLQ$XTiҴ r B4Nc s0gmdmem[smQNKG.[nQjb!$slQbf~bs0bPm@m\KW\jhmz\O6XLbyKQy\)b*b?\Ԃj2s#bN7X]GNLDD !iA|+_9&۲{y iA ,x abs  Ki5.00005.00005.0000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide8:;<=>?@ABCDEFGHIJ  + UXVZKi8.34008.34008.3400 receptorH3rat3 membranecortex; brain antagonistQ9QYN8rat`GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminebthioperamide\_`abcdefghijklmno Ki5.00005.00005.0000 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideprstuvwxyz{|}~  ]qD78'S|@W @tV^SMDL-00004583l0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203729;N[C@H](CCc1ccccc1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2eAC \dRJ1RPDU`faGAF} D !! Kd 07mrMQHK>[NQhaLQ~r0a5mHm@\KG\h8ma^rt{\\E\tKQ,bY\aab[NQ\E\aha_LQ~0arHV\QHm@MK\h8mG\[rt{\tKQ,bY\ab4.(Z6 jpd\VJ@6,& "n\ +  Ki7.64007.64007.6400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide   Ki5.01005.01005.0100 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&'()*+,-./  19N[C@H](Cc1cccs1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2 abs  Ki4.33004.33004.3300 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide023456789:;<=>?@AB  + MP NRKi7.53007.53007.5300 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideTWXYZ[\]^_`abcdefg  Ki5.03005.03005.0300 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidehjklmnopqrstuvwxyz  Ui|D589zX|@O{Gz@(\uVSMDL-000045850Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203731=N[C@H](Cc1ccc(F)cc1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2eADC DT"PGEL-uDaEUPDF"E_DGq=D !! I%X`0@i,sFԺ㰅u_҆Eis|,_ȅ|ĵU*UEBE"F8LULdBE!ƣ!)|?9&[y),CEFGHLJIK??absQS Ki4.40004.40004.4000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide{}~ +Ki8.24008.24008.2400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat D/ 9QZ{@? ףp= SMDL-000045860Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037329N[C@H](Cc1nccs1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2AH DE5UPB-E^d!\|bUP(#u1MW ~yySW9}IR뒏ST,~+S,aqR+#NVRAh~!s/?06۫ys/,??abs z rzZ p ` j 0 6l * >l n f \ R D : . $    R 6~xrF~vl^L@82&j  p |J8 . vpj>Z6 jpd\VJ@6,& RZd GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi4.00004.00004.0000 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide   Ki4.01004.01004.0100 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&'()*+  + 69 7;Ki8.34008.34008.3400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide=@ABCDEFGHIJKLMNOP  Ki4.02004.02004.0200 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideQSTUVWXYZ[\]^_`abc  >ReD/`9Bz@8r= ףp?NbX9?SMDL-000045870Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203733<N[C@H](Cc1c[nH]cn1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2QQNPCaSUxX B UI^d\|хbrA r! Eb r07mMQ\PHK%m\%\>[NQahaGVMLQ_~0arHm@K\h8mG\[rt{\tKQ,bY\ab?@ABCDEFGHIJKLMN  )=PD9 84)~@#@}?5^I*SMDL-00004589 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203735?N[C@H](Cc1csc2ccccc12)C(=O)N3CCN(CCCOc4ccc(cc4)C(=O)C5CC5)CC3 6 !DQAaQV%X C uI^da\C]|(Д!c䐲 0D0 Gb \%\r07m9$\bMQHK%m#uQaNQ>[haoQLQ~0arHm@K\h8mG\[rt{\tKQ,bY\ab}GG !-V}1>_ -V , ?? abs %' Ki4.82004.82004.8200 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideOQRSTUVWXYZ[\]^_`a +lomqKi7.52007.52007.5200 receptorH3rat membranecortex; brainN antagonistQ9QYN8ratCGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine0thioperamidesvwxyz{|}~ Ki5.01005.01005.0100 receptorH1human3 membranecloned antagonistP35367human@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineethioperamide @ tD5 HT7!9|@n(\@OnuSMDL-000045900Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203736=N[C@H](Cc1ccc(O)cc1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2ADC T"PGхK1uDaRaFHTE_@Gm>D !!I}XӀ*Qyze]h|:9 '_0D&&- of]8pU$jS6 ׈^Yf`^HLA,P55j e9X5j!|?ٛ9&[yr0,bdefgkihj??abs9pr?Ki4.48004.48004.4800 receptorH2human8 membranecloned antagonistP25021humanGPCR 17.2800rat | r h b \ x f ^ T J < 2 &   J 2  vpjR B D L V J`PZ  0 `  > x^VLB4*Bvlb\V*jbZPB0$ Nf``.xndZTN"> histaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide+  Ki7.56007.56007.5600 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&'(  Ki5.34005.34005.3400 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide)+,-./0123456789:;  *=D38Q,Xz@zG@|?5^SMDL-00004591 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203737:N[C@@H](C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1)c4ccccc4QDI 5TT"PQEL-EDQZ`CnQtT硃Q0X04i0sU_Ժt!&ir|0T_V$˥|ŅU-ȕU$v5""iȕUǵUEi_ !|?&{y b , ?? abs  Ki4.61004.61004.6100 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide<>?@ABCDEFGHIJKLMN  +Y\Z^Ki6.88006.88006.8800 receptorH3ratc membranecortex; brainc antagonistQ9QYN8rat-GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminerthioperamide`cdefghijklmnopqrs Ki4.92004.92004.9200 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidetvwxyz{|}~  auDA,8[*oG@[yGz@ˡE}bSMDL-00004592@0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203738DN[C@H](Cc1ccc(cc1)c2ccccc2)C(=O)N3CCN(CCCOc4ccc(cc4)C(=O)C5CC5)CC3fADC UBPBArFL5u``a!E_@ш"D%)D!Xu00$1Pܴ7E!.8la:Eݗᇱ2EQC1ᗇ!--=.2rp -1qmqqq }C=-Edqakhq5KCM,KTI!|?9&[y89G,OQRSTXVUW??0abs]_ed.Ki4.69004.69004.6900 receptorH2human2 membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide D+ 9Ȱx@(\?- SMDL-00004593i0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203740!f ?&9[y,??7.2800 receptorH3rat membranecortex; brain antagonistQ9QYN8??~l`XRF< T 6 h ` V L > 4 (    L  |rh^XR& f^VL>,  J b j \ *  tj`VPJjbXN@6* N6ztnVF2:DNdT^0d,> +   Ki7.54007.54007.5400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide   Ki4.34004.34004.3400 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide!"#$%&'()*+,-./01  35N[C@H](CC#N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1 }$ FE#PD+.vX"KTH`EЦ1@ўyyy!1ўBB!ҹbyLx1!aYRrQrґ(qm f abs   Ki4.14004.14004.1400 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide2456789:;<=>?@ABCD  + OR PTKi8.07008.07008.0700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideVYZ[\]^_`abcdefghi Ki4.79004.79004.7900 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidejlmnopqrstuvwxyz{|  Wk~D1,Hv7OuHz@Qףp= ?GzXSMDL-00004594.0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203741<CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1ADA 5T"PEbRElaHdP@tQ41ОByyay!1ўBB!ҹbҡyL񙻁x1!YRrQrґ(qmU!z _yjz@,EGHIJNLKM??absSUKi4.34004.34004.3400 receptorH2human membranecloned antagonistP25021human@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine@thioperamide} +Ki D1,8}tJy@@^I +SMDL-000045950Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203742;CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1恁ADC TrPB1ZTT!XlO< Tu0DŽ0$M5? Ş'_feI}f{Sp%#obDfօ_3jZep9Ş$jMfpԨ9X5j|{1!|_9&=[yb,??abs  > D| 8  Lz0 x r l @ xn`VJ@:.$ nV2vfT \ f nt~  R   N zpfXNB82&fZ6 jpd\VJ@6,& N GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKi4.66004.66004.6600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide   Ki4.72004.72004.7200 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&'()*+  + 69 7;Ki8.80008.80008.8000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide=@ABCDEFGHIJKLMNOP  Ki4.15004.15004.1500 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideQSTUVWXYZ[\]^_`abc  >ReD+8+Ww@8> ףp=?~jt ?SMDL-000045960Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037434CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1{$ Fz($T(""(VZ G IOqh*0auŞӀ|u%9(_Sp%JobuVY,iN'&nVjMf55jVbto|ͨ!|&[yJ,,./015324??abs:<OKi4.00004.00004.0000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidedfghijklmnopqrstuv +Ki7.92007.92007.9200 receptorH3rat membranecortex; brain antagonistQ9QYN8rat@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide Ki4.99004.99004.9900 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide D/8y@Gz@GzSMDL-000045970Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203744:CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1}QDJ 5TTD@PBREM1EDQ]$DXQ9 E !! Jb Z~Wyn]Vy W/g]o]-nmqm]Z7m~LӬWoh-YyXh"~9h9L],nyhe*n+ncYWh!Vhh!|_&{yZ ,wyz{|~}??abs  z p j ^ T J @ : 4  b H @ 8 .   , px < 4x 6  <j~rhbVLB82, ~d\RH:0$H0 ~tnhP@&H^NX$^v\TJ@2( @vlb\V*F"  Ki4.24004.24004.2400 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide   + "  $Ki8.40008.40008.4000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide&)*+,-./0123456789  Ki4.33004.33004.3300 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide:<=>?@ABCDEFGHIJKL  ';ND- 8{l8x@! ףp= @X9v(SMDL-00004598 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037455CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1 }$ Fz($T(""(VZ G IOqV;TH `$@*O/խj뭫%-KFM*o%+O -M/kM9LŭsM`׾M M !ƛ|&9[y R ƛ ,?? abs #% Ki4.22004.22004.2200 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideMOPQRSTUVWXYZ[\]^_ +3jm I@koKi6.79006.79006.7900 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideqtuvwxyz{|}~ OKi4.84004.84004.8400 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide  rD5<8S{@lGzG@/$sSMDL-000045990Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203746:N[C@H](CC1CCCCC1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2ADC T"PGRK1uRDWlVXuŕWQWQCpHCdXӀ*Qyze]h|:9 '_0D&&- of]8pU$jS6 pY|YS׌oؿ!]׸o ˨1Ű!m|?9&[y(pmc,`bcdeigfh??abs9np[Ki4.69004.69004.6900 receptorH2human membranecloned antagonistP25021humanrGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide e,????stP~ ~ d \ R H : 0 $    H0 x r l @ xpfXF:2,   d | f v D 2 (zpjd8rh\RL@6,"hD*"xLT^&^ Fxj`TJD8.$x  Ki8.64008.64008.6400 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide    Ki4.00004.00004.0000 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide!#$%&'()*+,-./0123  "5D)8dzwv@ 333333?"~jSMDL-00004600 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203747,CNCC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1y`Dr*!)JF$NqC3R0Ժ rC/VPGw_/Vf .Vf+w釂NEn}P na r+)a?@ABCDEF  + PS QUKi8.06008.06008.0600 receptorH3rat1 membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideWZ[\]^_`abcdefghij @Ki4.33004.33004.3300 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidekmnopqrstuvwxyz{|}  XlD/8y@R)\(@;vYSMDL-000046010Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037487CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1}AC DTG@PBBaEM1D"aE[qXDG9 D JFf ~Gy]^XT_g]xInp~­]F(n_L$Whyhh]$}nhZnx[nmShl8E}!ü|+&[yZ ü,HIJKOMLNabsTVKi4.30004.30004.3000 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide~ C+ D78'S|@(\ @n@SMDL-000046020Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203749;CN[C@H](Cc1ccccc1)C(=O)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2ADA 5T"PErK1UMPD!XlVaGAG} "E !! Ic ~Gy]^XxT_g]In­]F(nm_Lh$Whyp~h|g]$}nhZn[nShxV\lGfUVM[!.|9&[yr.,??abs9[0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203753@dl LT^L b R \  B t F z ` X N D 6 ,    D J& Zr`TLF:0&~  h ^ L  B~R@|PvhVJB<0& thnx`<TB Ki7.36007.36007.3600 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide Ki4.87004.87004.8700 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&  (Ki4.75004.75004.7500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide')*+,-./0123456789  + DG EIKi7.12007.12007.1200 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKNOPQRSTUVWXYZ[\]^  Ki4.46004.46004.4600 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide_abcdefghijklmnopq @ L`sD/8y@F)\(@;vMSMDL-000046030Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037507CN[C@H](C(C)C)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1h}ADA 5T"PTdaK1UDRZ`S@G5E d ~Gy]^XxT_g]In­]F(n_Lh$Wp~yhgmh$}n]hZn[nShxGh~g!|&{y@Z @,:<=>?CA@B??absHJKi4.31004.31004.3100 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidertuvwxyz{|}~ + Ki8.36008.36008.3600 receptorH3rate membranecortex; brain antagonistQ9QYN8rat@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineethioperamide @ e D)88OuMWv@Q?V-SMDL-00004604e0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037513O=C(C1CC1)c2ccc(OCCCN3CCN(CC3)[C@@H]4CC(=O)N4)cc2{$T(N0eJVDRh(G d=E#!p TTܰ\r݄l%\HڰyH64luܷݦ6!?9;& qe@.,??abs?D+8a7w@z?Q SMDL-00004606niz4X l d \ R D 2 &    ` P $. 4 n  z p f \ V P $ |tj`RH<2,  `H$ hX8 @ J `vfp@v 2 tlbXJ@4*$X2ztnBzpbPD<6*   Ki5.00005.00005.0000 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide Ki5.00005.00005.0000 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%  QDMNwP;l#xnxoPN'P~462-Z#JFdxBF zTzaL~c2\6\zH|6)e 5DxV.['F $x'ny Q@6rnP ~B Tp_p>4a4Q10I_pIbhbbdrdrdWgdgdxd{ MHd* zd5xdU'd"dd#dfRȪjJpPtjR]HjU^Hj1jzlBrlBrlpmr.rr [rt/yt{vKHvx~z [zf| LW| W {& [ n \~W $]}W \bW-V zWre nuWuVz0s4[S[c@VW/m99@WyTj {W [rr Q]t"r+ 14 26Ki7.37007.37007.3700 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide8;<=>?@ABCDEFGHIJK  Ki4.66004.66004.6600 receptorH1human membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideLNOPQRSTUVWXYZ[\]^  9M`D)88OuMWv@3Q?V-:SMDL-000046050Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037522O=C(C1CC1)c2ccc(OCCCN3CCN(CC3)[C@H]4CC(=O)N4)cc2{$T(N0eJVDRh(G d=E#!p$ TTܰ\r݄l%\HڰyH64luܷݦ6!?9;& q@@,&()*+0-,.??abs57Ki4.57004.57004.5700 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide_abcdefghijklmnopq +x{y} 3O=C(C1CC1)c2ccc(OCCCN3CCN(CC3)C(=O)[C@H]4CCN4)cc2}$ F bQXԊ-T:*U2*$ \ t T 0 n < * \ . vpj>~tj\RF<6*   Ki8.88008.88008.8800 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide Ki4.90004.90004.9000 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&  (Ki4.85004.85004.8500 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide')*+,-./0123456789  + DG EIKi7.89007.89007.8900 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideKNOPQRSTUVWXYZ[\]^  Ki5.00005.00005.0000 receptorH1human@ membranecloned antagonistP35367humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide_abcdefghijklmnopq @ L`sD+8a7w@F?Q MSMDL-000046070Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037544O=C(C1CC1)c2ccc(OCCCN3CCN(CC3)C(=O)[C@@H]4CCN4)cc2}$ F bQXԊ-T:*U?CA@B??absHJKi4.91004.91004.9100 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidertuvwxyz{|}~ Ki9.30009.30009.3000 receptorH3rate membranecortex; braint antagonistQ9QYN8rat@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine0thioperamide (   D)8dzwv@= ףp=?V-SMDL-000046080Bioorg. Med. Chem. Lett. 12(15)-2002 2035-203755 A-308830,NCCC(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1y  Fz("T(!D&RZ $9NБↁR0 |77an[jaq aM7|q!w.Pcm[Ml|!l?@AB  Ki4.02004.02004.0200 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamideCEFGHIJKLMNOPQRSTU  0DWD/ 8:x@*p= ף@S㥛 1SMDL-00004609 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037565O=C(C[C@H]1CCCN1)N2CCN(CCCOc3ccc(cc3)C(=O)C4CC4)CC2 ցQDI 5T>PBBD5TQ[(S\RqY=E J WshmQ0m}.Ls[QYbQ5s̗~hXb9s@VsE L ]m\\QEb;\zbb}s\~7 !9&< {q X , !"#'%$&??eabs,.Ki4.05004.05004.0500 receptorH2human membranecloned antagonistP25021humanGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamideVXYZ[\]^_`abcdefgh +svtxKi8.19008.19008.1900 receptorH3rat membranecortex; braino antagonistQ9QYN8rat2GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineCthioperamidez}~ Ki5.82005.82005.8200 receptorH1human0 membranecloned antagonistP35367humantGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamineethioperamide  {D+8+Ww@uףp= ?ףp= |SMDL-000046100Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037593C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1{$F0(QD&Rb*$7P!*F8a$zgEup&yh6D܎7ȋEv]ggp6!&9[qJ0,iklmnrpoq??abs1wy?Ki4.99004.99004.9900 receptorH2human9 membranecloned antagonistP25021humanGPCR 1SMDL-00004611r x n d Z T N j z p b X L B < 0 &    p X 4   x h 6 > H pv L   0 |rhZPD:4( hhD*"x~rjdXND:4.$|j$`<"p~Z@8.$ histaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide+   Ki8.05008.05008.0500 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&'  Ki5.76005.76005.7600 receptorH1human membranecloned antagonistP35367human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide(*+,-./0123456789:  )<D+8+Ww@ףp= ?ףp= 0Bioorg. Med. Chem. Lett. 12(15)-2002 2035-2037604C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(cc2)C(=O)C3CC3)CC1{$F0(QD&Rb*$7P!*F8a$zgEup&yh6D܎7ȋEv]ggVq6 !&9[q J , ?? abs  Ki4.97004.97004.9700 receptorH2human membranecloned antagonistP25021human GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide;=>?@ABCDEFGHIJKLM  Z^Dm%m%'`8+wu@[?K_SMDL-00009581%J. Med. Chem. 35(11)-1992 2074-20841 KW-4994'CN(C)CCSC1c2ccccc2COc3ccc(cc13)C(=O)O3yu T QO,A"тPD0`HDT"(Av~ET0}U[fq6|rҴ=qqe"uDFSqP SuJ}q=rqi5!f8.à 6f,NPQRSTXVUW?asuY\ @Ki7.85397.85397.8539 receptorH1 guinea pig membranecerebellum; brain. antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole]`abcdefghijklmnG {Dn%n%'`Vs@|@Zd;_SMDL-00009582%J. Med. Chem. 35(11)-1992 2074-20842@ ketotifen&CN1CCC(=C2c3ccsc3C(=O)Cc4ccccc24)CC1wes TQE*,eDLzС+ST%+BsB` DFJ2ȅʹ"r)}hb•-꒢rz>†B Q!GF^ @XA|!7]3>_PP $,oqrstuywvx?