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TABLE 1 Pharmacological Selectivity of ABT-102 ~IC50(μM) Target ~IC50(μM) Target Ligand Adenosine A1 [3H]DPCPX > 10 Benzodiazepine Central [3H]Flunitrazepam > 10 Adenosine A2A [3H]CGS 21680 > 10 Benzodiazepine Peripheral [3H]PK 11195 > 10 Adenosine A3 [125I]AB-MECA > 10 Ca2+ channel verapamil site [3H]D 888 > 10 Adrenergic 1 [3H]Prazosin > 10 K+ channel (volt. dependent) [125I]Dendrotoxin > 10 Adrenergic 2 [3H]RX821002 > 10 K+ channel (Ca2+ dependent) [125I]Apamin > 10 Adrenergic 1 [3H](-)CGP 12177 > 10 Na+ channel (Site 2) [3H]Batrachotoxin > 10 Adrenergic 2 [3H](-)CGP 12177 > 10 Neurokinin NK1 [125I][Sar9,Met(O2)11]-SP > 10 Angiotensin AT1 [125I][Sar1,Ile8]-ATII > 10 Neurokinin NK2 [125I]NKA > 10 Angiotensin AT2 [ Bombesin 125 I]CGP 42112A 125 7 Neurokinin NK3 [ [125I][Tyr4]bombesin > 10 Neuropeptide Y1 [125I]peptide YY > 10 Bradykinin B2 [3H]NPC 17731 > 10 Neuropeptide Y2 [125I]peptide YY > 10 Cl- channel [35S]TBPS > 10 Neurotensin NT1 [125I]Neurotensin > 10 CCKA [3H]Devazepide > 10 PACAP PAC1 [3H]PACAP1-27 > 10 CCKB [3H]CCK-8 > 10 Melanocortin MC4 [125I]NDP--MSH > 10 CCR1 [125I]MIP-1 > 10 Galanin GAL1 [125I]Galanin > 10 CGRP [125I]-CGRP > 10 Galanin GAL2 [125I]Galanin > 10 Cannabinoid CB1 [3H]Win 55212-2 > 10 Melatonin ML1 [125I]Iodomelatonin > 10 DA uptake [3H]GBR 12935 > 10 IL-8B (CXCR2) [125I]IL-8 > 10 Dopamine D1 [3H]SCH 23390 > 10 TNF [125I] TNF > 10 Dopamine D3 [3H]Spiperone > 10 PDGF [125I]PDGF BB > 10 Dopamine D4.4 [3H]Spiperone > 10 PGI2/IP [3H] iloprost > 10 3 > 10 Ligand I][MePhe ]- D5 3 > 10 Dopamine D5 [ H]SCH 23390 > 10 TXA2/PGH2/TP [ H]SQ 29548 > 10 Endothelin ETA [125I]Endothelin-1 > 10 Serotonin 5-HT1A [3H]8-OH-DPAT > 10 Endothelin ETB [125I]Endothelin-1 > 10 Serotonin 5-HT1B [3H]CYP > 10 GABA [3H]GABA > 10 Serotonin 5-HT2A [3H]Ketanserin > 10 Histamine H1 [3H]Pyrilamine > 10 Serotonin 5-HT2C [3H]Mesulergine > 10 Histamine H2 [ Muscarinic M1 125 I]APT 3 > 10 Serotonin 5-HT3 [ H]BRL 43694 > 10 [3H]Pirenzepine > 10 Serotonin 5-HT5A [3H]LSD > 10 Muscarinic M2 [3H]AF-DX384 > 10 Serotonin 5-HT6 [3H]LSD > 10 Muscarinic M3 [3H]4-DAMP > 10 Serotonin 5-HT7 [3H]LSD > 10 Muscarinic M4 [3H]4-DAMP > 10 Sigma [3H]DTG > 10 Muscarinic M5 [3H]4-DAMP > 10 SKCa [125I]apamin > 10 Opioid [3H]DADLE > 10 Somatostatin [125I]Tyr11-somatostatin > 10 Opioid [3H]U 69593 > 10 VIP1 (VPAC1) [125I]VIP > 10 Opioid [3H]DAMGO > 10 Vasopressin V1a [3H]AVP > 10 ORL1 [3H]Nociceptin > 10 ORL1 [3H]Nociceptin > 10 P2X [3H],MeATP > 10 PCP [3H]-TCP > 10 P2Y [35S]dATPS > 10 PACAP, pituitary adenylyl cyclase-activating protein; DPCPX, 8-cyclopentyl-1,3-dipropylxanthine; CGS 21680, 2-p-(2-carboxyethyl) phenethylamino-5-N-ethylcarboxamidoadenosine; AB-MECA, 4-aminobenzyl-5-N-methylcarboxamidoadenosine; RX 821002, 2-(2-methoxy-1,4-benzodioxan2yl)-2-imidazoline; CGP-12177, 4-[3-(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro2H-benzimidazol-2-one; SCH23390, R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5tetrahydro-1H-3-benzazepine; 4-DAMP, 4-diphenylacetoxy-N-methylpiperidine; DADLE, [DAla2,D-Leu5]-enkephalin; U-69593, (+)-(5,7, 8)-N-methyl-N-[7-(1-pyrrolidinyl)-1oxaspiro[4.5]dec-8-yl]benzeneacetamide; DAMGO, [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin; MeATP, methylene-ATP; 8-OH-DPAT, 8-hydroxy-2-dipropylaminotetralin; CYP, cyanopindolol; LSD, d-lysergic acid diethylamide; CCK, cholecystokinin; PDGF, platelet-derived growth factor; NE, norepinephrine; DA, dopamine; VIP, vasoactive intestinal peptide; AVP, arginine vasopressin; GBR12935, (1-[2-(diphenylmethoxy)ethyl-4-(3-phenylpropyl)-piperazine); PK11195,1-(2-chloro-phenyl)-N-methyl-N-(1-methylpropyl)-1-isoquinoline carboxamide; TBPS, tbutylbicyclophosphorothionate; CCR, chemokine receptor; ORL, opioid receptor-like; MIP, macrophage inflammatory protein; APT, aminopotentidine; VPAC, (vasoactive intestinal peptide) pituitary adenylate cyclase-activating peptide receptor; DTG, 1,3-di-o-tolyguanidine; WIN 552122, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo-[1,2,3-d,e]-1,4-benzoxazin-6-yl]1-naphthalenyl-methanone; AF DX384, 5,11-dihydro-11-[2-(-[8-dipropylamino)methyl]-1piperidinyl]-ethyl]amino]-carbonyl-6H-pyrido[2,3-b] [1,4]benzodiazepin-6-one;BRL 43694, granisetron; MDL 105,519, (E)-3-(2-phenyl-2-carboxylethenyl)-4,6-dichloro-1[3H]-indole-2- carboxylic acid; NPC 17731, D-Arg[Hyp3,D-HypE (transprolyl) 7,Oicc8]bradykinin; Ro41-1049, N(2-aminoethyl)-5-(m-fluorophenyl)-4-thiazole carboxamide HCl; CGP 39653, D,L-(E)-2-amino-4propyl-5-phosphono-3-pentenoic acid; CGP 42112A, N--nicotinoyl-Tyr-(N--CBZ-Arg)-Lys-HisPro-Ile-OH; D 888, verapamil derivative; NDP--MSH, Nle4-D-Phe7--melanocyte stimulating hormone; SP, substance P; SQ 29548, [1S-[1,2 (5Z),3,4]-7-[3-[[2-[(phenylamino) carbonyl]hydrazino]methyl]-7-oxabicyclo[2.2.1] hept-2-yl]-5-heptenoic acid.