@ncz}~@Ki9.50869.48419.5346 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole~G dm.53+@ Do%o%-`8 w@\(\@v/SMDL-00009583%J. Med. Chem. 35(11)-1992 2074-208410.OC(=O)c1ccc2OCc3ccccc3/C(=C\CCN4CCSCC4)/c2c1} T(AQ8#U@DtBAR٪ kt-Q<"0s(ܪx*[4߬#/T0"eSAb .19{ -Ӣ6 bA2ẨB.! 7ݛ5*߰١T J ,?? t R .n F 4 Z z p f ` Z  D J T B  j 4 .   > ~rh^TNH 08B*T*vl`VPD:0& jbXN@6* N6ztnVF NdT^d> Ki8.11928.09538.1445 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole fumaric acid salt  !$Dp%p%'`80Us@ ףp= @7A`%SMDL-00009584 %J. Med. Chem. 35(11)-1992 2074-2084 11*CN(C)C/C=C/1\c2ccccc2COc3ccc(cc13)C(=O)Osus TP 2!*$xB0$YTacHDqI9SALvuId&AL??JDxQTQJ&I>h&:m:C`9 6? !7݃*߰ $ ,?? E  " Ki7.92087.86337.9872 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole#&'()*+,-./01234G  @DDq%q%)`8qS6t@Ap= ףп?5^I ESMDL-00009585 %J. Med. Chem. 35(11)-1992 2074-2084 12+CN(C)C/C=C/1\c2ccccc2COc3ccc(CC(=O)O)cc13 wu TP |A(!$# h0`LHI +Z3ӆ"ӓƴ$M"}뢺|M$ĩO|úbvoSv4s?ц?lǣl{ !7݃*_7 , ,5789:><;=?? E ?B Ki7.95867.92457.9957 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizoleCFGHIJKLMNOPQRSTG  fumaric acid salt_b`dgDr%r%)`8qS6t@a(\@ClhSMDL-00009586%J. Med. Chem. 35(11)-1992 2074-208413+CN(C)CC/C=C/1\c2ccccc2COc3ccc(cc13)C(=O)Owu T(Pd#b` 0`HJI!(^S32ԨS'䅭2$Ѩ3'RhR"|Ruscrru^hk̳k!Ό7݃*߰ ,Ό,UWXYZ^\[]??4EceC)CKi8.37688.34498.4112 receptorH1 guinea pig membranecerebellum; brainM antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizolefijklmnopqrstuvwG aDs%s%)`8qS6t@(\@ClSMDL-00009587%J. Med. Chem. 35(11)-1992 2074-208414+CN(C)CC/C=C\1/c2ccccc2COc3ccc(cc13)C(=O)Owu T(Pd#b` 0`HJK!(O£⒓dFtģa~ãD'52vdvąr |qlclr!Ό7݃*߰ (,Ό,xz{|}~??dZm 20Ki7.69907.69907.6990 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizoleG Dt%t%+`882u@p= ףp?A`" SMDL-00009588%J. Med. Chem. 35(11)-1992 2074-208415!u7݃*7? ,??TN& x"  z t 0 ^ d n V " P (  * X   v p j & T Z d L zF  N rl`VLB<6 &0FvhbVLB82,~&X~nx@r\PB<0&   ,CN(C)CC/C=C/1\c2ccccc2COc3ccc(CC(=O)O)cc13{w TRq1(!$W,@ a1”#1<%'&I0OH0E [hF%tiFOHRDRѤ$tFZ붩8#Z%ؘ 4u E  Ki8.28408.26768.3010 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole G  HCl salt$' %),Du%u%+`882u@&p= ףp?A`"-SMDL-00009589 %J. Med. Chem. 35(11)-1992 2074-2084 16,CN(C)CC/C=C\1/c2ccccc2COc3ccc(CC(=O)O)cc13{w TRq1(!$W,@ a1”#1<f&F'{i17h1ǥ AjD)HEuQ#H7SS4mu%!&!!IH!4A|G !u7݃*7? 4u ,#! "?? Z (* Ki7.79597.78657.8055 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole+./0123456789:;<G  HLDv%v%-`8{0u@IHzG?CxMSMDL-00009590 %J. Med. Chem. 35(11)-1992 2074-2084 17-CN(C)CC/C=C/1\c2ccccc2COc3ccc(CCC(=O)O)cc13 y TR8(Ցf8D2xA)cU3Ecw#zML6N2O&bb#ʓˏЏJI6N.IIN̵m~q1O !u7݃*? <u ,=?@ABFDCE??EGJ&FKi8.37688.32248.4389 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizoleKNOPQRSTUVWXYZ[\G hlDw%w%-`8{0u@iHzG?CxmSMDL-00009591%J. Med. Chem. 35(11)-1992 2074-208418-CN(C)CC/C=C\1/c2ccccc2COc3ccc(CCC(=O)O)cc13y TR8(Ցf8D2xA)c+Ecw&FNQen e%SnKkD D ۙ DB=k’Bƴδ2!u7݃*? 2<u(,]_`abfdce??Zcgj2Ki7.82397.77217.8827 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizoleknopqrstuvwxyz{|G fumaric acid salt+p@ Dx%x%-`8ԇ.u@(\@lSMDL-00009592%J. Med. Chem. 35(11)-1992 2074-2084190CN(C)CC/C=C\1/c2ccccc2COc3ccc(\C=C\C(=O)O)cc13y TRN$ BUFa!3€A)+EGc0x&FNQenF   e%2nk Dۙ DB=k’Bƴ!k7݃*? :k,}??absKi7.53767.50867.5686 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRG @ p x \ 4  V .  < j v h b V L B 8 2 , x ~  r &  4 ~  nbTNB8.$dj^ j~pZN@:.$ VV0L<F\rXPB,  ( : histaminergic receptor[3H]pyrilamine astemizolefumaric acid salt  dm +  Dy%y%-`8ԇ.u@(\@oʡSMDL-00009593 %J. Med. Chem. 35(11)-1992 2074-2084 20-OC(=O)c1ccc2OCc3ccccc3/C(=C\CCN4CCCC4)/c2c1 { T(P$#ȠUG!<"TNE*+(^㑍~̓ҢtS'hS~ĢqӢ'S{Sq2us^duTkSYURRk !7?ݛ*߰ف : , ?? abs  Ki8.30108.27828.3251 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole !"#$%&'()*+,G  8<Dz%z%-`8{0u@9ffffff@~jt=SMDL-00009594 %J. Med. Chem. 35(11)-1992 2074-2084 21-CCN(CC)CC/C=C\1/c2ccccc2COc3ccc(cc13)C(=O)O y T(Pd#b` 0`HQ*53,w"2Kb~ vKN撥 b^n Q" ^ A؅ A2-1Ʊ򉀱 !^7݃*ف <^ ,-/0126435?? Z 7: Ki8.00008.00008.0000 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole;>?@ABCDEFGHIJKLG  X\D{%{%+`882u@Yo= ףp@rh]SMDL-00009595 %J. Med. Chem. 35(11)-1992 2074-208422,CN(C)CCC/C=C/1\c2ccccc2COc3ccc(cc13)C(=O)O{w T(P4(H#1PE0`ȈQ’CQ;@#.E%P.SH [%IEoPESHgdZ%FϦ䨦dZ֚ C! 7݃*߰ C4 ,MOPQRVTSU??EWZ^Ki8.20078.19458.2069 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole[^_`abcdefghijklG ex|D|%|%+`882u@yo= ףp@rh}SMDL-00009596%J. Med. Chem. 35(11)-1992 2074-208423,CN(C)CCC/C=C\1/c2ccccc2COc3ccc(cc13)C(=O)O{w T(P4(H#1PE0`ȈQ’AQ;`%v1G%'sR1/ 7%ÉGKRG/Hi4`†  4eGE E t! 7݃*߰ 4 ,mopqrvtsu??Z@wzKi8.23668.22998.2434 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole{~G dm+D}%}%-`8{0u@ ףp= ?Q8SMDL-00009597%J. Med. Chem. 35(11)-1992 2074-208424-CN(C)CCC/C=C/1\c2ccccc2COc3ccc(CC(=O)O)cc13y TR#W,qb` 8`!)c539Fc,x@zH:5J2^^ƋN JN6z澋MM uSM zRMIȵ5!3s7݃*7? <3s,??  n J j X  v4 "  B p v d 4  ^ 6 $ < j &  ~x4 bhrV&P(.\vpj&TZdBr< Nvlb\V>FPv|`fp:PZ*Z$ 8,  abs  Ki8.33728.32338.3516 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole G  y=DtVt#xnx zTzzz|2~~~bLD-xcPF-xaG;'s;jOp6Vy>^~.Nn9Y| [8s M{+\!O~!Ky@o6d*Ve7tA~?{FZ'T.[y )e (Um%n%o%p%q%r%s%t%u%v%w%x%y%z%{%|%}%~%%%%{&}&&*3+3/3FHGHJHKHMHNHPHQHRHSHTHUHVHWHXH[H]H^H`HbHRRRRRRRRTqWrWsWtWuWvWwWxWyWzW{W|W}W~WWWWWWWWW#'D~%~%+`(o7t@${Gz @R(SMDL-00009598 %J. Med. Chem. 35(11)-1992 2074-2084 25(CN(C)CC/C=C/1\c2ccccc2COc3ccc(CCO)cc13uu TR M ! +j@??ZBE@Ki9.20079.08629.3565 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizoleFIJKLMNOPQRSTUVWG fumaric acid salt@beeptcgjD%%)`h:;Vr@d)\(@ʡEkSMDL-00009600%J. Med. Chem. 35(11)-1992 2074-208427&CN(C)CC/C=C/1\c2ccccc2COc3ccc(C)cc13meq TR! M t*QKAX y58<(LvBV*v.7Hw8O-B-.|%8%N77*MM|**%<H!:7 \*? 5:9,XZ[\]a_^`??E\fhKi9.88619.85399.9208 receptorH1 guinea pig membranecerebellum; brain. antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizoleilmnopqrstuvwxyzG y,{??}*w@GP t j ` V P J 4 : D < d 6  . | p b \ P F < 2 , &  x  |  8   xl^XLB8.("~t x 4vhbVLB82,~& ~~ D%%)`8qS6t@ (\@ClSMDL-00009601 %J. Med. Chem. 35(11)-1992 2074-2084 28+CN(C)CC/C=C\1/c2ccccc2COc3cc(ccc13)C(=O)O wu PN4(0U`0`HHCw Q3$ӓ$é҆"uººT6DbvfQvT llt !x7݃*߰ ,x Z   Ki7.61987.59357.6478 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]pyrilamine astemizole G  ~Ki8.01008.01008.0100 receptorH2 guinea pig membranebrain antagonistGPCRhistaminergic receptor [125I]IAPT+./0123456789:;G  A27.22006.58007.8600 receptorH2 guinea pigright atriumhistamine-induced antagonist; contraction GPCRhistaminergic receptor<>?@ABCDEFGHIJe ,=LD{&{&5)|a2}@)Gz@E-SMDL-00009851 %J. Med. Chem. 35(12)-1992 2231-2238 31e 6Nc1ccc(cc1)C(=O)NCCNC(=NC#N)NCCCOc2cccc(CN3CCCCC3)c260M$QD!L 1_t`EFCWlхQFV,EYa$Ѷ E0pX X!*e+($}6db/:G ej[Q&OIC̡ "NQiQ&B؋!>+Y$S.SNj:ɻQ/T %:"!9'sIQ ,!"#$(&%'??encA24.57004.31004.8300 receptorH1 guinea pigileumehistamine-induced@antagonist; contractionGPCRhistaminergic receptorKMNOPQRSTUVWXYe eA25.80005.59006.0100 receptorH1 guinea pigileumhistamine-inducedantagonist; contractionGPCRhistaminergic receptorhklmnopqrstuvwe iyD}&}&5 ),`Bˆ@f)\(@R"jSMDL-00009853%J. Med. Chem. 35(12)-1992 2231-2238@31gp:Nc1c(I)cc(cc1I)C(=O)NCCNC(=NC#N)NCCCOc2cccc(CN3CCCCC3)c2Va,HDQDG\E_0ŔHOp`\Vcvc8O$! V#LT։Yh%N2H&~$IHL kZ\ tT4B&-wkCR)JĚ kR0v%N'MQ I%ƚP'r+AHH%i!o9/{[Q@ o,Z\]^_ca`b??@ncdg)-1A25.77005.59005.9500 receptorm3 guinea pigileumcarbachol-inducednantagonist; contractionGPCR; ion channel#muscarinic acetylcholine receptorxz{|}~e D&&5 )`l`qc@)\(@Gz. SMDL-00009855%J. Med. Chem. 35(12)-1992 2231-223831i!9󦁾'k[Q,??G .4 N ( t X B 8 * $    F , $   F  v x n F 4 |rh^XRrbTNB8.$\lRJ<2&dzL2rF*|8flv^:dR Ki8.58008.58008.5800 receptorH2 guinea pig membranebrain antagonistGPCRhistaminergic receptor [125I]IAPT G  A25.65005.43005.8700 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor !"#$%&'e )6Ic1cccc(c1)C(=O)NCCNC(=NC#N)NCCCOc2cccc(CN3CCCCC3)c260N(QA41zT@FuE -LtaVUP(ց 42QBaU ǚ V~L)LlZ\&s4V? !%>tN#eR)#&3JlR~H sU:6U%vl*"i&  nc Kb7.57007.57007.5700 receptorH2 guinea pigright atriumhistamine-induced antagonist; contraction GPCRhistaminergic receptor(*+,-./0123456e EC507.20767.11927.3188 receptorH3rat cortex; brain agonist; K(+)-induced [3H]histamine release Q9QYN8rat GPCRhistaminergic receptorBEFGHIJKLMNOPQRS EC506.00005.88616.1549 receptorH2 guinea pigright atrium; heart@ agonistspontaneously beatingGPCRhistaminergic receptorTVWXYZ[\]^_`abe CUdD*3*3 Lbbq[@\(\翺I +?ffffffDSMDL-00013098%J. Med. Chem. 35(23)-1992 4434-4441 histamine histamineNCCc1c[nH]cn1-QTabBu0 w#ł#%}9&tUuT!@<!2@wEC506.85396.63837.3010 receptorH1 guinea pigileum@agonist; histamine-induced contractiontGPCRhistaminergic receptorcefghijklmnopqe rac3|b+L-0 }EC507.92087.82398.0458 receptorH3ratcortex; brainagonist; K(+)-induced[3H]histamine releaseQ9QYN8ratGPCRhistaminergic receptor EC503.02693.00003.0555 receptorH2 guinea pigright atrium; heart. agonistspontaneously beatinghGPCRhistaminergic receptore a D+3+3l4ctfa@~*\(?;On?SMDL-00013099%J. Med. Chem. 35(23)-1992 4434-44415CC(N)C(C)c1c[nH]cn15QVbaCu01|ɷIڛ牪Iˍɷو !T\e", tpT,rtuvw{yxz??absEC503.74473.6383e t.~tlX P 6 *   r    v n h  ( T\fD J T , Z 4 >  v d  Nt l \ > 4 &   $ ~tj`XRfL:2,  JFX8*<4V~xlbXNHB|tf\PB<0& : 3.8861 receptorH1 guinea pigileum agonist; histamine-induced contraction GPCRhistaminergic receptorQDFwPjdT7yPLM{~<,D'V!b8fjty+!VXK^>L?J{8V6DFj;N Xh!>>^F\D_J[*~oVah';`2HDOlHjAzz ah';`2HDlHjzzfaXaX ͅR .5 F FH6GHD uzQ[=dg{R,TH4JHUHRH_SH\?/rWiCbHVT[HYTXHS yW H AQNH[IIZ pqW -tW© o}&W`H?QH=Z˕׍R ;|W>KLs/=Ϧ vW wW)IBPH3R  U/W˕>KLs/=Ϧ)  +  EC508.46858.26768.8539 receptorH3rat cortex; brain agonist; K(+)-induced [3H]histamine release Q9QYN8rat GPCRhistaminergic receptor !"#$%&'()*+,- EC503.38723.16123.8861 receptorH2 guinea pigright atrium; heart agonist spontaneously beating GPCRhistaminergic receptor.0123456789:;<e />D/3/3l4ctfa@*\(?;On?SMDL-00013103 %J. Med. Chem. 35(23)-1992 4434-4441 (+)-19C[C@@H](N)[C@H](C)c1c[nH]cn17 QVbaCu01'ai [3yT`jUٸe[e [kU`*JJf !T\e", tp T , ?? abs  EC503.37683.17393.7696 receptorH1 guinea pigileum agonist; histamine-induced contraction GPCRhistaminergic receptor=?@ABCDEFGHIJKe WIC505.74475.56865.9208 receptorPAFnrabbitplatelet-rich plasmaC18-PAF-inducedm"antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinZ]^_`abcdefghijc @[lDFHFH30{y@X@R\SMDL-00018502r%J. Med. Chem. 37(17)-1994 2697-27035/Clc1ccc2C(=C3CCN(Cc4ccncc4)CC3)c5ncccc5CCc2c1օT F%@TQDeM1EсS@F&dEQ9JY%6 D4 \34:}fYׁ[[v vQ*J4b N[NؿՊyY[HUđvZj [*F! $7w\Oـ@ C c,LNOPQUSRT??ncVYG@IC507.02696.82397.2291 receptorH1 guinea pigileumhistamine-induced?antagonist; contractionGPCRhistaminergic receptorkmnopqrstuvwxye m/Clc1ccc2C(=C3CCN(Cc4cccnc4)CC3)c5ncccc5CCc2c1,z|???ctx~ | n h \ R H > 6 0 p h T < 2 *   ` X  * " j  4 ,  N ~dX@2,  6<4,">Vv|T0L\jbR4* ~~IC505.39795.32795.4685 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein c  DGHGH30{y@~@R SMDL-00018503 %J. Med. Chem. 37(17)-1994 2697-2703 6 օT J%@TEDeDRO8TER!%цR=J]%b  űD4 \34:}fYׁ[ vQ[v4bJ[[H[ NؿՊyYjJU*Ƒv[*D !6$ww|Oـä@ 6 nc} IC507.03156.88617.1739 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor !"#$%&'()e nc47 59IC504.46854.30104.6198 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein;>?@ABCDEFGHIJKc <MDJHJH50hy@6(\@Cl=SMDL-00018506 %J. Med. Chem. 37(17)-1994 2697-2703 9 0Clc1ccc2C(=C3CCN(CCc4cccnc4)CC3)c5ncccc5CCc2c1扁T B%@TDSMQdāRLaEzЅrT@(qD-t0P ֘W5x\xy\8Lhg֨5TTYgcjz8pGK*:FsF09psY;:X;FcH*7X1fs$J*$ XI5Kj5 cZ;!4$7w\Oـ@ 4,*,-./3102?? HCl salt8:IC506.44376.10246.7959 receptorH1 guinea pigileumhistamine-induced antagonist; contractionGPCRhistaminergic receptorLNOPQRSTUVWXYZe fIC506.14276.04106.2441 receptorPAFrabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinilmnopqrstuvwxyc j{DKHKH30A 3m ~@g(\@B`"[kSMDL-00018507%J. Med. Chem. 37(17)-1994 2697-27037103Clc1ccc2C(=C3CCN(Cc4cncc(Br)c4)CC3)c5ncccc5CCc2c1lT J%@DAEAQJAԂHBU\ uXH1uPYx0`#ApkueivN{A՟@0!i6>2vևv]4]6m'fpvժ>21c^Ҫs夝&" !dww|O٠Lä@ v,[]^_`dbac??ncehkIC506.55286.46856.6198 receptorH1 guinea pigileumChistamine-inducedcantagonist; contraction@GPCRhistaminergic receptorz|}~e c DMHMH3PٙB5F{@@MbX9SMDL-00018509%J. Med. Chem. 37(17)-1994 2697-2703121Clc1ccc2C(=C3CCN(Cc4cccnc4Cl)CC3)c5ncccc5CCc2c1!{ $wwӛۀä@ ,??$ncnc)f `  ( n Lz n d V P D : 0 &   X r j F 2    > 6     H  ,zrf\RH@: fr|0 *8*j2 2`bZ>( |vbJ@8,"nfx IC50 <4.0000 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein 扁THTH4ЁdTQE5T`.aCqxL9uP-t0!T4 \V[3[*4: 4b}„fYׁ[[v vJ N[N3ĿՊyYjJU*ƑvZH d{ IC506.45596.18056.7212 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptore +IC504.43184.21474.6576 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein.123456789:;<=>c /@DNHNH5Bz@,)\(@MbX0SMDL-00018510 %J. Med. Chem. 37(17)-1994 2697-2703 133COc1ccc(CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2)cn1 T V5@a8`AEETF,SO]`FZD ma1URabPHD!@7_7Y7:MՀլ*jYځ [^vQvQ^H7bM[^*F^NNլHjJy„v*Ƶ !Q$w_ћقߛä@ Q , "#$%)'&(?? nc*- IC506.42026.27576.5686 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor?ABCDEFGHIJKLMe ncX[C50Y]IC50 <4.0000 receptorPAFrabbitplatelet-rich plasmaC18-PAF-induced"antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein_bcdefghijklmc `oDPHPH7(TƮ|@Z\(\@/$aSMDL-00018512%J. Med. Chem. 37(17)-1994 2697-2703@158COC(=O)c1cncc(CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2)c1BHU ĠhQ QTQNQ5UC%xCY(VQO9^ G p VD[[#xKfV)4T T)# frjhoV4)GEE?io:G:vbgW $@e:WZi)*b!IB$فߛæ@ IB,NPQRSWUTV?? HCl salt\^IC506.72126.48156.9586 receptorH1 guinea pigileumhistamine-inducedantagonist; contractionGPCRhistaminergic receptornpqrstuvwxyz{|e c DQHQH5(g?{@Q@!rhSMDL-00018513%J. Med. Chem. 37(17)-1994 2697-2703167OC(=O)c1cncc(CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2)c1BHU ĠhQ QTQNQ5UC CY(ЇUSG׀Ñ0E@7_֬7jJ7:ՀUjJ^HjYځ >M7bJvQ^vM[^Nά*F U^*Fyvڵ!?$فߛæ@ 7?9,}??$nc2Cc1ccc(CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2)cn1 p v. 4h ( <j ~ t j ` X R hT<2* ` X 6 B L  * j  0 ,$F|rh^VP JNJ&H RnXN@:.$BdP8.&T^ IC504.07063.95084.1871 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein IC506.45596.36656.5376 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptore IC505.04584.74475.3565 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein*-./0123456789:c +<DRHRH50hy@333333@jt,SMDL-00018514 %J. Med. Chem. 37(17)-1994 2697-2703 17扁T R%@ XPQDJ=ԔS^V`BUpXH-uTHt0` ָV5[x[xKf4 T Tfcjzho:EsEs#ֈ)0ior::s:vbgW)1e#:WKiG *b !$w|Oߙä@  , "#$%'&(?? HCl saltIC507.43187.21477.6576 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor;=>?@ABCDEFGHIe UIC504.88614.40895.3565 receptorPAFrabbitplatelet-rich plasmaC18-PAF-induced"antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinX[\]^_`abcdefghc YjDSHSH50hy@V333333@jtZSMDL-00018515t%J. Med. Chem. 37(17)-1994 2697-2703180Cc1ncccc1CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2扁T N@F tЀ TQD1T!XŁ vCqXL9uP1t0 X иV/[s[xKf4m#TЈ) Tlf ]jvhomE4E+io4:m:vbfW+e ):WGi#*b!$w|oـä@ ,JLMNOSQPR??ncTWIC506.56866.49496.6383 receptorH1 guinea pigileumhistamine-inducedantagonist; contractionGPCRhistaminergic receptoriklmnopqrstuvwe ncNIC505.43185.31885.5528 receptorPAFrabbitplatelet-rich plasmaC18-PAF-inducedrc ADTHTH50hy@333333@jtSMDL-00018516%J. Med. Chem. 37(17)-1994 2697-2703192Cc1cncc(CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2)c1扁T J%@DAEAQJAE %BYpXH1uLax0\ ָV5[x[xKf4T T fs#cjzhoֈ):EsE0ios:::vb)gWr1e#:WKiG)*b!,$w|Oä@ ,0,xz{|}~?? HCl salt?20?? ,  Z N *T ,  V z p f \ T N nVLD8.$ zr8 > H <   2 NF* hxZR.&vRv0~~vpvbJ@8,"f "antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinIC508.40898.30988.4949 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor e IC504.82394.72124.9208 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein #$%&'()*+,-./0c !2DUHUH50hy@333333@jt"SMDL-00018517 %J. Med. Chem. 37(17)-1994 2697-2703 0Cc1ccncc1CN2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2扁T R@F 4`AE]HQ.T!xP :PDQlXH1uPmx0I\ иV/[s[xKf4m#TЈ) Tf]jvho 4EmE )+io4:m:vbfWl+e:WGi# 4*b !$w|oä@  ,nc IC507.45597.16757.7447 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor13456789:;<=>?e KIC503.86973.42604.3098 receptorPAF rabbitplatelet-rich plasmaC18-PAF-inducedc"antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinNQRSTUVWXYZ[\]^c O`DVHVH-(h Mw@Lp= ף@^I +@PSMDL-00018518%J. Med. Chem. 37(17)-1994 2697-27031 loratadine.CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc4cccnc24)CC1} TU$4h WE2uJUg$TDc*²d1`3"Th̫<<.hh$g&k*d*ͬ3TcL#\#;lTSP#M%dSU!$7.їكH J,ABCDEIGFHncJMIC506.53766.31886.7696 receptorH1 guinea pigileumhistamine-inducedantagonist; contractionGPCRhistaminergic receptor_abcdefghijklme zIC506.07576.03156.1549 receptorPAFprabbitplatelet-rich plasmaC18-PAF-inducedt"antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein}c ~DWHWH+ v@{FzG@-FSMDL-00018519%J. Med. Chem. 37(17)-1994 2697-27032 SCH-37370,CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc4cccnc24)CC1}y T(VA4hWJ2uD%3N$Tq,&@ `D ИW/x\sy\Ш58LhgH*TTYg4X;mY;]j4FmFv8p4$+9pFc6X+fm$ XGj c!$7.߶їقH :,npqrstxvuw?ncy|IC507.00006.85397.1024 receptorH1e   p R J &    j n ( z p h b vldXND:2,L &R \ 8 h*$ nfJ4* hJB xnxf |rh`ZJ,$  guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptorIC506.65766.60216.7212 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein !"#$%c 'DXHXH3(z@zG@Zd;O SMDL-00018520 %J. Med. Chem. 37(17)-1994 2697-2703 3 <[O-][n+]1ccc(cc1)C(=O)N2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2 eA9 QN% uRfԔB n 6a5@0 <6E1hYli㥴blid,MNeN}mHf٥`]e=(LФ٥bD(ۇ-\\j[9I+ !YT@$7of߾'їقكK YT ,  ?? nc IC506.67786.58506.7696 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor&()*+,-./01234e @IC505.82395.69905.9586 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinCFGHIJKLMNOPQRSc DUD[H[H3(z@Ao= ףp@/$ESMDL-00018523%J. Med. Chem. 37(17)-1994 2697-2703226Oc1ccc(cn1)C(=O)N2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2TPO Ȁ DAHT tQHF) :!EQt!@ i`keReN3>BiƠ0{A@%i3>2v6]]栚m'>Rpvu0c^vs"!VT$/w .џقߛîH VT,5789:><;=??nc?BIC506.40896.10796.7212 receptorH1 guinea pigileum histamine-inducedantagonist; contractionGPCRhistaminergic receptorTVWXYZ[\]^_`abe nIC50 <4.0000 receptorPAFrabbitplatelet-rich plasmaC18-PAF-induced"antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteinqtuvwxyz{|}~c rD]H]H3 ('%|@o(\@ffffffsSMDL-00018525@%J. Med. Chem. 37(17)-1994 2697-2703245Clc1ccc2C(=C3CCN(CC3)C(=O)c4cccnc4Cl)c5ncccc5CCc2c1!DPP@d(T uTRNaZe!5T@( BDVkҖ>N3匷ĖizAE@0A>iFӖuF]Ԗ]dm'0ovb^sUqV>"!R$'w.ӿۂîH @jR,cefghljik??@ncmp)-1IC506.88616.65767.1192 receptorH1 guinea pigileumhistamine-inducedantagonist; contractionGPCRhistaminergic receptore 6D^H^H3 ('%|@ (\@ffffff,????> ~ b L B 4 . "    6f H @    v v d  xpj |dZRF<2( TZdP N\T8" v 2 xrBlpzVjB0RJ.  IC50 <4.0000 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein c  SMDL-00018526 %J. Med. Chem. 37(17)-1994 2697-2703 257Clc1ccc2C(=C3CCN(CC3)C(=O)c4ccc(Cl)nc4)c5ncccc5CCc2c1 TPO Ȁ DPHT tQHF) :!EQt@ BEpkuRuN3>bi0{Aş@ժ1!i3>2v6]]ćm'֪>bpv01c^s夝" !U$'w .ӟقߛîH jU nc  IC507.19387.18057.2007 receptorH1 guinea pigileum histamine-induced antagonist; contraction GPCRhistaminergic receptor !"#$%&'()e 4IC50 <4.0000 receptorPAF rabbitplatelet-rich plasmaC18-PAF-induced "antagonist; platelet aggregationGPCRplatelet-activating factorglycoprotein7:;<=>?@ABCDEc 8GD`H`H5(g?{@5Q@fffff9SMDL-00018528 %J. Med. Chem. 37(17)-1994 2697-2703 277COc1ccc(cn1)C(=O)N2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2 TPO Ȁ DAHT tQHF)E :ąSUGх B(E@7U7b_V7:M^7YՀU^*Ƭ*jYN^NHځZ^vQv [jM[جUy„v*Ƶ!W$/w .џقߛîH W ,+,-.20/1nc36IC507.46857.30107.6383 receptorH1 guinea pigileumhistamine-inducedantagonist; contractionGPCRhistaminergic receptorFHIJKLMNOPQRSTe `IC505.50865.26765.7447 receptorPAFrabbitplatelet-rich plasmaC18-PAF-induced("antagonist; platelet aggregationGPCRplatelet-activating factorglycoproteincfghijklmnopqrsc duDbHbH5EBz@a(\@`"yeSMDL-00018530%J. Med. Chem. 37(17)-1994 2697-2703296Cc1cncc(c1)C(=O)N2CCC(=C3c4ccc(Cl)cc4CCc5cccnc35)CC2!DPAAd "TuRM Q ] ea5dP$ BD@"Z"OI*J\"f"5k.pIpU^)NSISũ_VI 8aIZKۗ.NyޗZ߾ϠC!C$w.џîH C ,UWXYZ^\[]??nc_bIC506.45596.31886.6021 receptorH1 guinea pigileumhhistamine-induced2antagonist; contraction=GPCRhistaminergic receptortvwxyz{|}~e E DRRu <_GX@Qh|?5?SMDL-00021199"J. Med. Chem. 38(2)-1995 266-2711a VUF-8319NCc1c[nH]cn1)tQTabBu0 Pz}$k$oгtb$!+@<%<1 %p +@,7SMDL-000212001b,,-.10/wn< 2  D :h | ` J @ 2 ,   4 f H @    v  ~ v d  zpf^X~jRH@4( vnBHR @\T8" v jV>4,  bZ~l A2 <3.0000 receptorH3 guinea pig jejunum #antagonist; acetylcholine release GPCRhistaminergic receptor Ki <3.0000 receptorH1 guinea pig membrane transfected CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramine O  Ki <3.0000 receptorH2human transfected CHO cell antagonistP25021human GPCRhistaminergic receptor[125I]iodoaminopotentidine !"#$%&'()*+  A26.20005.90006.5000 receptorH3 guinea pig jejunum #antagonist; acetylcholine release GPCRhistaminergic receptor256789:;<=>?@E Ki4.90004.90004.9000 receptorH1 guinea pig membrane transfected CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramineACDEFGHIJKLMNOPQO  3BSDRRu Lbbq[@\(\翺I +?ffffff4"J. Med. Chem. 38(2)-1995 266-271 histamineNCCc1c[nH]cn1-QTabBu0 zc~$3l$oCu"ʢ$!@<!2=?7Ki3.60003.50003.7000 receptorH2human transfected CHO cell antagonistP25021humanrGPCRhistaminergic receptor[125I]iodoaminopotentidineacdefghijklmnopqr A27.80007.60008.0000 receptorH3 guinea pig jejunum#antagonist; acetylcholine releaseGPCRhistaminergic receptor~E Ki3.90003.80004.0000 receptorH1 guinea pig membrane transfected CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramineO  DRRu70d@q= ףp?NbX9SMDL-00021204"J. Med. Chem. 38(2)-1995 266-2711f VUF-4732NCCCCCCc1c[nH]cn1=SaQdAu0|#n$qS$#wº$ӓ$R$!{<2?  A26.00005.70006.3000 receptorH3 guinea pig jejunum #antagonist; acetylcholine release GPCRhistaminergic receptorKNOPQRSTUVWXYE Ki6.20006.10006.3000 receptorH1 guinea pig membrane transfected2 CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramineZ\]^_`abcdefghijO  L[lDRRu=yXk@ffffff @v/MSMDL-00021206"J. Med. Chem. 38(2)-1995 266-2711h VUF-4734NCCCCCCCCCCc1c[nH]cn1Oa`TPPPq,RxH  A A ʵ+K0*ˎVg++@}*ˤ* !3<2 bH@2& t ">  xf F t xh^XLB8.("|zt(tnbXND>8lbzVP,  membraneclonedHEK-293 cell antagonistP28335human GPCRserotonergic receptor [3H]mesulergine Ki <5.2000 receptor5-HT2Ahuman membraneclonedHEK-293 cell antagonistP28223human GPCRserotonergic receptor [3H]ketanserin   Ki <5.0000 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor [3H]-8-OH-DPAT !"#$%&'()G  Ki <4.0000 receptor5-HT1Ehuman membranecloned CHO cell antagonistP28566human GPCRserotonergic receptor [3H]-5-HT *,-./0123456789:  Ki <5.0000 receptor5-HT3 rat membranehippocampus; brain antagonistP35563rat ligand-gated ion channelserotonergic receptor [3H]BRL-43694 ;=>?@ABCDEFGHIJ  Ki <5.0000 receptor5-HT4 porcine membranehippocampus; brain antagonistGPCRserotonergic receptor [125I]SB-207710 KMNOPQRSTUVWXG  Ki <5.0000 receptorD1human membranecloned Ltk- cell antagonistGPCRdopaminergic receptor [3H]SCH-23390Y[\]^_`abcdefgO  Ki <4.5000 receptorD2human membranecloned CHO cell antagonistP14416humanGPCRdopaminergic receptor[125I]iodosulpiridehjklmnopqrstuvwx  Ki <4.5000 receptorD3human membranecloned CHO cell antagonistP35462human GPCRdopaminergic receptor[125I]iodosulpiridey{|}~ @ Ki <5.0000 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]mepyramineG  Ki <5.5000 receptoralpha1rat membranecortex; brain antagonistGPCRadrenergic receptor[3H]prazosinG  Ki <6.0000 receptoralpha2rabbit membranecortex; brain antagonistGPCRadrenergic receptorG NCCc1c[nH]c(n1)c2ccsc2Nnx p d Z P D 8 2 , F~ f ^ P > 2 *    $ L 2 *   ^ ~ x r $ xlbVLF:.("j rXPB4*8L|rfZTNvl^RH<2( FT:2$Tf ~2jPH>4& ~[3H]RX-821002 8 +<LZizKi <5.0000 receptorGABA-Arat membranecortex; brain antagonistligand-gated ion channelgamma-aminobutyric acid [3H]muscimol G D26.36006.36006.3600 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor"#$%&'()*+,-.e  0DqWqW\͒5(h@333333?rh|?տ!SMDL-00022385 $J. Med. Chem. 38(8)-1995 1287-129426NCCc1c[nH]c(n1)c2cccs2CaQRSTdWXTha ;2D;66vAT2D5@cw0x076 !pP,02 [p  p ,?? maleic acid salt EC505.00005.00005.0000 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor/123456789:;<=e ID26.37006.37006.3700 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptorLOPQRSTUVWXYZ[e (EC505.27005.27005.2700 receptorH1 guinea pigaortaa6agonist; histamine stimulation; histamine-stimulated contractioneGPCRhistaminergic receptor\^_`abcdefghije M]lDrWrW\&f@J?oʡ?NSMDL-00022386$J. Med. Chem. 38(8)-1995 1287-129427NCCc1c[nH]c(n1)c2ccco2CaQRSTdWXTha ;2D;66vAT2D5@cw0x076!/P,2 [x/,>@ABCGEDF??maleic acid saltHK2Kb9.16009.16009.1600 receptorH1 guinea pigaortahmepyramine-stimulatedtantagonist; contractiontGPCRhistaminergic receptorkmnopqrstuvwxye D25.86005.86005.8600 receptorH1 guinea pigileum6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptore e DsWsWd |~!f@{GzzG?SMDL-00022387-$J. Med. Chem. 38(8)-1995 1287-129428NCCc1c[nH]c(n1)c2ccc[nH]2WCaQRSTdWXThb[a(aNOclcClI%HHT>[#>4vӉcM!P,2 [p^@,z|}~??bmaleic acid salt4ve maleic acid salt6agonist; histamine stimulation; histamine-stimulated contractionmGPCRe m8.8100e~F*2 v l b X R L F $B ` <    j P F 8 2 &     > ~tf`TJ@6.(~phX     2 x   vnh(>6&XDXb~XF>zpdXRL EC504.99004.99004.9900 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor Kb9.03009.03009.0300 receptorH1 guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptore D26.52006.52006.5200 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor)*+,-./012345'7DtWtW\͒5(h@333333?rh|?տ(SMDL-00022388 $J. Med. Chem. 38(8)-1995 1287-129429CaQRTXcSiTVa ;2;D66vA5T2D@cw0x076 !-,02 ۪p  - , !"#%$&?? EC505.21005.21005.2100 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor689:;<=>?@ABCDe PD26.11006.11006.1100 receptorH1 guinea pigileum@6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptorSVWXYZ[\]^_`abe EC504.94004.94004.9400 receptorH1 guinea pigaorta6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptorcefghijklmnopqe TdsDuWuWT` D( q@Qףp= ?y&1USMDL-00022389$J. Med. Chem. 38(8)-1995 1287-129430NCCc1c[nH]c(n1)c2csc(Br)c2M^ 0Q;5.XS(A3 #;bvU!~(06a2< ۫p  ,??maleic acid saltt??n d V P D : 0 &  &    F " z 4 N|\ T 8    v v>4&  > 0(F J  j F T r ~tf`TJ@6.(~D<,^|VD"vlb\VVL>8," EC503.83003.83003.8300 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor Kb8.92008.92008.9200 receptorH1 guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptore (D25.26005.26005.2600 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor+./0123456789:e EC503.89003.89003.8900 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor;=>?@ABCDEFGHIe ,<KDwWwWl[ i@)?S-SMDL-00022391 $J. Med. Chem. 38(8)-1995 1287-129432NCCc1c[nH]c(Cc2ccsc2)n1 K^ PP8L).XQAaZcaADlU3l TDJ Mb";bO> vU ! p~(06!2< [p   , !"&$#%maleic acid salt'* Kb8.97008.97008.9700 receptorH1 guinea pigaorta.mepyramine-stimulatedrantagonist; contractionuGPCRhistaminergic receptorJLMNOPQRSTUVWXe dD26.54006.54006.5400 receptorH1 guinea pigileum6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptorgjklmnopqrstuve hxDxWxW\ aa7l[p@eGz?S㥛iSMDL-00022392h$J. Med. Chem. 38(8)-1995 1287-129433NCCc1c[nH]c(n1)c2cncc(Br)c2mQ` XF%"Da / Za#a1VLXHՓdqRȔOu(N=]",!'@, ۚp',Y[\]^b`_a??maleic acid saltcfKb9.03009.03009.0300 receptorH1 guinea pigaortamepyramine-stimulatedantagonist; contractionGPCRhistaminergic receptorwyz{|}~e D26.20006.20006.2000 receptorH1e  DyWyWl^].gg@{Gz?}?5^IܿSMDL-00022393$J. Med. Chem. 38(8)-1995 1287-129434NCCc1c[nH]c(n1)c2ccccc2I^ PDHq Q0XʰT `|RpRO8!P?,[q ,??maleic acid salt | r h b \ 6 . V  L ( < T z ` V H B 6 , "   N ~tf`TJ@60* ~ $   4  ldH.$XN@:.$XJB2`d\nvlb\VVL>8,"  guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptorEC505.20005.20005.2000 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor e Kb8.87008.87008.8700 receptorH1 guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptor !"#$%e 1D26.75006.75006.7500 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor4789:;<=>?@ABCe 5EDzWzWd`q:Gp@2Q?;On6SMDL-00022394 $J. Med. Chem. 38(8)-1995 1287-129435NCCc1c[nH]c(n1)c2cccc(Br)c2 O` X(QB$q( C Q4ƒ @dDfŽضȞb&} r&|(fqX !@p?, [q   ,&()*+/-,.?? maleic acid salt03 EC505.60005.60005.6000 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptorDFGHIJKLMNOPQRe ^D26.68006.68006.6800 receptorH1 guinea pigileum6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptoradefghijklmnope brD{W{Wd#*Hs@_@֣p= cSMDL-00022395a$J. Med. Chem. 38(8)-1995 1287-129436NCCc1c[nH]c(n1)c2cccc(I)c2O` X(QB$q( C Q4ƒ dDŽhض&b&F} &r}qXl!p?, [qt i,SUVWX\ZY[??maleic acid salt]`EC505.59005.59005.5900 receptorH1 guinea pigaorta6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptorqstuvwxyz{|}~e D25.87005.87005.8700 receptorH1 guinea pigileum6agonist; histamine stimulation; histamine-stimulated contraction9GPCRhistaminergic receptore aD|W|W|6(i@HzG?x&1SMDL-00022396$J. Med. Chem. 38(8)-1995 1287-129437Cc1cccc(c1)c2nc(CCN)c[nH]2M` X(QB$q(ƒDb`-ٱ0# §QĀ%B%⿭q։9!;p,9[q ;,??maleic acid salte n9h ` P    |  @  p * Hv x n f ` &@< |P Z l f @ .  6 tj\VJ@6,$tzth^TJD>8(H"x\B8*$0( Bh`P Kb9.04009.04009.0400 receptorH1 guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptor D}W}Wdo@@)\(SMDL-00022397 $J. Med. Chem. 38(8)-1995 1287-129438!NCCc1c[nH]c(n1)c2ccccc2C(F)(F)F ]%g P! "5bĈ0 b090X@I1H+:,^z9g#Pީu+'r v _Nz#B_"8 !$]t?/f6[q  $] ,?? maleic acid salt D24.47004.47004.4700 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor !"#$%&'()*+,e 8D26.81006.81006.8100 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor;>?@ABCDEFGHIJe <LD~W~Wdo@9@)\(=SMDL-00022398 $J. Med. Chem. 38(8)-1995 1287-129439#NCCc1c[nH]c(n1)c2cccc(c2)C(F)(F)F ]%g P upĈ%dD:9 0ZHj1,:n.V$a._"q$9Qh#mqs vx J8h`_v$ ! \t?/f \,-/0126435??maleic acid salt7: $EC505.89005.89005.8900 receptorH1 guinea pigaorta6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptorKMNOPQRSTUVWXYe eiDWWdo@f@)\(jSMDL-00022399@$J. Med. Chem. 38(8)-1995 1287-129440#NCCc1c[nH]c(n1)c2ccc(cc2)C(F)(F)F]%g Q)!BD#F(!Fe 0``1xڕu%1!edjeeؽu6!\bT?/fِ \bM,Z\]^_ca`b??(maleic acid saltdgPD24.60004.60004.6000 receptorH1 guinea pigileum6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptorhklmnopqrstuvwe D26.43006.43006.4300 receptorH1 guinea pigileum26agonist; histamine stimulation; histamine-stimulated contraction.GPCRhistaminergic receptore aDWWdT:Xp@p= ף@x&SMDL-00022400$J. Med. Chem. 38(8)-1995 1287-129441$NCCc1c[nH]c(n1)c2cccc(OC(F)(F)F)c2c5i X(FPq0 $J8E$RL&<A8pZpq}0}#uMY,{ON7puOOp͙M)s7)M1,!@Vt?/f6{q@V,xz{|}~??maleic acid saltKb8.92008.9200H1e . &  H ` t~t $ n H 6 ,Z | r d ^ R H > 4 . (  |   "  D   |nh\RH>60xrf\RHB< 6 *&L ~vf.$H.BzVNnTJ<6*   8.9200 receptor guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptor DWWtDVq@(\@nSMDL-00022401 $J. Med. Chem. 38(8)-1995 1287-129443%NCCc1c[nH]c(Cc2cccc(OC(F)(F)F)c2)n1 gEk Qň#AE$EeDx0x$ W V^^ D^n[[b8OOJ_ZB !9@t>+f616<{q  9@ , ?? maleic acid salt D24.57004.57004.5700 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor !"#$%&'e 3D25.11005.11005.1100 receptorH1 guinea pigileum 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptor69:;<=>?@ABCDEe EC503.24003.24003.2400 receptorH1 guinea pigaorta 6agonist; histamine stimulation; histamine-stimulated contraction GPCRhistaminergic receptorFHIJKLMNOPQRSTe 7GVDWWt0vm@4\(\@= ףp=8SMDL-00022402$J. Med. Chem. 38(8)-1995 1287-129445NCCc1c[nH]c(Cc2ccccc2Cl)n1Sc PD8HEC)1|DD@݌jτqQ P=O&tQY%Z(6!6 <[q | ,dfghimkjl??maleic acid saltnqKb8.81008.8100e    j ` R L @ 6 , "   j \ T D  r v  $ z ~tnh &@xn`ZND:0*$xDXbpjD2>f^N "b>n(jldH.$  receptorH1 guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptorDWW|ҩm@Gz@`"SMDL-00022404 $J. Med. Chem. 38(8)-1995 1287-129447NCCc1c[nH]c(n1)c2ccc3ccccc3c2 [%i XF?@ABCDe 6FDWW DPNdf@3p= ףp?$C?7SMDL-00022405 $J. Med. Chem. 38(8)-1995 1287-129449NCCc1c[nH]c(n1)C(F)(F)F ?aQRTEv010vP\e#R0_5nj:IރGrPvCx6ċ6 ! T?/f? [p \ ,')*+,0.-/?? HCl salt14 Kb9.19009.19009.1900 receptorH1 guinea pigaorta mepyramine-stimulated antagonist; contraction GPCRhistaminergic receptorEGHIJKLMNOPQRSe D26.70006.70006.7000 receptorH1 guinea pigileum6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptor_bcdefghijklmne EC505.94005.94005.9400 receptorH1 guinea pigaorta6agonist; histamine stimulation; histamine-stimulated contractionGPCRhistaminergic receptoroqrstuvwxyz{|}e m `pDWW Lbbq[@\(\翺I +?ffffffaSMDL-00022406n$J. Med. Chem. 38(8)-1995 1287-1294 histamine histaminemNCCc1c[nH]cn1t-QTabBu0 f*ot`>E]kCey??$!@<!2?@ABCDEG  Ki <5.0000 receptorH1 guinea pig membranebrain antagonistGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine FHIJKLMNOPQRSG  6GUC[C@H]1NCC[C@@H]1c2c[nH]cn2@absi24@8.D27.10006.90007.3000 receptorH3 guinea pigileumelectrically-inducedantagonist; contraction-GPCRhistaminergic receptorTVWXYZ[\]^_`abe Ki7.48157.46857.4949 receptorH3 guinea pig membranebrain antagonistGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminepnopqrstuvwxyz{lDXXlߡ(b@p= ףp?+?mSMDL-00022728%J. Med. Chem. 38(10)-1995 1593-1599(-)-4a= QWbXaSZSCUS"``-7Ӗ'-W֢'<((&!a\e6#< p9a-,cefghjik??G SMDL-000235104a,}WXY][Z\brai r h \ N H < 2 (    \ T 0 f \Z R 6    t | n h \ P J D | h`RH<.( <  vlbZT~F<.(NFL(X Ki <5.0000 receptorH1 guinea pig membranebrain antagonistGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine | Ki8.82398.69909.0000 receptorH3 guinea pig membranebrain antagonistGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine  !"#$%&'()*G  Ki <5.0000 receptorH1 guinea pig membranebrain antagonistGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine +-./012345678G  D28.20008.00008.4000 receptorH3 guinea pigileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor9;<=>?@ABCDEFGe ,:IDXX \e-K_@ףp= ӿx/?SMDL-00022729 %J. Med. Chem. 38(10)-1995 1593-1599 C[C@@H](N)Cc1c[nH]cn1 3 QTab$u0 Pʆ373'٦3 !T!<)p   ,R  D25.40005.30005.5000 receptorH1 guinea pigileum electrically-inducedantagonist; contraction GPCRhistaminergic receptorHJKLMNOPQRSTUVe 5_A27.00006.80007.2000 receptorH3 guinea pig jejunum@electrically-inducedantagonist; contraction@GPCRhistaminergic receptorbefghijklmnopqe @Ki3.50003.00004.0000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyraminertuvwxyz{|}~O 2 csD[[ m2j@`أp= ?333333(\?d%J. Med. Chem. 38(12)-1995 2244-2250 burimamideCNC(=S)NCCCCc1c[nH]cn1GTaQ"e&u@ Q Xm\s>~s+s՜~~nm6m)ns .scsm!ʣ2 8 , "     F JB&N dh | ` < \ vpj`X<$ z2zth^TJD>T8Zdp*&~d\ND8*$  A28.00007.90008.1000 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptor Ki4.70004.60004.8000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramine O  "Ki4.70004.60004.8000 receptorH2human membranecloned CHO cell antagonistP25021human GPCRhistaminergic receptor[125I]iodoaminopotentidine!#$%&'()*+,-./0123  @A28.00007.90008.1000 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptorCFGHIJKLMNOPQRe Ki4.80004.70004.9000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramineSUVWXYZ[\]^_`abcO  DTeD[[  c n@A?"~jESMDL-00023519%J. Med. Chem. 38(12)-1995 2244-22505b VUF-4614CCNC(=S)NCCCCCc1c[nH]cn1Wa ` *^XaD @ 9V0"2D<;=?0oxalic acid salt?BN@Ki5.00004.90005.1000 receptorH2human membranecloned CHO cell antagonistP25021humanGPCRhistaminergic receptor[125I]iodoaminopotentidinedfghijklmnopqrstuv A27.70007.60007.8000 receptorH3 guinea pig jejunumelectrically-inducedantagonist; contractionGPCRhistaminergic receptore Ki5.50005.40005.6000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramineO @ D[[ No@Q@MbSMDL-00023520%J. Med. Chem. 38(12)-1995 2244-22505c VUF-4615CCCNC(=S)NCCCCCc1c[nH]cn1Wc`c!D*Vhˆ: @ @66W%7]Lrۄc[Vs\\fs!4ʣr T z V L vpdZPF@: ~tj`ZTx`TF@4*  L*4@\4.H.&f~xlbXNHBnVJ<6*    receptorH2human membranecloned CHO cell antagonistP25021human GPCRhistaminergic receptor[125I]iodoaminopotentidineA27.70007.60007.8000 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptor !"#$%&'()*+e Ki4.90004.80005.0000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramine,./0123456789:;<O  ->D[[ No@)\(@(\SMDL-00023521 %J. Med. Chem. 38(12)-1995 2244-2250 5d VUF-4616CC(C)NC(=S)NCCCCCc1c[nH]cn1 Wc*a+B)D1XPB: A 4W5#[Ü5 ܂cJrVqܿܩϜf !Sʣ#2Kn9o/N ̶ЅV9 焹m46XG6/1!ˣ<#2<1 ,?oxalic acid salt6 0 $    D l  0 v p H 6 8f8    V . @~rh^TNHh B| ~ ,  r l D 2 4 b ldZPB6, :rj\PF:,&480<RzVJh`VL>2(  jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptorKi5.60005.50005.7000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramine O  Ki4.90004.80005.0000 receptorH2human membranecloned CHO cell antagonistP25021human GPCRhistaminergic receptor[125I]iodoaminopotentidine !"#$%&'()  6A27.70007.50007.9000 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptor9<=>?@ABCDEFGHe Ki5.40005.30005.5000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramineIKLMNOPQRSTUVWXYO  :J[D[[! 9r@7(\@A`";SMDL-00023524 %J. Med. Chem. 38(12)-1995 2244-2250 5g VUF-4619!S=C(NCCCCCc1c[nH]cn1)NCc2ccccc2iUm*a,( )."CGD1aD( m mw~{ss\b~]sgx~F,sms:nm~Om֙s[sqmsN~n!ˣ> 2g朢8>813⦍6B): 9[|'sZ6oHm3 O !ˣ<62 4 . ( j ~ t h Z T H > 4 * $  b f ^ B *   j    " . x |rlf0|rlfrfXRF<2("^BV`RvF@<Z@8.$ xxnhbH@$ [125I]iodoaminopotentidine A28.10007.90008.3000 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptore Ki5.80005.70005.9000 receptorH1 guinea pig membranecloned CHO cell antagonistGPCRhistaminergic receptor[3H]mepyramine !"#$%&'()*+,-.O  0D[[! 1@ ;u@ Gz @$CSMDL-00023526 %J. Med. Chem. 38(12)-1995 2244-2250 VUF-4742%Clc1ccc(CNC(=S)NCCCCCc2c[nH]cn2)cc1 oeo*a2(C+ FbĐF 3jFb P"c`Z8W۵+4C=s;d{{ڇi\ws|] B_ZNJPK] ! ˣ> 6?@A  MKi7.95867.82398.1549 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization2Q9QYN8ratmGPCRhistaminergic receptorPSTUVWXYZ[\]^_`ab Ki8.10008.10008.1000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidecefghijklmnopqrstu Kb5.30005.30005.3000 receptorH2 guinea pigatrium; heart"antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalinevxyz{|}~E @QdwDHtHtt(`o l2w@N\(\ @V-RSMDL-00029768$J. Med. Chem. 39(6)-1996 1220-12264!Ic1ccc(NC(=O)OCCCc2c[nH]cn2)cc1c5i@`DbB:jXbF #J=:@qRMX e1xi0CJ9i6 6UFAx %J06 %\ %M 6k0Lkw0>h06!>#6<31te,BDEFGKIHJ??@maleic acid saltLOaliKb4.40004.40004.4000 receptorH1 guinea pigsmooth muscleileumelectrically-inducedantagonist; contraction-GPCRhistaminergic receptorg DItItt(`o l2w@\(\ @V-SMDL-00029769$J. Med. Chem. 39(6)-1996 1220-12265e!Ic1cccc(NC(=O)OCCCc2c[nH]cn2)c1c5i`D3!B+ @p # *:@VM` uZt,~KYz\z7tZLiMi.c[z,nXˮtt/^zNi tZz!Gp<#616< aqGc,??6??ڔ  H $ n \  P~X P 4   r  d J B  t vlbXRL$zH8& D  V 2 | j $ ^ zpjd. ztnzn`ZND:0*$f@T^T|H  Ki7.79597.69907.9208 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor  Ki8.10008.10008.1000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%&'  Kb5.30005.30005.3000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaline(*+,-./0123456E  )8maleic acid saltKb5.10005.10005.1000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor79:;<=>?@ABCDEFg PKi7.60217.52297.6990 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarizationQ9QYN8ratGPCRhistaminergic receptorSVWXYZ[\]^_`abcde Ki7.60007.60007.6000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidefhijklmnopqrstuvwx Kb4.60004.60004.6000 receptorH2 guinea pigatrium; heart"antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaliney{|}~E @TgzDJtJtt(`o l2w@Q\(\ @V-USMDL-00029770$J. Med. Chem. 39(6)-1996 1220-1226Ic1ccccc1NC(=O)OCCCc2c[nH]cn2c5iTTZ0`1)Zá$p:A TMX kmчn! sWvv(slmbH~+bZ s sZm~m,bmmKjm)sY}\b@!?+<#1pt,HIJNLKMmaleic acid saltORtorKb4.80004.80004.8000 receptorH1 guinea pigsmooth muscle2ileumelectrically-inducedantagonist; contraction@GPCRhistaminergic receptorg  DKtKt(`7XOx@Q @dX9HSMDL-00029771$J. Med. Chem. 39(6)-1996 1220-12267"Ic1ccc(CNC(=O)OCCCc2c[nH]cn2)cc1gEk `D2C+ Fbİ Fjt0(⠚(ހ/͎ `P)yH]逞  IZ |B޴z!> 6 6   X X > 6  h |vj`VLF@xn<,  8x  B  p ^  J |rlf"xpL:,&8BzRvfTD<6*  @rR Ki7.92087.85398.0000 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor Ki7.90007.90007.9000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%  Kb4.50004.50004.5000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaline&()*+,-./01234E  '6Kb5.10005.10005.1000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor5789:;<=>?@ABCDg PKi7.69907.56867.8861 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8ratGPCRhistaminergic receptorSVWXYZ[\]^_`abcde Ki8.10008.10008.1000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidefhijklmnopqrstuvwx Kb4.50004.50004.5000 receptorH2 guinea pigatrium; heart"antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaliney{|}~E rTgzDLtLtl(`~Bv@Q@USMDL-00029772$J. Med. Chem. 39(6)-1996 1220-12268 Ic1ccc(cc1)C(=O)OCCCc2c[nH]cn2_%g`DbP (! Y51D.^^]a΅0Ή.p2i+iJ-)f!4-? ?@ABCDg PKi7.40897.31887.5229 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8ratGPCRhistaminergic receptorSVWXYZ[\]^_`abcde Ki7.70007.70007.7000 receptorH3rat membranecortex; brain@ antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidefhijklmnopqrstuvwx Kb4.60004.60004.6000 receptorH2 guinea pigatrium; heart"antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaliney{|}~E rTgzDNtNtl(`~Bv@Q@USMDL-00029774$J. Med. Chem. 39(6)-1996 1220-122610Ic1ccccc1C(=O)OCCCc2c[nH]cn2_%g )TZ2&Dĉ0x(bl4H1J5A1|agK6XOVqbJڎa~)B]K^na&bKbbr!-P= <!qr.n,EGHIJNLKM??rmaleic acid saltOR.31Kb5.90005.90005.9000 receptorH1 guinea pigsmooth muscleileumelectrically-inducedantagonist; contraction@GPCRhistaminergic receptorg @ DOtOt|(`jt#w@333333@HzGSMDL-000297750$J. Med. Chem. 39(6)-1996 1220-122611!Cc1ccc(cc1I)C(=O)OCCCc2c[nH]cn2c5iS J@b 4*:` jBc0O^GctC@srFk=[FtE΃mcΓhSEYt;KGkr UGPt!G(- ;16G(0,??(maleic acid salt?( receptorH2d salt \ pzr  l F 4 (V(  B < "  L th`ZND:0*$ld\R  b v &  z T B . \ tj`VPJphD2$0:~xrJvfTD<6*  8 Ki7.52297.39797.6990 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor Ki8.30008.30008.3000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%  Kb4.20004.20004.2000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaline&()*+,-./01234E  '6Kb4.90004.90004.9000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor5789:;<=>?@ABCDg PKi6.83566.75956.9281 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8ratGPCRhistaminergic receptorSVWXYZ[\]^_`abcde Ki7.50007.50007.5000 receptorH3rat@ membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidefhijklmnopqrstuvwx Kb4.60004.60004.6000 receptorH2 guinea pigatrium; heart"antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaliney{|}~E iTgzDPtPtl(g\8@Q@+NUSMDL-00029776$J. Med. Chem. 39(6)-1996 1220-122612$Nc1c(I)cc(cc1I)C(=O)OCCCc2c[nH]cn2gEkQ@D "ȪeFBaF& Ju0jlǛDkÛ ^D[2_2.WSEbY^Z^ڀ2!Jp/p? @jJpi,EGHIJNLKM??emaleic acid saltOR1Kb5.90005.90005.9000 receptorH1 guinea pigsmooth muscleileumNelectrically-inducedantagonist; contractionhGPCRhistaminergic receptorg  DQtQt|(`jt#w@@ʡESMDL-00029777$J. Med. Chem. 39(6)-1996 1220-122613!Ic1ccc(CC(=O)OCCCc2c[nH]cn2)cc1c5i`TP+)¡ !%JHbF*1: jb`Lsޣ=Fq_DEcqC"Zq{rDmq{KDCUDcPq!->6 <316,??maleic acid salttG  j ~ . z T B 6d6 .  P < "  L th`ZND:0*$ld\R  p  4  z T B < j tj`VPJphD2$0:~xrJvfTD<6*  8 Ki7.85397.72128.0458 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor Ki7.90007.90007.9000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide !"#$%  Kb3.60003.60003.6000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenaline&()*+,-./01234E  '6Kb4.50004.50004.5000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor5789:;<=>?@ABCDg QD2/>^F8& '2~~~2 }.is;j-@b@;vS0xG;(fF@Vt{HLf\0B2~~~ }.s;j-@b@;vS0xG;(fF@Vt{HLf\0B<uv%<uw%<R> Rt>>8>0@@BBBZBZB9B†DÌWD8DvD=ƌD=njFQFTtH H JJJJVHJ o%LH]ΌN StPPqPrR ƛT .IT ?NTwX Z Z üZ \ W\\a\g\(^sW^` hb sBZBZB†DÌWD8DvH H JJJJVHJ o%PR ƛT .IT ?NTwX Z Z üZ \ W\\a\g\(^sW^` hb sQKi7.32797.21477.4815 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptorTWXYZ[\]^_`abcdef Ki7.10007.10007.1000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamidegijklmnopqrstuvwxy eKb3.6000z|}~E Uh{DRtRt(`Gjx@R(\@\(\VSMDL-00029778$J. Med. Chem. 39(6)-1996 1220-122614"Ic1ccc(CCC(=O)OCCCc2c[nH]cn2)cc1gEk`TP+)Ō( FR %jt @@FՄ@~f|vu9GFG*8g6g8D5'D(fGƥ9!->6 ,EGHIJOLKM??maleic acid saltPSst 8 x f Z R L @ 6 , "   ^ V N D   @ x     d R tj`VPJphD2$0:~xrJvfTD<6*  8 ~~ guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalineKb4.80004.80004.8000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor g "Ki6.63456.54526.7471 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor%()*+,-./01234567 Ki6.70006.70006.7000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide8:;<=>?@ABCDEFGHIJ  Kb4.50004.50004.5000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalineKMNOPQRSTUVWXYE  &9L[DStSt!8`&py@#RQ@3^I 'SMDL-00029779$J. Med. Chem. 39(6)-1996 1220-122615$COc1ccc(CCC(=O)OCCCc2c[nH]cn2)cc1Ioeo`TP a[ȣ%L0 2fPЁakcKb <4.0000 receptorH1 guinea pigsmooth muscleileumelectrically-inducedantagonist; contractionGPCRhistaminergic receptorZ\]^_`abcdefgg sKi7.38727.28407.5229 receptorH3rat synaptosome@cortex; brainK(+)-induced/antagonist; histamine release; depolarizationQ9QYN8ratGPCRhistaminergic receptorvyz{|}~ Ki7.50007.50007.5000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminethioperamide @Kb4.00004.00004.0000 receptorH2 guinea pigE wDTtTt!(`l`x@t(\@lqxSMDL-00029780$J. Med. Chem. 39(6)-1996 1220-122616#Ic1ccc(CCCC(=O)OCCCc2c[nH]cn2)cc1kUm`TP)iHc ),D2J@ 4Mz@ɍhM-hݧTmJk |͏-MmA- !->6 ?@ABCDEFGHI  Kb5.20005.20005.2000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalineJLMNOPQRSTUVWXE  %8KZDUtUtl`'UHyt@"@/$&SMDL-00029781$J. Med. Chem. 39(6)-1996 1220-122617Ic1ccc(OCCCc2c[nH]cn2)cc1Uc`TP0ѡ/HpABDpcCrB俴Ȗ3kCiofiC#cܖi{iҖ.!ٻ>6 l:2TZ@8j ~xlbXNHBzp>. :t8r`@n ~tnh$X>6 histaminergic receptorisoprenalineKb6.20006.20006.2000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor g Ki8.30108.22188.3979 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor!$%&'()*+,-./0123 Ki9.00009.00009.0000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide46789:;<=>?@ABCDEF  Kb5.20005.20005.2000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalineGIJKLMNOPQRSTUE  "5HWDWtWt|`ZB>bu@ @xi#SMDL-00029783 $J. Med. Chem. 39(6)-1996 1220-122619Ic1ccc(COCCCc2c[nH]cn2)cc1Ye`TP0ѡ0Hႄ*5 (z<אW<7JX;L'<כf⦥<0!z>6 bu@r @xivSMDL-00029784$J. Med. Chem. 39(6)-1996 1220-122620Ic1cccc(COCCCc2c[nH]cn2)c1Ye`TP<#*&j5 `@vezǶ>'.ڈ-fNJֳ&љw10>g?06!ִ<6 <1( ִ,fhijkomln??maleic acid saltps?g P 6 . ` | t n b X N D > 8  x p f 4 $    0 bv &  \ J  .\~tjd^z,~tfTH@:.$ rLD<2f:NX`~Z4"4tf`TJ@60*| uKb5.80005.80005.8000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor Ki7.45597.35657.5850 receptorH3rat synaptosome cortex; brain K(+)-induced/antagonist; histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor"#$%&'()*+,-./01 Ki8.10008.10008.1000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistamine thioperamide2456789:;<=>?@ABCD  Kb5.10005.10005.1000 receptorH2 guinea pigatrium; heart "antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalineEGHIJKLMNOPQRSE   3FUDYtYt`}\*#w@Q@/$!SMDL-00029785 $J. Med. Chem. 39(6)-1996 1220-122621Ic1ccc(CCCOCCCc2c[nH]cn2)cc1a5i`TPx"0H̐E  : Ң9Wϝ[ւ [44[ VpΓebRIfҗf"Ӿ!>6 @Kb5.20005.20005.2000 receptorH1 guinea pigsmooth muscletileum@electrically-inducedantagonist; contractionGPCRhistaminergic receptorTVWXYZ[\]^_`abcg oKi7.85397.74478.0000 receptorH3rat@ synaptosomecortex; brainK(+)-induced/antagonist; histamine release; depolarization@Q9QYN8ratGPCRhistaminergic receptorruvwxyz{|}~ Ki8.90008.90008.9000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat@GPCRhistaminergic receptor![3H]-(R)-Nalpha-methylhistaminecthioperamide  Kb4.90004.90004.9000 receptorH2 guinea pigatrium; heartt"antagonist; positive chronotropyGPCRhistaminergic receptorisoprenalineE esDZtZt| <,Ԛrr@p\(\ @jttSMDL-000297860$J. Med. Chem. 39(6)-1996 1220-122622Brc1ccc(COCCCc2c[nH]cn2)cc1Ye`TP0ѡ0Hႄ*# `Bfz֌??NjۊFћG0?糋1ƽ1&1f!z@>6 ?@AE  4CD\t\t0Bx4t@Q?S!SMDL-00029788 $J. Med. Chem. 39(6)-1996 1220-1226 impromidine impromidine %Cc1[nH]cnc1CSCCNC(=N)NCCCc2c[nH]cn2 ueo `-b5LFe3JxAF 0hS Dx х'(q4&qԌZN hIԌa g|&9bSge|^BX  !k@#?@ABCDEFH  Ki5.15995.09965.2299 receptor5-HT1D porcine membranecortex; brain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-5-HT 5-HTGIJKLMNOPQRSTUVWXG  Ki6.82396.79596.8539 receptoralpha1bovine membranebrain antagonistGPCRadrenergic receptorepinephrine / norepinephrine[3H]prazosin prazosinY[\]^_`abcdefghijG Ki7.52297.48157.5686 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor histamine[3H]pyrilamine tripolidinekmnopqrstuvwxyz{|}~ Ki4.65964.64404.6757 receptorD1bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390r(+)-butaclamolG  Ki6.95866.92087.0000 receptorD2bovine membranestriatum; brain antagonistGPCRdopaminergic receptor. dopamine[3H]raclopride spiperoneG  Ki7.04587.01777.0757 receptorsigmarat@ membranehippocampus; brain antagonist[3H]-1,3-di-o-tolylguanidine haloperidoleG1,&8HZl% ,??G @5.09155.0915A2rh^V"P>   N | p f \ R L F  x ^ V H 4 (    > 4 "  ~xD ~pfZPF:0&pj\D*"r~th^TJD> hNF8."6,~tjd^:vn`VJ@6*   x IC507.44377.37687.5229 receptor5-HT1Arat hippocampus agonist; forskolin-inducedGPCRserotonergic receptor 5-hydroxytryptamine [alpha-32P]ATP Ki9.39799.37689.4202 receptor5-HT1Abovine membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-8-OH-DPAT buspirone  !"#$%&'()*+,-.G  Ki6.72126.71226.7305 receptoralpha1bovine membranebrain antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosin prazosin/123456789:;<=>?@G  Ki7.15497.07577.2518 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]pyrilamine tripolidine ACDEFGHIJKLMNOPQRST   Ki6.88616.87296.8996 receptorD2bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]raclopride spiperone UWXYZ[\]^_`abcdefG 20BVhDnjnj/Kv@RQ @Cl{SMDL-00036039"J. Med. Chem. 40(6)-1997 952-960(-)-32*O=C(NCCN1CCN(CC1)C2CCCc3ccccc23)c4ccccc4} BHS^5,D EdR&FȚƃB`饶,3l鶩~ʃ!kmC3! ~( ~ȥ&̃~xx$NkN*bm^mejeqp9 !==7&ᕙ 1 iD=5 HCl salt@re IC507.85397.79597.9208 receptor5-HT1Arat hippocampustagonist; forskolin-inducedGPCRserotonergic receptorn5-hydroxytryptamine[alpha-32P]ATPgijklmnopqrstuv% Ki8.82398.79598.8539 receptor5-HT1Abovine membranebrain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]-8-OH-DPAT buspironeG Ki5.69045.63645.7520 receptor5-HT1C porcine membranechoroid plexus; brain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]mesulergineG DȌȌ/ w@Q @x&SMDL-00036040"J. Med. Chem. 40(6)-1997 952-96033-Fc1ccc(cc1)C(=O)NCCN2CCN(CC2)C3CCCc4ccccc34}!OTPBTD 2EE5UX%tF QVنу@(AH MԴMztW aMauWCsWXkWZkWvWC+aWϊkaWMzC4aCjMi#awkj!p=7&ᕙ 1 p,wyz{|~}?? HCl salt @ ~ t j d ^ , n f X N B 8 . "    V v R : L (  BpB *   T L:. Z~rjdXND:4.tT<4&&vlf`(tZlHfTxZJB8," Ki5.92815.89625.9626 receptor5-HT2 bovine membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]ketanserin ketanserin Ki5.45975.37065.5719 receptor5-HT3 NG 108-15 cell antagonistligand-gated ion channelserotonergic receptor 5-hydroxytryptamine [3H]BRL-43694 ICS-205930 !"H  Ki5.01014.98095.0414 receptor5-HT1D porcine membranecortex; brain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-5-HT 5-HT#%&'()*+,-./01234G  Ki7.09697.08627.1079 receptoralpha1bovine membranebrain antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosin prazosin5789:;<=>?@ABCDEFG  Ki6.85396.82396.8861 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]pyrilamine tripolidine GIJKLMNOPQRSTUVWXYZ  Ki4.92084.90524.9370 receptorD1bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390(+)-butaclamol[]^_`abcdefghijklG  Ki7.15497.11357.2007 receptorD2bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]raclopride spiperonemopqrstuvwxyz{|}~G  Ki6.55286.53766.5686 receptorsigmarat membranehippocampus; brain antagonist[3H]-1,3-di-o-tolylguanidine haloperidolGt,$6H\n IC507.28407.21757.3625 receptor5-HT1Arat hippocampusagonist; forskolin-inducedGPCRserotonergic receptor5-hydroxytryptamine[alpha-32P]ATP% G Dʌʌ/ w@Q @x&SMDL-00036042"J. Med. Chem. 40(6)-1997 952-960(-)-33-Fc1ccc(cc1)C(=O)NCCN2CCN(CC2)C3CCCc4ccccc34}!OTPBTD 2EE5UX%tF QVنу@(AH MԴMztW aMauWCsWXkWZkWvWC+aWϊkaWMzC4aCjMi#awkj!p=7&ᕙ 1 p3,??p HCl saltSMDL-00036046IC50p T `j0 ` &  N | r f \ R H @ : ^ > 0    n    |rlf( ~vhTH>8,"^TB4 dzpfZPF<60|dJB4" ( ~tjd^,vn`VJ@6*   Ki9.30109.26769.3372 receptor5-HT1Abovine membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-8-OH-DPAT buspirone  Ki6.55286.52296.5850 receptor5-HT1C porcine membranechoroid plexus; brain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]mesulergine mianserin  !"#$G  Ki5.86015.82685.8962 receptor5-HT2 bovine membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]ketanserin ketanserin%'()*+,-./0123456G  Ki6.90666.88946.9245 receptoralpha1bovine membranebrain antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosin prazosin79:;<=>?@ABCDEFGHG  Ki7.23667.22187.2518 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]pyrilamine tripolidine IKLMNOPQRSTUVWXYZ[\  Ki5.51005.48955.5317 receptorD1bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390(+)-butaclamol]_`abcdefghijklmnG  Ki7.15497.10797.2076 receptorD2bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]raclopride spiperoneoqrstuvwxyz{|}~G  Ki5.80415.71905.9101 receptorD3 membranecortex; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone haloperidoliF ] Ki6.88616.87616.8962 receptorsigmarat membranehippocampus; brain antagonist[3H]-1,3-di-o-tolylguanidine haloperidolG(&8J^p IC507.82397.76967.8861 receptor5-HT1Arat@ hippocampusagonist; forskolin-inducedGPCRserotonergic receptor5-hydroxytryptamine0[alpha-32P]ATP% DΌΌ1\(w@@"~ ,77.3279v BpL 4   ^ ~ r j ` T J @ 6 0 * h | j ^ D < .   " (  zt6 vbVLF:0&lbPB( r~th^TJD>hNF8."6,~tjd^:vn`VJ@6*  p Ki7.76967.76207.7773 receptor5-HT1Abovine membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-8-OH-DPAT buspirone  G  Ki7.18057.11357.2596 receptor5-HT2 bovine membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]ketanserin ketanserin !"#$%&'()*+,G  Ki5.50035.37065.6861 receptor5-HT3 NG 108-15 cell antagonistligand-gated ion channelserotonergic receptor 5-hydroxytryptamine [3H]BRL-43694 ICS-205930-/0123456789:;<H  Ki7.74477.72587.7645 receptoralpha1bovine membranebrain antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosin prazosin=?@ABCDEFGHIJKLMNG  Ki7.37687.34687.4089 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]pyrilamine tripolidine OQRSTUVWXYZ[\]^_`ab Ki6.00005.99236.0079 receptorD1bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390(+)-butaclamolcefghijklmnopqrstG @ Ki6.95866.90667.0177 receptorD2bovine membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]raclopride spiperoneuwxyz{|}~G  Ki7.52297.49497.5528 receptorsigmarat membranehippocampus; brain antagonist[3H]-1,3-di-o-tolylguanidine haloperidoltG$ .>Pdv"J. Med. Chem. 40(6)-1997 952-960MB-35MB-35-Fc1ccc(cc1)C(=O)CCCN2CCN(CC2)C3CCCc4ccccc34}!TSWTPbAH =APMaUX%TFPVن0 IB1$6Q6]61dg]]bmhmh_YY],=k_=+/7Iӄ^͢^ 6Qϫ!H]=7Q& D1 LH] IC506.67786.64216.7167 receptor5-HT1Arat hippocampusagonist; forskolin-inducedGPCRserotonergic receptor5-hydroxytryptamine[alpha-32P]ATP% eD k% 1ԕOmt@Q@-ףp= @SMDL-00040224%J. Med. Chem. 40(25)-1997 4146-41531 clozapine,wJD  X z p h b & f F 8 "    v "   ztn0 ~p\PF@4*  f\J<"lxnbXND>8zbH, 0 |rlf.vn`VJ@6*   ^r Z 6 h ^ : IC506.88616.88616.8861 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390  G  IC506.48156.48156.4815 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone  !"#$%&'G  IC508.10798.10798.1079 receptor5-HT2Arat membranebrain antagonistP14842rat GPCRserotonergic receptor 5-hydroxytryptamine [3H]ketanserin(*+,-./0123456789:  IC507.95867.95867.9586 receptor5-HT2Crat membraneclonedNIH 3T3 cell antagonistP08909rat GPCRserotonergic receptor 5-hydroxytryptamine [3H]mesulergine ;=>?@ABCDEFGHIJKLMN  IC507.63837.63837.6383 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]mepyramineOQRSTUVWXYZ[\]^_`a  IC508.03628.03628.0362 receptoralpha1rat membranebrain antagonistGPCRadrenergic receptorepinephrine / norepinephrine[3H]prazosinbdefghijklmnopqrG )<Pct'CN1CCN(CC1)C2=Nc3cc(Cl)ccc3Nc4ccccc24uuu XS!D 4hURZ5ȑC*"ZJ);E< a$]Ǝ]ݾ# Ÿ{b737[󪘓r$^ 3M:h2&g$N[Q#! ,.ߛ ,IC508.02698.02698.0269 receptorm1human membranecloned CHO-K1 cell@ antagonistP11229human@GPCR; ion channel@#muscarinic acetylcholine receptornacetylcholine0[3H]pirenzepine@suvwxyz{|}~ IC506.03156.03156.0315 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390G @IC505.0915 G 4D""k' 9({@zGz @X9SMDL-00040226%J. Med. Chem. 40(25)-1997 4146-415337CN1CCN(CC1)C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc4ccccc24 PA(%CFMGaETnx$ ud9P 0M0QxY,u^YMWCbUl^JkXbT.)ؘB^R^`T ,UC e"mU.ڌԤeBX!oF- d,?7    ( ` T : 2 $   r  X X 4R *  ` v l f Z P F < 4 . t\TF<0(:6(H~ndXPF:0&^F,$p~tj`XR|tfRF>8,"BJ`&   receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone IC506.25966.25966.2596 receptor5-HT2Arat membranebrain antagonistP14842rat GPCRserotonergic receptor 5-hydroxytryptamine [3H]ketanserin   IC506.20766.20766.2076 receptor5-HT2Crat membraneclonedNIH 3T3 cell antagonistP08909rat GPCRserotonergic receptor 5-hydroxytryptamine [3H]mesulergine  !"#$%&'()*+,-./01  IC506.14276.14276.1427 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]mepyramine256789:;<=>?@ABCD   3FIC507.45597.45597.4559 receptorm1human membranecloned CHO-K1 cell antagonistP11229human GPCR; ion channel #muscarinic acetylcholine receptor acetylcholine [3H]pirenzepine EGHIJKLMNOPQRSTUVWX  IC507.19387.19387.1938 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390dghijklmnopqrstuG  IC507.50867.50867.5086 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperonevxyz{|}~G @IC508.09698.09698.0969 receptor5-HT2Aratr membranebrain@ antagonistP14842rat GPCRserotonergic receptor5-hydroxytryptamine[3H]ketanserin IC507.46857.46857.4685 receptor5-HT2Crat membraneclonedNIH 3T3 cell antagonistP08909ratGPCRserotonergic receptor5-hydroxytryptamine[3H]mesulergine6   ew!D##k' 9({@333333@S㥛 fSMDL-00040227%J. Med. Chem. 40(25)-1997 4146-41534 GMC-11697CN1CCN(CC1)C2=Nc3ccccc3Nc4ccc(OS(=O)(=O)C(F)(F)F)cc24%CA %DCaT @GaET=Bnx (h9uP,L0Q@/Wi;~VISVU|{JY**4԰.6BXBbf vjSǚ`u~U¥ a%!oF- d,Y[\]^_ca`b7 F .   | Z r h \ T J > 4 *   t bV<4&t |tn "L L (@ :  TndZL<2& fvn&zpbRH<4* fB*TvjPH:& 7.32797.3279 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]mepyramineIC507.92087.92087.9208 receptoralpha1rat membranebrain antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinG  IC505.92085.92085.9208 receptorm1human membranecloned CHO-K1 cell antagonistP11229human GPCR; ion channel #muscarinic acetylcholine receptor acetylcholine [3H]pirenzepine "#$%&'()*+,-./0123  Ki9.30109.30109.3010 receptor alpha1a rat membranesubmaxillary gland antagonistP43140rat GPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine>ABCDEFGHIJKLMNOPQR  Ki9.60219.50869.7212 receptoralpha1rat membranesubmaxillary gland antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamineSUVWXYZ[\]^_`abcdG  Ki8.95868.95868.9586 receptor alpha1brat membraneliver antagonistP15823ratGPCRadrenergic receptor0epinephrine / norepinephrine[3H]prazosinphentolamineeghijklmnopqrstuvwx Ki5.79625.71605.8945 receptoralpha2human membraneBSR-2AH cell antagonistGPCRadrenergic receptorepinephrine / norepinephrine[3H]clonidinet clonidiney{|}~K Ki5.74215.74215.7421 receptor alpha2a@human@ membraneBSR-2AH cell antagonistP08913humandGPCRadrenergic receptornepinephrine / norepinephrine [3H]MK-912 @Ki7.25187.25187.2518 receptor alpha2bhuman membrane antagonistP18089human@GPCRadrenergic receptor@epinephrine / norepinephrine[3H]yohimbinea oG 8?Tfz#4GZm~DppC+ 92r4w@Q@Clg@SMDL-00045680%J. Med. Chem. 41(17)-1998 3128-31411L/COc1ccccc1N2CCN(CCn3c(=O)[nH]c4ccccc4c3=O)CC2}PBTG@! QIJ)E& ehцDQSEE@  ,SaֳqVEFegr`T1uŀ'\~Zp1`*Y!&e\I}&eee2[ILe)ʤrhI&|aѳI`!2<.y 2,46789=;:<?7 receptorD3human membrane2rhbVb z r h ^ P D : . "    Z L ,   Z vfZPF:0&z bR2 rpd\RF<2("n^>& j ~* \ $ "P~p`VJ@:.$T4dld\RD:.&  ~Ki5.82105.82105.8210 receptor5-HT1 rat membranecortex; brain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-5-HT  Ki7.79597.79597.7959 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-8-OH-DPAT !G   Ki6.74476.74476.7447 receptor5-HT2 guinea pig membranebrain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]ketanserin"$%&'()*+,-./012G   Ki7.49497.49497.4949 receptorD2human membrane CHO cell antagonistP14416human GPCRdopaminergic receptor dopamine[3H]spiperone 356789:;<=>?@ABCDE   Ki6.87946.87946.8794 receptorD2human membrane CHO cell antagonistP14416human GPCRdopaminergic receptor dopamine[3H]spiperone FHIJKLMNOPQRSTUVWX   Ki7.13677.13677.1367 receptorD3human membrane CHO cell antagonistP35462humanGPCRdopaminergic receptor dopamine[3H]spiperoneY[\]^_`abcdefghijk  Ki6.16436.16436.1643 receptorH1 guinea pig membranelung antagonistGPCRhistaminergic receptor histamine[3H]pyrilaminelnopqrstuvwxyz{|G  Ki5.43425.43425.4342 receptorNa(+) channelrat membranebrain antagonistvoltage-gated ion channel[3H]batrachotoxin}GKi9.18719.11359.2757 receptor alpha1arat membranesubmaxillary gland antagonistP43140rat@GPCRadrenergic receptorepinephrine / norepinephrine[3H]prazosinphentolamine pG @0'9L^oDqqC-`)1w-wx@HzG @ZdSMDL-00045681%J. Med. Chem. 41(17)-1998 3128-31414/COc1ccccc1N2CCN(CC3CN4C(=N3)c5ccccc5NC4=O)CC2օ`B eSJ$1T 1TQ`UPdEHiOqP P ~XyIInP~O8:|c mZw|cJc$JcY;mHY,;m,YWyOG=mYH]FG]mV~c!<ٶ 1P9,?7SMDL-000456825P,??F@.N|B d L D < 2 $   J :  4 | ( ~ x r  |pb\PF<2,&j vjPH>4& vpj*xj^RHB6," b\D*" n|rh^XR|tfTH@6*   Ki9.03158.97479.0969 receptoralpha1rat membranesubmaxillary gland antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine     Ki8.25968.22918.2924 receptor alpha1b rat membraneliver antagonistP15823rat GPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine !"#$%  Ki6.63836.55756.7375 receptoralpha2human membraneBSR-2AH cell antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]clonidine clonidine &()*+,-./01234567K  Ki6.26206.21476.3152 receptor alpha2a human membraneBSR-2AH cell antagonistP08913human GPCRadrenergic receptor epinephrine / norepinephrine [3H]MK-9128:;<=>?@ABCDEFGHIJ  Ki6.59696.55446.6440 receptor alpha2b human membrane antagonistP18089human GPCRadrenergic receptor epinephrine / norepinephrine[3H]yohimbine KMNOPQRSTUVWXYZ[\  Ki5.60215.60215.6021 receptor5-HT1rat membranecortex; brain antagonistGPCRserotonergic receptor5-hydroxytryptamine [3H]-5-HT]_`abcdefghijklmG Ki6.62346.62346.6234 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]-8-OH-DPATnpqrstuvwxyz{|}~G  Ki6.43306.43306.4330 receptor5-HT2 guinea pig membranebrain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]ketanserinG i Ki5.65765.65765.6576 receptorD3human membrane CHO cell antagonistP35462humanGPCRdopaminergic receptor dopamine[3H]spiperone  Ki6.01736.01736.0173 receptorH1 guinea pig membranelung antagonistGPCRhistaminergic receptor histamine@[3H]pyrilamineG mGi 6.0066/COc1ccccc1N2CCN(CC3CN=C4N3C(=O)Nc5ccccc45)CC2rac6ac6.2373f NV` L > $    ^ | r h ^ X R  p h Z P D 6 ,   J F .  X ~th^TJD>nVND:,  6(~tjd^6h`RB6," V>.ztnNxjTH@6*   pKi5.39795.39795.3979 receptorsigma guinea pig membranebrain antagonist[3H]-(+)-pentazocine     Ki9.58509.55289.6198 receptor alpha1a rat membranesubmaxillary gland antagonistP43140rat GPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine !"#$%Ki9.67789.63839.7212 receptoralpha1rat membranesubmaxillary gland antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine&()*+,-./01234567G  Ki9.17399.14279.2076 receptor alpha1b rat membraneliver antagonistP15823rat GPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine8:;<=>?@ABCDEFGHIJK  Ki6.22696.22266.2314 receptoralpha2human membraneBSR-2AH cell antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]clonidine clonidine LNOPQRSTUVWXYZ[\]K uKi6.80976.80976.8097 receptor5-HT1Arat membranecortex; brain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]-8-OH-DPAT^`abcdefghijklmnG 6 Ki6.42376.42376.4237 receptor5-HT2 guinea pig membranebrain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]ketanserinoqrstuvwxyz{|}~G  Ki6.80136.80136.8013 receptorD2human. membrane CHO cell antagonistP14416humanbGPCRdopaminergic receptorP dopamine[3H]spiperone  Ki6.62166.62166.6216 receptorD2human membrane CHO cell antagonistP14416humanGPCRdopaminergic receptor dopamine[3H]spiperone @ Ki6.00666.0066 DrrC-`)1w-wx@HzG @Zd%J. Med. Chem. 41(17)-1998 3128-3141օ`B QODG 2T -TQ `UPdEI=HirP P :YiaI{: ]z8*z­ Kr lwxw\X]nxdh'hgΎ(ρ!<ٶ 6.3947 receptorH1xn ~ 4 ~ r f \ V J @ 6 , & v p d J B 8 .     |rlf$ |n\PH>2(^\J* jxnbZNB8.$jZ:" zvjbVJ@6,& <  J B rdZN@6*    CHO cell antagonistP35462human GPCRdopaminergic receptor dopamine[3H]spiperone  Ki5.63455.63455.6345 receptorH1 guinea pig membranelung antagonistGPCRhistaminergic receptor histamine [3H]pyrilamine    G  ,'9M_p Ki5.20275.20275.2027 receptorsigma guinea pig membranebrain antagonist[3H]-(+)-pentazocine !"#$%&'(G 4Ki8.61628.61628.6162 receptor alpha1a human recombinant antagonistP35348human GPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosin7:;<=>?@ABCDEFGHI  Ki5.43655.43655.4365 receptor alpha1b rat recombinant antagonistP15823rat GPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinJLMNOPQRSTUVWXYZ[  Ki5.06005.06005.0600 receptor alpha1de canine; dog1 recombinant@ antagonistGPCRadrenergic receptorepinephrine / norepinephrine[3H]prazosin\^_`abcdefghijkE Ki6.11925.93746.4377 receptor alpha2aehumanl recombinant antagonistP08913human1GPCRadrenergic receptorgepinephrine / norepinephrine[3H]rauwolscine]lnopqrstuvwxyz{|} Ki5.89255.82515.9722 receptor alpha2bhumanb recombinanto antagonistP18089humanGPCRadrenergic receptorpepinephrine / norepinephrine[3H]rauwolscine~  Ki5.64905.62915.6698 receptor alpha2chuman recombinant antagonistP18825humanGPCRadrenergic receptorepinephrine / norepinephrine[3H]rauwolscine Ki6.3089  DA 4 . ( v V > 6 , "    ~rh^TNHzbZL<,  @<LrbXL@6,"L zhpz ,.  R 4bZLB6(r ztn\P6.$ human recombinant antagonistP35367human GPCRhistaminergic receptor histamine [3H]pyrilamineKi6.36966.28746.4711 receptor5-HT1Ahuman recombinant antagonistP08908human GPCRserotonergic receptor 5-hydroxytryptamine [3H]-5-HT     $8K]m 5.44015.7799 receptor5-HT1Bhuman recombinant antagonistP28222human GPCRserotonergic receptor 5-hydroxytryptamine [3H]-5-HT  !"#$%&'()*+  D27.40007.30007.5000 receptorH3rat cortexelectrically-inducedantagonist; contraction Q9QYN8rat GPCRhistaminergic receptor histamine 7:;<=>?@ABCDEFGHI  D27.40007.30007.5000 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine JLMNOPQRSTUVWXYe  D28.20008.10008.3000 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor histamine2![3H]-(R)-Nalpha-methylhistamineeZ\]^_`abcdefghijkl D26.10006.00006.2000 receptorH2 guinea pigatriumelectrically-inducedantagonist; contractionGPCRhistaminergic receptor histamine0mopqrstuvwxyz{|e 8K[n~D  Lbbq[@\(\翺I +?ffffff9SMDL-00050955$J. Med. Chem. 42(7)-1999 1115-1122 histamine histamineNCCc1c[nH]cn1-QTabBu0 @gcDcL3lD}fiQs!@<!2 "  r  \dn  n \  (V ~ r d ^ R H > 4 . ( x *8|n\PHB6," x`F>" n|rh^XR x j D 2  " tlbXJ:0&J4~Bl^D<2( z histamine D26.15006.07006.2300 receptorH3 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine      e  D27.60007.50007.7000 receptorH3rat membranecortex; brain antagonistQ9QYN8rat GPCRhistaminergic receptor histamine ![3H]-(R)-Nalpha-methylhistamine  !"#$  D24.90004.80005.0000 receptorH2 guinea pigatriumelectrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine %'()*+,-./01234e  &6D24.50004.40004.6000 receptorH1 guinea pig jejunum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine 589:;<=>?@ABCDEe  + PS abs TV QUXD27.08006.93007.2300 receptorH3rat cortexelectrically-inducedantagonist; contraction Q9QYN8rat GPCRhistaminergic receptor histamineZ]^_`abcdefghijkl D26.64006.58006.7000 receptorH3 guinea pig jejunumelectrically-inducedantagonist; contractionGPCRhistaminergic receptor histaminemopqrstuvwxyz{|e D28.76008.66008.8600 receptorH3rat membranecortex; brain antagonistQ9QYN8ratGPCRhistaminergic receptor histamine![3H]-(R)-Nalpha-methylhistamine} D24.80004.70004.9000 receptorH2 guinea pigatriumelectrically-inducedantagonist; contractionGPCRhistaminergic receptor histamine0e [n~D  L9ߡ(^@R Q?\SMDL-00050957$J. Med. Chem. 42(7)-1999 1115-11221b VUF-5297N[C@H]1C[C@@H]1c2c[nH]cn25 QQTXed!UVCcեZ5GWJ3m!|?}4k ěp2,GHIJKOMLNS,S3WYD25.00004.90005.1000 receptorH1 guinea pig jejunum@electrically-inducedantagonist; contractionGPCRhistaminergic receptor histaminepe o,         wmSMDL-000521979a7mp^vX$Rx ^ V : "     t \ R D > 2 (     V F 8     j xrf\RHB<vnf\@(^ 4  ~ " Z t |pf\RLF0jbF.$( |rlf<|dXJD8.$^ |IC507.44377.44377.4437 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390                G  IC508.12498.12498.1249 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone     ! " # $ % & ' ( ) * + , G  IC508.30988.30988.3098 receptorD2human membranecloned A9L cell antagonistP14416human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamol- / 0 1 2 3 4 5 6 7 8 9 : ; < = > ? @ A   IC508.00008.00008.0000 receptorD3human membranecloned CHO cell antagonistP35462human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamolB D E F G H I J K L M N O P Q R S T U V   IC508.18718.18718.1871 receptorD4.2human membranecloned CHO-K1 cell antagonistGPCRdopaminergic receptor dopamine[3H]spiperone(+)-butaclamolW Y Z [ \ ] ^ _ ` a b c d e f g h i O  IC507.25967.25967.2596 receptor5-HT2Arat membranecortex; brain antagonistP14842ratGPCRserotonergic receptor@5-hydroxytryptaminee[3H]ketanserinj l m n o p q r s t u v w x y z { |   IC50 <6.0000 receptor5-HT2Crat membraneclonedNIH 3T3 cell antagonistP08909ratGPCRserotonergic receptorC5-hydroxytryptamine[3H]mesulerginer}                  yIC50 <6.0000 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor histamine[3H]mepyramine                  IC507.74477.74477.7447 receptoralpha1ratr membranebrain antagonistGPCRadrenergic receptor0[3H]prazosin               G o(  . C X k ~    D;+`( N`}w@@Qk333333@ŏ1 SMDL-00052193%J. Med. Chem. 42(12)-1999 2235-22445 haloperidol.OC1(CCN(CCCC(=O)c2ccc(F)cc2)CC1)c3ccc(Cl)cc3y @UP!t02TBTqQCb#G@"BI! Bt__CQr&e4&Qt5jsP놕4@֫4:aMe9!Q0 ;`  AFQ IC506.25966.25966.2596 receptorm1human membranecloned bVLF:0&l z r h \ R H > 6 0 d r X P H > 0 &   ( 4   |H r`TLB6," tZH<" l~th^XLB8.& p^R80&~tj`XR|tfRF>8,"l J, \   t CHO-K1 cell antagonistP11229human GPCR; ion channel muscarinic acetylcholine[3H]pirenzepine                  IC506.88616.88616.8861 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390             ! " # $ G  IC506.48156.48156.4815 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone % ' ( ) * + , - . / 0 1 2 3 4 5 G  IC506.58506.58506.5850 receptorD2human membranecloned A9L cell antagonistP14416human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamol6 8 9 : ; < = > ? @ A B C D E F G H I J   IC506.34686.34686.3468 receptorD3human membranecloned CHO cell antagonistP35462human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamolK M N O P Q R S T U V W X Y Z [ \ ] ^ _   IC507.28407.28407.2840 receptorD4.2human membranecloned CHO-K1 cell antagonistGPCRdopaminergic receptor dopamine[3H]spiperone(+)-butaclamol` b c d e f g h i j k l m n o p q r O @IC507.92087.92087.9208 receptor5-HT2Arat membranecortex; brain antagonistP14842ratGPCRserotonergic receptor5-hydroxytryptamine[3H]ketanserins u v w x y z { | } ~         rIC507.95867.95867.9586 receptor5-HT2Crate membraneclonedNIH 3T3 cell antagonistP08909rateGPCRserotonergic receptort5-hydroxytryptamines[3H]mesulergine                    oIC507.63837.63837.6383 receptorH1rat@ membranebrain antagonistP31390ratGPCRhistaminergic receptor histamine@[3H]mepyramine                   0G n( & 7 L a t   D;% 1ԕOmt@Q@-ףp= @ SMDL-00052194%J. Med. Chem. 42(12)-1999 2235-2244 4 clozapine 'CN1CCN(CC1)C2=Nc3cc(Cl)ccc3Nc4ccccc24uuu XS!D 4hURZ5ȑC*"ZJ);E< a$Ԧhjʮ–*BA%㡂l+!XG)wA"k5sX^i+`.! ,.ߛ 2,9,         G 7CN1CCN(CC1)C2=Nc3ccccc3Nc4ccc(OS(=O)(=O)C(F)(F)F)cc24human membranerane@pf$,b z p b X L D > 2 (    Z T < "    h nbZPD:0& hVJ0( zvlfZPF<4. ~l`F>4*&xnf`t`TLF:0&j X( R   dH2(x |  IC508.03628.03628.0362 receptoralpha1rat membranebrain antagonistGPCRadrenergic receptor [3H]prazosin       IC508.02698.02698.0269 receptorm1human membranecloned CHO-K1 cell antagonistP11229human GPCR; ion channel muscarinic acetylcholine[3H]pirenzepine  !"  IC507.19387.19387.1938 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390 ,-./0123456789:IC507.50867.50867.5086 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone ;=>?@ABCDEFGHIJKG  IC506.85396.85396.8539 receptorD2human membranecloned A9L cell antagonistP14416human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamolLNOPQRSTUVWXYZ[\]^_`  IC507.27577.27577.2757 receptorD3human membranecloned CHO cell antagonistP35462humanGPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamolacdefghijklmnopqrstu oIC506.92086.92086.9208 receptorD4.2human membranecloned CHO-K1 cell antagonistGPCRdopaminergic receptor dopamine[3H]spiperone(+)-butaclamolvxyz{|}~O pIC507.36657.36657.3665 receptor5-HT2Arat@ membranecortex; brain@ antagonistP14842ratoGPCRserotonergic receptorp5-hydroxytryptamine][3H]ketanserin IC507.46857.46857.4685 receptor5-HT2Crat membraneclonedNIH 3T3 cell antagonistP08909ratGPCRserotonergic receptor5-hydroxytryptamine@[3H]mesulerginea r 9(*<Mbw$D;' 9({@333333@S㥛 +%J. Med. Chem. 42(12)-1999 2235-22449 GMC-1169%CA %DCaT @xGaE!UT=Bn8 \qP,L0Q@]^t՝^AYLVfњZɂc󮘆aʞ^u#RRKar#U%~+!oF- 4dM,$%& (')9c,456:879?75-FLz | r f ^ T H > 4 * "  l T : 2 *  ~  |th^TJB< znTLB8*4|pf\RJD"nfXD80* <J>$ \ D 8  |rl`VLB:4 vn`VJB8," IC507.32797.32797.3279 receptorH1rat membranebrain antagonistP31390rat GPCRhistaminergic receptor histamine [3H]mepyramine      IC507.92087.92087.9208 receptoralpha1rat membranebrain antagonistGPCRadrenergic receptor [3H]prazosin !"G   IC50 <6.0000 receptorm1human membranecloned CHO-K1 cell antagonistP11229human GPCR; ion channel muscarinic acetylcholine[3H]pirenzepine #%&'()*+,-./0123  IC506.03156.03156.0315 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390 ;>?@ABCDEFGHIJKLG  IC505.09155.09155.0915 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone MOPQRSTUVWXYZ[\]G  IC506.25966.25966.2596 receptor5-HT2Arat membranecortex; brain antagonistP14842ratGPCRserotonergic receptor5-hydroxytryptamine[3H]ketanserin^`abcdefghijklmnop tIC506.20766.20766.2076 receptor5-HT2Crat membraneclonedNIH 3T3 cell antagonistP08909ratGPCRserotonergic receptor5-hydroxytryptamine [3H]mesulergine9qstuvwxyz{|}~ IC506.14276.14276.1427 receptorH1rat. membranebraine antagonistP31390rataGPCRhistaminergic receptor histamine0[3H]mepyramine  IC50 <6.0000 receptoralpha1rat@ membranebrain antagonistGPCRadrenergic receptor[3H]prazosinG @<N_rD;' 9({@zGz @X9=SMDL-00052199%J. Med. Chem. 42(12)-1999 2235-22447CN1CCN(CC1)C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc4ccccc24 PA(%CFMrGaE!UTnx$ u\P 0M0Q}*P6|ݔf]4 :>JŘ YuAz:֝ffe)QNb1UٯFT.e!oF- d IC507.45597.45597.4559 receptorm1    \ D < . $    l  0 "  B xh^RJ@4* | X@& j|pf\RJDnfXD80*  < n ( @$TvlbZT|tj\RF>8," cloned CHO-K1 cell antagonistP11229human GPCR; ion channel muscarinic acetylcholine[3H]pirenzepine IC507.18057.18057.1805 receptorD1rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]SCH-23390  !"#$G  IC507.39797.39797.3979 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone %'()*+,-./012345G  IC507.28407.28407.2840 receptorD2human membranecloned A9L cell antagonistP14416human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamol689:;<=>?@ABCDEFGHIJ  IC507.53767.53767.5376 receptorD3human membranecloned CHO cell antagonistP35462human GPCRdopaminergic receptor dopamine[3H]spiperone (+)-butaclamolKMNOPQRSTUVWXYZ[\]^_  IC506.82396.82396.8239 receptorD4.2human membranecloned CHO-K1 cell antagonistGPCRdopaminergic receptord dopamine[3H]spiperone@(+)-butaclamol`bcdefghijklmnopqrO IC507.31887.31887.3188 receptor5-HT2Arat membranecortex; brain3 antagonistP14842rattGPCRserotonergic receptor@5-hydroxytryptaminen[3H]ketanserinsuvwxyz{|}~ IC507.00007.00007.0000 receptor5-HT2Crata membraneclonedNIH 3T3 cell antagonistP08909ratPGPCRserotonergic receptor-5-hydroxytryptamine3[3H]mesulergine IC506.92086.92086.9208 receptorH1rat membranebrain antagonistP31390ratGPCRhistaminergic receptor histamine[3H]mepyramine @ IC507.56867.5686  G (&7Lat D;'HpU{@@X9vSMDL-00052206%J. Med. Chem. 42(12)-1999 2235-224418a7CN1CCN(CC1)C2=Nc3ccccc3Oc4ccc(OS(=O)(=O)C(F)(F)F)cc24%CA1QCT @xFaE!UT=Bn8 \qP8đ,L0Q@]^՝^tAYL WfѲZɚcƘaʶ^6u;RRc*a#V &+!o2FM-  ,    ?7 &  z 8 | n ^ T H @ 6 *    r N6 `~th^VJ@6,$n\P6.$ znd^RH>4,&vjPH:& $ 6H H $@   P~nR<2( 7.5686 receptoralpha1rat membranebrain antagonistGPCRadrenergic receptor [3H]prazosin IC506.30986.30986.3098 receptorm1human membranecloned CHO-K1 cell antagonistP11229human GPCR; ion channel muscarinic acetylcholine[3H]pirenzepine    )D %qqUq@Q@bX9*SMDL-00057263 $J. Med. Chem. 43(6)-2000 1071-10848 $NCCc1c[nH]c(n1)C(c2ccccc2)c3ccccc3gUo X(Q!F(AbE D!lCF)Q<A$ .uK&I]sMҽ==FGɉ?/'΅˃:7mÂ]N5D7}2 !t?-6ۋq  , !"#'%$&?7 EC505.59005.48005.7000 receptorH1 guinea pigsmooth muscle ileum agonist contraction GPCRhistaminergic receptor histamine (+,-./0123456789g  EID '9J^c6r@F ףp= @ʡEJSMDL-00057264 $J. Med. Chem. 43(6)-2000 1071-10849 %NCCc1c[nH]c(CC(c2ccccc2)c3ccccc3)n1 keq P'(Q &LĆ'Q5"t0P ڨ+k`y^¨ &蹿)[  ! t?)6#<[q  ,:<=>?CA@B?? maleic acid saltDG EC504.39004.34004.4400 receptorH1 guinea pigsmooth muscle ileum agonist contraction GPCRhistaminergic receptor histamine HKLMNOPQRSTUVWXYg  fEC506.74006.72006.7600 receptorH1 guinea pigsmooth muscleileum agonist contractionGPCRhistaminergic receptor histamineilmnopqrstuvwxyzg EC505.71005.69005.7300 receptorH1 guinea pigendothelium denudedaaorta agonist contractionGPCRhistaminergic receptor histaminer{}~g  j|D )Js@g ףp= @S㥛 kSMDL-00057265$J. Med. Chem. 43(6)-2000 1071-108410histaprodifeni&NCCc1c[nH]c(CCC(c2ccccc2)c3ccccc3)n1qus PNa+&LĈ&Q",`o(gq( ! YjGjz)) Bh)5ϪF)ߋ! t?)k<Sq$ ,Z\]^_`dbac?0maleic acid salteh000EC506.51006.47006.5500 receptorH1 guinea pigintact endothelium; aortal agonistn contractiontGPCRhistaminergic receptor histaminee @D +K7As@\(\@Mb SMDL-00057266$J. Med. Chem. 43(6)-2000 1071-108413!t)k<9Sq,??6.7200 receptorH1g NCCc1c[nH]cn1@H1rf\x (V x j d X N D : 2 , x ~ t \ N H < 2 (    ` dJB2& h r   & 4 v  ~tlfBV`LtF <xpjz. tN<6d>" |RlTL>4(  EC507.24007.22007.2600 receptorH1 guinea pigsmooth muscle ileum agonist contraction GPCRhistaminergic receptor histamine    g  EC506.31006.28006.3400 receptorH1 guinea pigendothelium denuded aorta agonist contraction GPCRhistaminergic receptor histamine  !"#$%&'()*g  ,'CNCCc1c[nH]c(CCC(c2ccccc2)c3ccccc3)n1 uu PNa+&LĈQDDYb1d "%P#&PB&f&!(&ZRfS:Sj:U՟&S , oxalic acid salt EC507.11007.04007.1800 receptorH1 guinea pigintact endothelium; aorta agonist contraction GPCRhistaminergic receptor histamine +-./0123456789:e  FEC507.08007.04007.1200 receptorH1 guinea pigsmooth muscle ileum agonist contraction GPCRhistaminergic receptor histamine ILMNOPQRSTUVWXYZg  EC506.08006.04006.1200 receptorH1 guinea pigendothelium denudedaortae agonist@ contractionGPCRhistaminergic receptor histamine[]^_`abcdefghijkg  J\mD -#t@G333333@x&1KSMDL-00057267$J. Med. Chem. 43(6)-2000 1071-108414*CN(C)CCc1c[nH]c(CCC(c2ccccc2)c3ccccc3)n1yw PN !„(*TADoŃbC|K?KMDT/!#|)k<9SqR4#t,;=>?@DBAC??oxalic acid saltEHEC506.92006.85006.9900 receptorH1 guinea pigintact endothelium; aorta@ agonist contractionGPCRhistaminergic receptor histaminelnopqrstuvwxyz{e D -#t@RQ@S%SMDL-00057268t$J. Med. Chem. 43(6)-2000 1071-108415(CCNCCc1c[nH]c(CCC(c2ccccc2)c3ccccc3)n1yw PNa+&LADoŃbPC>LtGLƢ 4M9,M0LVQL+C ,4s[LT`Դ= +>cN\l!/!|t)k<Sq4|,|~??toxalic acid salt084EC506.52006.48006.5600 receptorH1 guinea pigsmooth muscleileum agonist contractionGPCRhistaminergic receptor histamineg g, ??EC506.70006.6800[\]^_`abeis   ~ t j b \  8 L V 2 \ ,   2 z p f \ T N  vpdZPF>8rjZND2$0* > H "N$ 4Bzpf^XzndRD>2( Ph|` ybd~5xQ+nCGFFFFijgeQxZ5*-F # ;[<}2RVQV "Z" $^$&e&(o(#*{*#,{,*.}.10y02]224>4a444 6@6`66{8Z5*-F # ;[<}XX[[[[[[[[[[HtItJtKtLtMtNtOtPtQtRtStTtUtVtWtXtYtZt\t]tƌnjȌʌΌ "#pqr =nstuvxyz{|}"#$%Ό "#pqr  EC506.83006.79006.8700 receptorH1 guinea pigsmooth muscle ileum agonist contraction GPCRhistaminergic receptor histamine g  !D /*"*ޗu@ (\@ ףp=SMDL-00057269 $J. Med. Chem. 43(6)-2000 1071-108416-C(Cc1c[nH]c(CCC(c2ccccc2)c3ccccc3)n1)NC4CC4 { PPXq&`xaF&QXR1 b%BP#&P-&&/M~%&>^(&~̡9SS՟&FSjvS !O|?)6k<Sq :O oxalic acid salt   EC505.64005.61005.6700 receptorH1 guinea pigendothelium denuded aorta agonist contraction GPCRhistaminergic receptor histamine "#$%&'()*+,-./0g  <@D 1 Mxv@=Gz@CASMDL-00057270i$J. Med. Chem. 43(6)-2000 1071-108417.C(Cc1nc(CCN2CCCC2)c[nH]1)C(c3ccccc3)c4ccccc4} PZPABĉ)LbpW"I&"jsŃDa@C>LlGLƢ|V 4ML9M/ƛQL[;|V +3 ,4ۨ3SNLԴ=*>S!/!9|)k<SqB9,13456:879??oxalic acid salt;>EC506.53006.48006.5800 receptorH1 guinea pigsmooth muscleileum agonist contractionGPCRhistaminergic receptor histamine?BCDEFGHIJKLMNOPg  guinea pigsmooth muscleileum agonist@ contraction0GPCRhistaminergic receptor histaminemEC505.65005.63005.6700 receptorH1 guinea pigendothelium denudedaorta@ agonist contractionGPCRhistaminergic receptor histaminecfghijklmnopqrstg h dvD Lbbq[@\(\翺I +?ffffffSMDL-00057271$J. Med. Chem. 43(6)-2000 1071-10841 histamine-QTab$u0 ZWD ϱZ ; W !@<!2 2 (    ~  x n \ N  p * F p d Z H : 4 (    8 F 2  x > ldTH>&*|l`VD60$JBT xx6.50006.46006.5400 receptorH1 guinea pigintact endothelium; aorta agonist contraction GPCRhistaminergic receptor histamine S  +  Ki <5.6990 receptor alpha1b human membranecloned CHO cell antagonistP35368human GPCRadrenergic receptor epinephrine / norepinephrine [125I]HEAT!$%&'()*+,-./0123  Ki7.28407.24417.3279 receptor alpha1d human membranecloned CHO cell antagonistP25100human GPCRadrenergic receptor epinephrine / norepinephrine [125I]HEAT46789:;<=>?@ABCDEFG  Ki9.48159.44379.5229 receptor alpha1a human membranecloned CHO cell antagonistP35348human GPCRadrenergic receptor epinephrine / norepinephrine [3H]MK-912 WB-4101 HJKLMNOPQRSTUVWXYZ[\  Ki6.77216.72826.8210 receptor alpha2b rat membranecortex; kidney antagonistP19328ratiGPCRadrenergic receptorepinephrine / norepinephrine[3H]yohimbinephentolamine]_`abcdefghijklmnop Ki7.63837.52297.7959 receptorD2Lahuman@ membranecloned CHO cell antagonistGPCRdopaminergic receptor dopamine[3H]spiperone haloperidolqstuvwxyz{|}~O Ki7.60217.52297.6990 receptorD2Sahumann membranecloned CHO cell antagonistGPCRdopaminergic receptor] dopamine[3H]spiperone@ haloperidolO Ki7.20767.16757.2518 receptorD3human membranecloned CHO cell antagonistP35462humanGPCRdopaminergic receptor dopamine[3H]spiperone sulpiride @ Ki6.11926.05706.1918 receptorCa(2+) channelrat membranecortex; brainGD==D C ~rXPB6, 6*zpf\VP:x`XND6*  HvlbXRL*h`VL>2(& DDLV  r , >xh\>0* t antagonistvoltage-gated ion channel L-type[3H]nitrendipine nifedipine Ki7.42027.34687.5086 receptorH1 guinea pig membranecortex; brain antagonistGPCRhistaminergic receptor central histamine [3H]pyrilamine pyrilamine     G  Ki6.11185.96946.3251 receptor5-HT1 rat membranecortex; brain antagonistGPCRserotonergic receptor 5-hydroxytryptamine [3H]-5-HT 5-HT !"#$%&'()*+G   Ki7.82397.69908.0000 receptor5-HT1Ahuman membranecloned CHO cell antagonistP08908human GPCRserotonergic receptor 5-hydroxytryptamine [3H]-8-OH-DPAT metergoline ,./0123456789:;<=>?@  0"5I^r-B Ki8.00007.92088.0969 receptor5-HT7 human membranecloned CHO cell antagonistP34969human GPCRserotonergic receptor 5-hydroxytryptamine [3H]lysergic acid diethylamide5-HTACDEFGHIJKLMNOPQRSTU  maleic acid salt^a _cKi8.23668.20078.2757 receptorH3rat synaptosomecortex; brainK(+)-induced3antagonist; [3H]histamine release; depolarizationQ9QYN8ratGPCRhistaminergic receptor histamineehijklmnopqrstuvwx A27.00007.00007.0000 receptorH3 guinea pigsmooth muscleileumelectrically-inducedantagonist; contraction GPCRhistaminergic receptor histaminey{|}~g D2 <4.0000 receptorH2 guinea pigsmooth muscle@atrium; heartagonist; electrically-induced@ contractionGPCRhistaminergic receptor histamine g fzDnn (nn@`p= ף@L7A`g%J. Med. Chem. 43(17)-2000 3335-33431CC(O)c1ccc(OCCCc2c[nH]cn2)cc1[%g`TP1\d…BE)bH!E Uk j4|{$smxө\g7 WoVg\7mnKm+g \cgǖm! g   /@!COC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 a5i`Б(1c a :@ ;Z; fav*e1^vO"(Of(*fYճe !0= r zndZPJDhVD60$`N4,\|lZJB<0& h.4>z& maleic acid salt     Ki8.82398.74478.9208 receptorH3rat synaptosome cortex; brain K(+)-induced3antagonist; [3H]histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor histamine                ! " #   A26.20006.20006.2000 receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine $ & ' ( ) * + , - . / 0 1 2 3 4 g  A2 <4.3000 receptorH2 guinea pigsmooth muscle atrium; heart electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine 5 7 8 9 : ; < = > ? @ A B C g   % 6 E Duu  )^ Dp@ \(\?On SMDL-00060277 %J. Med. Chem. 43(17)-2000 3335-3343 8 !NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 a5i`"06QbF a$< @ c`'PSb$,lN,ƫS]XI?k]?El;l?[?{l !/?u+E.y5yD9¶Tb=եTTT63}6j65!W,/< 1 W,,U W X Y Z ^ \ [ ] ??ncc e  A24.90004.90004.9000 receptorH1 guinea pigsmooth muscleileumelectrically-inducedGPCR             "g g ~ x r   x r l , j ` N @ : . $    d X>6.$~x f\ b l Jn^hb \ 4 " ( V |`H>, B~lZLF:.("xv\T8 rjdXND:4.$<  histamine maleic acid salt ""  ""Ki9.35659.22919.5376 receptorH3rat synaptosome cortex; brain K(+)-induced3antagonist; [3H]histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor histamine """""""""""" "!"""#"$"%"  A28.00008.00008.0000 receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine &"(")"*"+","-"."/"0"1"2"3"4"5"6"g  D23.80003.80003.8000 receptorH2 guinea pigsmooth muscle atrium; heart agonist; electrically-induced contraction GPCRhistaminergic receptor histamine 7"9":";"<"=">"?"@"A"B"C"D"E"F"G"g  "'"8"I"Dxx |(un@ "@K7A` "SMDL-00060280 %J. Med. Chem. 43(17)-2000 3335-3343 11ON=Cc1ccc(OCCCc2c[nH]cn2)cc1_%gdTPĎX„ !F   H.D ǦH\\8;=v;}h{׍p||h;x0z !>W2($O$Dzz  )^ Dp@$p= ף?:v$SMDL-00060282 %J. Med. Chem. 43(17)-2000 3335-3343 !NC(=NO)c1ccc(OCCCc2c[nH]cn2)cc1 c5i`$*Б&2QbF q$< @ @!N_`)e'N(!(($_ v!ڞu#!&&>$$e& !V/?W(&?&@&A&B&C&g  D23.90003.90003.9000 receptorH2 guinea pigsmooth muscle atrium; heart agonist; electrically-induced contraction GPCRhistaminergic receptor histamine D&F&G&H&I&J&K&L&M&N&O&P&Q&R&S&T&g   &4&E&V&SMDL-00060284 %J. Med. Chem. 43(17)-2000 3335-3343 CC(NO)c1ccc(OCCCc2c[nH]cn2)cc1a5i`TP5dd"ŋT b@< $jjh+Jg+j<c82D*"RvdVPD:0& znTLD:|",`t~<^~f\J<6*   antagonist; contraction GPCRhistaminergic receptor histamine D24.90004.90004.9000 receptorH1 guinea pigsmooth muscle ileum agonist; electrically-induced contraction GPCRhistaminergic receptor histamine ((( ( ( ( ( (((((((((g  maleic acid salt (#( !(%(Ki8.08098.04588.1192 receptorH3rat synaptosome cortex; brain K(+)-induced3antagonist; [3H]histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor histamine '(*(+(,(-(.(/(0(1(2(3(4(5(6(7(8(9(:(  A26.90006.90006.9000 receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine ;(=(>(?(@(A(B(C(D(E(F(G(H(I(J(K(g  D23.80003.80003.8000 receptorH2 guinea pigsmooth muscle atrium; heart agonist; electrically-induced contraction GPCRhistaminergic receptor histamine L(N(O(P(Q(R(S(T(U(V(W(X(Y(Z([(\(g  ((<(M(^(D `)X4r@"(= ףp=@Cl)(SMDL-00060287%J. Med. Chem. 43(17)-2000 3335-334318'CC(=NNC(=O)N)c1ccc(OCCCc2c[nH]cn2)cc1qeo JHGx 6fThAa T a{7/c!%(rT-;B*-fB{z'DTjz't!E7  nVL:,&P |tdB0 :(xrl6VF4$ BdxTvlbXRL>$ D24.50004.50004.5000 receptorH2 guinea pigsmooth muscle atrium; heart agonist; electrically-induced contraction GPCRhistaminergic receptor histamine (******* * * * * ****D24.60004.60004.6000 receptorH1 guinea pigsmooth muscle ileum agonist; electrically-induced contraction GPCRhistaminergic receptor histamine ************** *!*g  maleic acid salt,*/* -*1*Ki8.34688.26768.4437 receptorH3rat synaptosome cortex; brain K(+)-induced3antagonist; [3H]histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor histamine 3*6*7*8*9*:*;*<*=*>*?*@*A*B*C*D*E*F*  A27.90007.90007.9000 receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine G*I*J*K*L*M*N*O*P*Q*R*S*T*U*V*W*g  D24.70004.70004.7000 receptorH2 guinea pigsmooth muscle.atrium; heart@agonist; electrically-induceds contraction GPCRhistaminergic receptor histaminemX*Z*[*\*]*^*_*`*a*b*c*d*e*f*g*h*g 4*H*Y*j*D !(R5q@.*(\@)\5*SMDL-00060289%J. Med. Chem. 43(17)-2000 3335-3343020#CCCC(=NO)c1ccc(OCCCc2c[nH]cn2)cc1hkUmdTP'($  Qb4)d`Pr,b>>6\ÿ\ \{8\}哜 ۓ4o9<ȓ60$\~n |rlf.n\J<6*   D25.00005.00005.0000 receptorH2 guinea pigsmooth muscle atrium; heart agonist; electrically-induced contraction GPCRhistaminergic receptor histamine *,,,,,, , , , , ,,,,,**,,D24.90004.90004.9000 receptorH1 guinea pigsmooth muscle ileum agonist; electrically-induced contraction GPCRhistaminergic receptor histamine ,,,,,,,,,,,,, ,!,",g  maleic acid salt,,/, -,1,Ki8.35658.23668.5229 receptorH3rat synaptosome cortex; brain K(+)-induced3antagonist; [3H]histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor histamine 3,6,7,8,9,:,;,<,=,>,?,@,A,B,C,D,E,F,  A27.60007.60007.6000 receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine G,I,J,K,L,M,N,O,P,Q,R,S,T,U,V,W,g  D24.70004.70004.7000 receptorH2 guinea pigsmooth muscleeatrium; heartagonist; electrically-induced contractiondGPCRhistaminergic receptor histaminezX,Z,[,\,],^,_,`,a,b,c,d,e,f,g,h,g 4,H,Y,j,D !(&eq@.,333333@X95,SMDL-000602920%J. Med. Chem. 43(17)-2000 3335-334323%ON=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2lmUoUPV 1d2"`E 4ȨД: b@u)w\!+ uM.;/zR9pFS$$v8050$s$;30,!#J?EW(< ;1 #J,,($,%,&,',+,),(,*,asu0,2,D25.00005.00005.0000 receptorH1 guinea pigsmooth muscleileumagonist; electrically-induced contractionGPCRhistaminergic receptor histaminei,k,l,m,n,o,p,q,r,s,t,u,v,w,x,y,g maleic acid salt,,060,,Ki6.43066.31346.5918 receptorH3rat synaptosome@cortex; brain,K(+)-induced3antagonist; [3H]histamine release; depolarizationQ9QYN8ratGPCRhistaminergic receptor histamine,,,,,,,,,,,,,,,,,, zA26.20006.20006.2000,,,,,,........ . .g ,, ..D 8#Edr@,Q @p= ף,SMDL-00060298%J. Med. Chem. 43(17)-2000 3335-334327#COc1cc(OCCCc2c[nH]cn2)ccc1C(=NO)CkUm$ЩU"ɱD`Q# 3Ȣ2`Fs/$G LXU젙gȠULM K )^yKI)ޏJ).!;}w{(<sq  ;,z,|,},~,,,,,,??asu,,,P F < 6 0 Z j b Z P  ( v H $ b P P~ v l Z L F : 0 &    n n\J<6*  fT:2br`PHB6," n .2~x@n\J<6*  f  receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine A2 <4.3000 receptorH2 guinea pigsmooth muscle atrium; heart electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine . .............g  A2 <5.0000 receptorH1 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine ..... .!.".#.$.%.&.'.(.g  4.Ki8.85398.69909.0969 receptorH3rat synaptosome cortex; brain K(+)-induced3antagonist; [3H]histamine release; depolarization Q9QYN8rat GPCRhistaminergic receptor histamine 7.:.;.<.=.>.?.@.A.B.C.D.E.F.G.H.I.J.  A27.50007.50007.5000 receptorH3 guinea pigsmooth muscle ileum electrically-inducedantagonist; contraction GPCRhistaminergic receptor histamine K.M.N.O.P.Q.R.S.T.U.V.W.X.Y.Z.[.g  D24.40004.40004.4000 receptorH2 guinea pigsmooth muscleatrium; heartagonist; electrically-induced. contractionGPCRhistaminergic receptor histaminet\.^._.`.a.b.c.d.e.f.g.h.i.j.k.l.g 8.L.].n.D (0A0B0C0D0E0F0G0H0I0J0K0L0M0N0O0P0Q0  IC507.91007.91007.9100 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor 5-hydroxytryptamine [3H]mesulergine R0T0U0V0W0X0Y0Z0[0\0]0^0_0`0a0b0c0d0  ?0S0f0D"" ' [ffr@<0333333@rh|@0SMDL-000637780Bioorg. Med. Chem. Lett. 12(24)-2002 3573-35771a$CN(C)CC1CC2N(O1)c3ccccc3Cc4ccccc24oes TPF"T %BȂF'R }*`W\mտX=`]ٌ<޿ հ޵YY1 @eFb TO1ɀmEh2!-x8G}&D˖ gp,.2030405090706080dm:0=0D0IC508.17008.17008.1700 receptorH1humancloned CHO cell antagonistP35367humanGPCRhistaminergic receptor histamine[3H]pyrilaminee0g0h0i0j0k0l0m0n0o0p0q0r0s0t0u0v0w0 0IC508.46008.46008.4600 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor5-hydroxytryptamine[125I]R-91150000000000000000000 IC508.98008.98008.9800 receptor5-HT2Chumancloned CHO cell antagonistP28335human.GPCRserotonergic receptorT5-hydroxytryptamine[3H]mesulergine000000000000000000 o 002D## 't3t@0@x&0SMDL-000637790Bioorg. Med. Chem. Lett. 12(24)-2002 3573-35771b(CN(C)CC1CC2N(O1)c3cc(Cl)ccc3Cc4ccccc24uuu TPU@'pP/$Z:HZ<! (ƪꪥf.nꅎˊM Yn!J+3/}B]K/l?.!s -x8G}'D˖ e.s.,x0z0{0|0}000~00?? dm00D eDI y p@4333333?HzG? 4n?6. x j ^ T J @ 4 *    p X @ &   x j  ( @  zpj^TJ@82 ~rh^TH>4*"lT:2(~",*P$zth^TJD>,f^N,$rZP>0* IC508.63008.63008.6300 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor histamine [3H]pyrilamine02222222 2 2 2 2 222222rel 2 2 2"2IC506.41006.41006.4100 receptor5-HT2Ahuman cloned L929 cell antagonistP28223human GPCRserotonergic receptor 5-hydroxytryptamine [125I]R-91150 $2'2(2)2*2+2,2-2.2/20212223242526272  IC507.90007.90007.9000 receptor5-HT2Chuman cloned CHO cell antagonistP28335human GPCRserotonergic receptor 5-hydroxytryptamine [3H]mesulergine 82:2;2<2=2>2?2@2A2B2C2D2E2F2G2H2I2J2  %292L2D$$ %|3vr@2 @n@&2SMDL-00063780 0Bioorg. Med. Chem. Lett. 12(24)-2002 3573-35772 ,CN(C)C[C@H]1C[C@H]2N(O1)c3cnccc3Cc4ccccc24{uu$TPH UT#Y:h +8V<@50eEШܩܹhj7 r:Ш7 "p:8ZDj[gt !۷-x8G}&D ۷ ,222222222?? dm!2#2 IC50 <6.0000 receptorH1human cloned CHO cell antagonistP35367human GPCRhistaminergic receptor histamine [3H]pyrilamineK2M2N2O2P2Q2R2S2T2U2V2W2X2Y2Z2[2  rel0f2i2rg2k2IC50 <6.0000 receptor5-HT2Ahumancloned L929 cell antagonistP28223humanGPCRserotonergic receptor 5-hydroxytryptamine[125I]R-91150m2p2q2r2s2t2u2v2w2x2y2z2{2|2}2~2 0IC506.04006.04006.0400 receptor5-HT2Chuman7cloned CHO cell antagonistP28335humannGPCRserotonergic receptor25-hydroxytryptamine2[3H]mesulergine222222222222222222 0 n222D%% %|3vr@h2 @vo2SMDL-0006378170Bioorg. Med. Chem. Lett. 12(24)-2002 3573-35773n,CN(C)C[C@H]1C[C@H]2N(O1)c3ccccc3Cc4ncccc24{uu$T(QU(,LHE *8RHA<@1 fE͉I(cY( _뿔 H3)ze+V ʹjj[ !-x8G}&D˖ |,\2^2_2`2a2e2c2b2d2??0dmj2l2 MeIC507.78007.78007.7800 receptorH1human3cloned CHO cell antagonistP35367humanGPCRhistaminergic receptor histamine[3H]pyrilamine222222222222222222 8SMDL-00065023t$J. Med. Chem. 34(4)-1991 1314-132815a%g$T(* #IZ!Ae aB WJFmJFWRQ2wWmy&ŏ|2 ŏe !]a'-.սEi ]a0,202224222?a[3H]ketanserinorz>  x Ft v j ` V P D : 0 &   p t l b X J > 4 *   P 8 X J   hpz $ f ~tfZPF@4( `vndZL@6," R:"zZL Xp`j&hvl^RH>8," + 44 44 4#CN(C)CC[C@H]1CN(C)C(=S)c2cccnc2O1 abs 44 IC504.67784.67784.6778 receptorH1 guinea pig membranecortex; brain antagonistGPCRhistaminergic receptor histamine [3H]mepyramine 4 4 44444444444444G  + $4'4 %4)4,4DI y p@&4333333?HzG?-4SMDL-00065024 $J. Med. Chem. 34(4)-1991 1314-132816$CN(C)CC[C@@H]1CN(C)C(=S)c2cccnc2O1a%g$T(* #IZ!Ae aB WJFmJFWRQ2wWmy&ŏ|2 ŏe !]a'-.սEi ]a ,04444#4!4 4"4abs (4*4 IC507.52297.52297.5229 receptorH1 guinea pig membranecortex; brain antagonistGPCRhistaminergic receptor histamine [3H]mepyramine+4.4/404142434445464748494:4;4<4G  + G4J4 H4L4O4DI L2r@I4@tVP4SMDL-00065025 $J. Med. Chem. 34(4)-1991 1314-132817'CN(C)CC[C@H]1CN(C)C(=S)c2cc(Cl)cnc2O1 g5i $T@Q DF_ …0:4@ 0$ 2zPzW2EnT*>y?bVJn@6ExP-~6]\(V~,#- ! '-.սMi  ,=4?4@4A4B4F4D4C4E4?? abs K4M4 IC504.92454.92454.9245 receptorH1 guinea pig membranecortex; brain antagonistGPCRhistaminergic receptor histamine [3H]mepyramineN4Q4R4S4T4U4V4W4X4Y4Z4[4\4]4^4_4G +4j4m4k4o4r4DI L2r@l4@tVs4SMDL-00065026$J. Med. Chem. 34(4)-1991 1314-132818(CN(C)CC[C@@H]1CN(C)C(=S)c2cc(Cl)cnc2O1g5i $T@Q DF_ …0:4@ 0$e 2zPzW2EnT*>y?bVJn@6ExP-~6]\(V~,#-! '-.սMi ,`4b4c4d4e4i4g4f4h4??absn4p4IC508.72128.72128.7212 receptorH1 guinea pig membranecortex; brain4 antagonistGPCRhistaminergic receptor histaminec[3H]mepyramineq4t4u4v4w4x4y4z4{4|4}4~44444G 4+@444444DI Ws`}s@4(\@MbX4SMDL-00065027$J. Med. Chem. 34(4)-1991 1314-132819&CN1C[C@H](CCN2CCC2)Oc3ncc(Cl)cc3C1=SmEm $T@Q DE,!E*UB%_QB D =_+"}_˼LE1 +]mM m?n|"|<(..+Ȇm2! ',.սMi - @,444444444??abs 44UIC506.06056.06056.0605 receptorH1 guinea pig membranecortex; brain antagonistGPCRhistaminergic receptor histamine [3H]mepyramine4444444444444444G mDI Ws`}s@ 6(\@MbX6SMDL-00065028,444666666??L??5-hydroxytryptaminezt. @n8 *   J x <  z T B D r &  ~ 8 f n x r*  lF42 `  ~vp*X`jd^8&$R zphbJR\f`:( |rjd LT^& + 6 6 6 66$J. Med. Chem. 34(4)-1991 1314-132820'CN1C[C@@H](CCN2CCC2)Oc3ncc(Cl)cc3C1=S mEm $T@Q DE,!E*UB%_QB D2=_+"}_˼LE1 +]mM m?n|"|<(..+Ȇm ! ',.սMi  abs  6 6 IC509.58509.58509.5850 receptorH1 guinea pig membranecortex; brain antagonistGPCRhistaminergic receptor histamine [3H]mepyramine6666666666666666G  *6.6DI !PTr3Ss@+6ףp= @K7 /6SMDL-00065029 $J. Med. Chem. 34(4)-1991 1314-132828$CN(C)CCC(c1ccc(Cl)cc1)c2ccc(Cl)cn2_Ek #,D1D؂ŊQcx 0.P6G  J6N6DI 0rZ|6^ze!f=2>WXzf,6666666666nc666y@ x r  l @ R| .2 $ Z ~ l ` R L @ 6 , "   p d   PfV` 8 v xpbPD60$pHjv|j^PJ>4* b >|nh\RH>60  *R|L& methysergideIC507.43187.43187.4318 receptoralpha1rat membranecortex; brain antagonistGPCRadrenergic receptor epinephrine / norepinephrine[3H]prazosinphentolamine88888 8 8 8 8 88888888G  IC507.63837.63837.6383 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone sulpiride 8888888888 8!8"8#8$8%8&8G  Ki9.16129.16129.1612 receptor5-HT2 rat membranebrain antagonistGPCRserotonergic receptor [3H]ketanserinmethysergide'8)8*8+8,8-8.8/80818283848586878G  Ki <6.0000 receptor5-HT1Arat membranehippocampus; brain antagonistGPCRserotonergic receptor [3H]-8-OH-DPAT5-HT88:8;8<8=8>8?8@8A8B8C8D8E8F8G  Ki7.53767.53767.5376 receptoralpha1rat membranecortex; brain antagonistGPCRadrenergic receptor [3H]prazosinphentolamineG8I8J8K8L8M8N8O8P8Q8R8S8T8U8V8W8G  Ki7.65767.65767.6576 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor[3H]spiperone sulpirideX8Z8[8\8]8^8_8`8a8b8c8d8e8f8g8h8G  688(898H8Y8j8Ki8.22188.22188.2218 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]mepyraminepromethazinei8k8l8m8n8o8p8q8r8s8t8u8v8w8x8y8G 8IC509.30109.30109.3010 receptor5-HT2rat membranebrain antagonistGPCRserotonergic receptor5-hydroxytryptamine[3H]ketanserinmethysergide88888888888888888G IC506.98726.98726.9872 receptoralpha1rat membranecortex; brain antagonistGPCRadrenergic receptor8epinephrine / norepinephrine[3H]prazosinphentolamine88888888888888888G rG c 88::":3:D:S:D /(I)vz@8@)\8SMDL-00066526$J. Med. Chem. 34(8)-1991 2477-248324 RP-622034Fc1ccc(cc1)N2CCN(CCCN3c4cccc5cccc(c45)S3(=O)=O)CC2P2H YT BI%@^CSXQ5D puX(uUCP q$@P?).:?Ók|jVU-j)*U9Yj|:TjwZu^Ւݞ۲wP#!i1owݣD) ip,z8|8}8~8888888?inc88?i PANES.EPL~v x j X L D : . $     n T B *   ~ d h nx0 ,f $  4btnbXND>8 jX>6(x~xr&th`VJ>82jrXPB8,$*8&FxfZRH<2(| IC50 <6.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor dopamine[3H]spiperone sulpiride 8::::::: : : : : :::Ki9.58509.58509.5850 receptor5-HT2 rat membranebrain antagonistGPCRserotonergic receptor [3H]ketanserinmethysergide::::::::::::::: :G  Ki7.15497.15497.1549 receptor5-HT1Arat membranehippocampus; brain antagonistGPCRserotonergic receptor [3H]-8-OH-DPAT5-HT!:#:$:%:&:':(:):*:+:,:-:.:/:0:1:G  Ki7.42027.42027.4202 receptoralpha1rat membranecortex; brain antagonistGPCRadrenergic receptor [3H]prazosinphentolamine2:4:5:6:7:8:9:::;:<:=:>:?:@:A:B:G  Ki <6.0000 receptorD2rat membranestriatum; brain antagonistGPCRdopaminergic receptor [3H]spiperone sulpiride C:E:F:G:H:I:J:K:L:M:N:O:P:Q:G   Ki7.60217.60217.6021 receptorH1 guinea pig membranecerebellum; brain antagonistGPCRhistaminergic receptor[3H]mepyraminepromethazineR:T:U:V:W:X:Y:Z:[:\:]:^:_:`:a:b:G PLEX200z*WBPaneChangewbChangeFormButton$$$SHARED$$$VAR$$$INFO$$$L "+"+LQ"O;;QfLLQe&QV?/ LL* QD* QCJO"L%"Q+ "+KKStatic Str ErrorUnable to change forms.:6:7:8:9:::;:<:=:>:?:@:A:B:2@G   C:     E@F@KiG@<6.0000 H@receptorI@D2J@rat K@membraneL@striatum; brain M@antagonistN@GPCRO@dopaminergic receptor P@[3H]spiperone Q@sulpiride D@C:E:F:G:H:I:J:K:L:M:N:O:P:Q:C@G  R@ R:   T@U@KiV@7.6021W@7.6021X@7.6021Y@receptorZ@H1[@guinea pig\@membrane]@cerebellum; brain ^@antagonist_@GPCR`@histaminergic receptora@[3H]mepyramineb@promethazine .>vjb\PD>8pzbZL:.&0@. H|pf\RLFjbT@4,& cc LW SMDL.IDTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x m   { ; #`$ |<' Hw/w"ArialrNewxCourierNewPArialNew Romanxact#( },Root>act.list>id-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #$ |<' Hw/w "ArialrNewxCourierNewPArialrw Romanxtarg_type( },Root>act.list>target.type-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #e$ |<' Hw/w "ArialrNewxCourierNewPArialrw Romanxtarget_name( },Root>act.list>target.name-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #$ |<' Hw/w "ArialrNewxCourierNewPArialrw Romanxact_type( },Root>act.list>type-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #$ |<' Hw/w"ArialrNewxCourierNewPArialrw Romanxact_val( },Root>act.list>value-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #$ |<' Hw/w"ArialrNewxCourierNewPArialrw Romanxact_min( },Root>act.list>min-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #$ |<' Hw/w"ArialrNewxCourierNewPArialrw Romanxact_max( },Root>act.list>max-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX #_$ |<' Hw/w"ArialxCourierPArialrw Romanxinhib%( },Root>act.list>inhib-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX!"QR SU9 keyw struct EmbedEPL0Part 0 of pl startup program eplfilenamekeyw_17847Last SAR Table v<@!1 c:c!1 8b!1 L!1 V!1%# struct EmbedEPL0Part 0 of pl startup program eplfilenamekeyw_17847Last SAR Table8v<@!1 c:c!1 8b!1 L!1 V!1%#yw_17847Last SAR Table hZ nxew Romand z@ACDEv ArialxFGHIJKLMNOB :x B    | Hw/wArialrxCourierPformulayRoot>*fmla_mol.strTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x B     Hw/w ArialrxCourierPmol_weightyRoot>*mol.weight_mol.strTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x      Hw/w ArialrxCourierPreferencey Root>mol.refTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x     { ; #$ |<' Hw/w!ArialrNewxCourierNewPstructure_keywords(},Root>mol.kw>kw-Times New Romand./ 01~35VWYZ[w Arialx\]^_`abcdeX!"QR SU :x ;]z    | Hw/wArialrxCourierPmolnamey Root>mol.nameTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x w    y Root>mol.smiTimes New Romannz@ACDEv ArialxFGHIJKLMNOB :x B     Hw/w ArialrxCourierPest_LogKowyRoot>est.logkowTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x  B'     Hw/w ArialrxCourierPest_LogWSolyRoot>est.logwsolTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x B     Hw/w Arialrw RomanxCourierw RomanPexp_LogKowyRoot>exp.logkowTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x B '     Hw/w ArialNew RomanxCourierw RomanPexp_LogWSolyRoot>exp.logwsolTimes New Romand z@ACDEv ArialxFGHIJKLMNOB :x ];z    | Hw/wArialrxCourierPSMDL_IDy Root>/< 7????>>u ??=gA4Lhikl Hw/wArialrxArialrd&[Database Name]moqrgc Hw/w ArialrdPage &[Page]s :x bC0     ~ Hw/w "ArialrNewxArialrNewnKeywords ykeywwbChangeFormButton Arialx z@ACDEv ArialxFGHIJKLMNOB :x K    ~ Hw/w "ArialrNewxArialrNewn< Main > y enter_1 Arialx z@ACDEv ArialxFGHIJKLMNOB :x Cy   y Ariald z@ACDEv ArialxFGHIJKLMNOB :x C    :x y    :x    y Arialx z@ACDEv ArialxFGHIJKLMNOB :x W   y Root>SMDL.IDx Arialx z@ACDEv ArialxFGHIJKLMNOB :x W   y Root>SMDL.SID Arialx z@ACDEv ArialxFGHIJKLMNOB :x ~2X     Hw/w"Arialrw RomanxArialrw RomandArialrw RomandArialrw Romandwww.sunsetmolecular.com y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  }    73 Hw/w "Arialrw RomanxArialrw RomanxArialrw RomanArialrw RomanArialrw RomanArialrw RomanArialrw RomanW O M B A T y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 9W     Hw/w "Arialrw RomanxArialrw RomannSunset Molecular Discovery, LLC y Arialx z@ACDEv ArialxFGHIJKLMNOB :x ] w     Hw/w ArialrNewxCourierNewPCourierNewPstructurey 1602Struct Root>mol.str Arialx z@ACDEv ArialxFGHIJKLMNOB :x z     Hw/w ArialrxCourierPgeneric_nameyRoot>mol.gnameTimes N-> l NOB :x Sv m   Dy!Root>act.list>bind.radioligandTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x Sml   Ey!Root>act.list>bind.nonspecificTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x 5G   F ~zP Hw/w$ArialNew RomanxArialNew RomanPfamily@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  5>   G zvP Hw/w$ArialNew RomanxArialNew RomanPname@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  55   H zvP Hw/w$ArialNew RomanxArialNew RomanPtype@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x S   IyRoot>act.list>otherTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x O H    JyRoot>act.list>id Arialx z@ACDEv ArialxFGHIJKLMNOB :x ~H*    K P Hw/w $ArialNew RomanxArialNew RomanPactivity #@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x H   LyRoot>act.list>value Arialx z@ACDEv ArialxFGHIJKLMNOB :x ~*    M P Hw/w $ArialxArialPand value@y Arialx z@ACDEv ArialxFGHIJKLMNOB9 n x z@ACDEv ArialxFGHIJKLMNOB :x  1 f   6 P Hw/w $ArialNew RomanxArialNew RomanPsubstrate@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  1 e   7 ~P Hw/w $ArialNew RomanxArialNew RomanPreactant@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  1 \   8 ~P Hw/w $ArialNew RomanxArialNew RomanPcofactor@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  1 [   9 ~P Hw/w $ArialNew RomanxArialNew RomanPradiosub@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  1 S   : ~zP Hw/w$ArialNew RomanxArialNew RomanPactdet@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x ^    ;yRoot>act.list>swissp.idTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x ^    <yRoot>act.list>swissp.speciesTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x SFD   =yRoot>act.list>rec.familyTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x SD<   >yRoot>act.list>rec.nameTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x S<:   ?yRoot>act.list>rec.typeTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x SWV   @yRoot>act.list>pro.familyTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x SV M   AyRoot>act.list>pro.nameTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x SM K   ByRoot>act.list>pro.typeTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x Sw v   Cy# Root>act.list>bind.endogenligandTimes New Romandz@ACDEv ArialxFGHIJKLMDB w/w $ArialrxArialrPstimulus@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x w"|   ( ~zP Hw/w$ArialrxArialrPeffect@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x W    )yRoot>act.list>enz.familyTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    *yRoot>act.list>enz.nameTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    +yRoot>act.list>enz.typeTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    ,yRoot>act.list>enz.ecTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    -yRoot>act.list>enz.substrateTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    .yRoot>act.list>enz.reactantTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    /yRoot>act.list>enz.cofactorTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W    0y# Root>act.list>enz.radiosubstrateTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x W x   1yRoot>act.list>enz.actdetTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x 1    2 ~zP Hw/w$ArialNew RomanxArialNew RomanPfamily@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 1 x   3 zvP Hw/w$ArialNew RomanxArialNew RomanPname@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 1 o   4 zvP Hw/w$ArialNew RomanxArialNew RomanPtype@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 1 n   5 vrP Hw/w$ArialNew RomanxArialNew RomanPEC@y Arialx+D fic@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x S8y    |xP Hw/wArialNew RomanxArialNew RomandOthery Arialx z@ACDEv ArialxFGHIJKLMNOB :x H    yRoot>act.list>bio.speciesTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x H    yRoot>act.list>bio.tissuetypeTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x H    y!Root>act.list>bio.tissuesourceTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x H    yRoot>act.list>bio.cellTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x H   y!Root>act.list>bio.intracellstrTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x H    yRoot>act.list>bio.stimulusTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x H   !yRoot>act.list>bio.effectTimes New Romandz@ACDEv ArialxFGHIJKLMNOB :x w "   " |P Hw/w$ArialrxArialrPspecies@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 3 "   # P Hw/w $ArialNew RomanxArialNew RomanPtissue_type@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x "   $ P Hw/w $ArialNew RomanxArialNew RomanPtissue_source@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x w "   % zvP Hw/w$ArialrxArialrPcell@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x "   & P Hw/w$ArialNew RomanxArialNew RomanPintracell_struct@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x w"   ' ~P H:F y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 9 6 s    ~zP Hw/wArialrxArialrdEnzymey Arialx z@ACDEv ArialxFGHIJKLMNOB :x @     vrP Hw/w$ArialNew RomanxArialNew RomanPID@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x @ |    |P Hw/w$ArialNew RomanxArialNew RomanPspecies@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x <]"    ~P Hw/w ArialrxArialrdReceptory Arialx z@ACDEv ArialxFGHIJKLMNOB :x S~@1    |P Hw/wArialrxArialrdProteiny Arialx z@ACDEv ArialxFGHIJKLMNOB :x 55    ~zP Hw/w$ArialNew RomanxArialNew RomanPfamily@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x q5-    zvP Hw/w$ArialNew RomanxArialNew RomanPname@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x p5$    zvP Hw/w$ArialNew RomanxArialNew RomanPtype@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x S Ga    |P Hw/wArialrxArialrdBindingy Arialx z@ACDEv ArialxFGHIJKLMNOB :x  1c    P Hw/w $ArialNew RomanxArialNew RomanPendogen_lig@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x C 1b    P Hw/w $ArialNew RomanxArialNew RomanPradio_lig@y Arialx z@ACDEv ArialxFGHIJKLMNOB :x C1R    P Hw/w $ArialNew RomanxArialNew RomanPnonspeciJH N7????>>u ??=gA4LhiklP Hw/wArialNew RomanxArialNew Romand&[Database Name]moqrgcP Hw/w ArialNew RomandPage &[Page]s :x <    zvP Hw/w"Arialrw RomanxArialrw RomannMain y structwbChangeFormButton Arialx z@ACDEv ArialxFGHIJKLMNOB :x b<0     P Hw/w "Arialrw RomanxArialrw Romann< Keywords > y enter_1 Arialx z@ACDEv ArialxFGHIJKLMNOB :x Cy   y Ariald z@ACDEv ArialxFGHIJKLMNOB :x Cb    :x 0 y    :x    y Arialx z@ACDEv ArialxFGHIJKLMNOB :x W   y Root>SMDL.IDx Arialx z@ACDEv ArialxFGHIJKLMNOB :x W   y Root>SMDL.SID Arialx z@ACDEv ArialxFGHIJKLMNOB :x ~2X    P Hw/w"ArialNew RomannArialNew Romandwww.sunsetmolecular.com y Arialx z@ACDEv ArialxFGHIJKLMNOB :x  }    P Hw/w "ArialNew RomandArialNew RomanW O M B A T y Arialx z@ACDEv ArialxFGHIJKLMNOB :x 9W    P Hw/w "ArialNew RomanArialNew RomannSunset Molecular Discovery, LLC y Arialx z@ACDEv ArialxFGHIJKLMNOB :x ^2    P Hw/w ArialNew RomannCourierw RomanPstructurey 1602Struct Root>mol.str Arialx z@ACDEv ArialxFGHIJKLMNOB :x 1     |P Hw/wArialrxArialrdBiologyy Arialx z@ACDEv ArialxFGHIJKLMNOB :x @ L     P Hw/w ArialrxArialrdSwissProtZJ Wcol_stdbond: 0 $col_no: 52 $col_name: "bind.nonspecific" $col_field: 53 $col_label: "bind nonspecific" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 53 $col_name: "other" $col_field: 54 $col_label: "other" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 Z ol_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 39 $col_name: "enz.substrate" $col_field: 40 $col_label: "enz substrate" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 40 $col_name: "enz.reactant" $col_field: 41 $col_label: "enz reactant" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 41 $col_name: "enz.cofactor" $col_field: 42 $col_label: "enz cofactor" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 42 $col_name: "enz.radiosubstrate" $col_field: 43 $col_label: "enz radiosubstrate" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 43 $col_name: "enz.actdet" $col_field: 44 $col_label: "enz actdet" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 44 $col_name: "rec.family" $col_field: 45 $col_label: "rec family" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 45 $col_name: "rec.name" $col_field: 46 $col_label: "rec name" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 46 $col_name: "rec.type" $col_field: 47 $col_label: "rec type" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 47 $col_name: "pro.family" $col_field: 48 $col_label: "pro family" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 48 $col_name: "pro.name" $col_field: 49 $col_label: "pro name" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 49 $col_name: "pro.type" $col_field: 50 $col_label: "pro type" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 50 $col_name: "bind.endogenligand" $col_field: 51 $col_label: "bind endogenligand" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 51 $col_name: "bind.radioligand" $col_field: 52 $col_label: "bind radioligand" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $/N _field: 26 $col_label: "target name" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 26 $col_name: "bio.species" $col_field: 27 $col_label: "bio species" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 27 $col_name: "bio.tissuetype" $col_field: 28 $col_label: "bio tissuetype" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 28 $col_name: "bio.tissuesource" $col_field: 29 $col_label: "bio tissuesource" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 29 $col_name: "bio.cell" $col_field: 30 $col_label: "bio cell" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 30 $col_name: "bio.intracellstr" $col_field: 31 $col_label: "bio intracellstr" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 31 $col_name: "bio.stimulus" $col_field: 32 $col_label: "bio stimulus" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 32 $col_name: "bio.effect" $col_field: 33 $col_label: "bio effect" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 33 $col_name: "swissp.id" $col_field: 34 $col_label: "swissp id" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 34 $col_name: "swissp.species" $col_field: 35 $col_label: "swissp species" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 35 $col_name: "enz.family" $col_field: 36 $col_label: "enz family" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 36 $col_name: "enz.name" $col_field: 37 $col_label: "enz name" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 37 $col_name: "enz.type" $col_field: 38 $col_label: "enz type" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 38 $col_name: "enz.ec" $col_field: 39 $col_label: "enz ec" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $c&P 8 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 12 $col_name: "mol.smi" $col_field: 11 $col_label: "mol smi" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 13 $col_name: "kw" $col_field: 13 $col_label: "kw" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 14 $col_name: "est.logkow" $col_field: 14 $col_label: "est logkow" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 15 $col_name: "est.logwsol" $col_field: 15 $col_label: "est logwsol" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 16 $col_name: "exp.logkow" $col_field: 16 $col_label: "exp logkow" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 17 $col_name: "exp.logwsol" $col_field: 17 $col_label: "exp logwsol" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 18 $col_name: "act.list>id" $col_field: 19 $col_label: "act list>id" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 19 $col_name: "type" $col_field: 20 $col_label: "type" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 20 $col_name: "value" $col_field: 21 $col_label: "value" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 21 $col_name: "min" $col_field: 22 $col_label: "min" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 22 $col_name: "max" $col_field: 23 $col_label: "max" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 23 $col_name: "inhib" $col_field: 24 $col_label: "inhib" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 24 $col_name: "target.type" $col_field: 25 $col_label: "target type" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 25 $col_name: "target.name" $col5R $SARTableDef: "" $source: "WINDOWS" $version: 3 $orient: 0 $labels: 1 $labels_fontsize: 100 $labels_fontstyle: 0 $labels_font: "Arial" $startrow: 0 $startcol: 0 $writequery: 1 $rowformat: 1 $rowheight: 500 $colwidth: 25 $displayhierarchy: 0 $displaycollabels: 0 $rg_link: "Root>mol.str" $rg_prompt: 1 $rg_train: 1 $rg_footnotes: 1 $rg_abbrev: 0 $rg_includemappings: 0 $rg_substdb: "" $substfootnote_fontsize: 80 $substfootnote_fontstyle: 0 $substfootnote_font: "Arial" $substfootnote_stdbond: 180 $substfootnote_format: 2 $rgroupcore_fontsize: 80 $rgroupcore_fontstyle: 0 $rgroupcore_font: "Arial" $rgroupcore_stdbond: 180 $rgroupcore_format: 2 $totcols: 54 $col_no: 0 $col_name: "Root>ID" $col_field: 1 $col_label: "Root>ID" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 1 $col_name: "SMDL.ID" $col_field: 2 $col_label: "SMDL ID" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 2 $col_name: "SMDL.IDx" $col_field: 3 $col_label: "SMDL IDx" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 3 $col_name: "SMDL.SID" $col_field: 4 $col_label: "SMDL SID" $col_width: 8 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 4 $col_name: "mol.ref" $col_field: 5 $col_label: "mol ref" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 5 $col_name: "mol.name" $col_field: 6 $col_label: "mol name" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 6 $col_name: "mol.gname" $col_field: 7 $col_label: "mol gname" $col_width: 20 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 7 $col_name: "mol.str" $col_field: 8 $col_label: "mol str" $col_width: 25 $col_height: 720 $col_format: 0 $col_hlabels: 2 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 180 $col_no: 8 $col_name: "mol.str_chiral" $col_field: 3001 $col_label: "mol str chiral" $col_width: 6 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 0 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 9 $col_name: "mol.str_composition" $col_field: 3000 $col_label: "mol str composition" $col_width: 15 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 10 $col_name: "*fmla_mol.str" $col_field: 9 $col_label: "fmla mol str" $col_width: 15 $col_height: 128 $col_format: 0 $col_hlabels: 0 $col_halign: 0 $col_valign: 0 $col_wrap: 1 $col_nochiral: 0 $col_repeat: 1 $col_range: 0 $col_fontsize: 100 $col_fontstyle: 0 $col_font: "Arial" $col_stdbond: 0 $col_no: 11 $col_name: "*mol.weight_mol.str" $col_field: 10 $col_label: "mol weight mol str" $col_width: 8 $col_height: 12ET