Table 2

In vitro receptor binding selectivity of ABT-594

ReceptorLigandKi
nM
Muopioid[3H]DAMGOa >1000
Delta opioid[3H]pCl-Phe-DPDPE>1000
Kappa opioid[3H]U 69593>1000
P2X[3H]α,β-MeATP>1000
P2Y[3H]ADPβS>1000
Muscarinic-M1[3H]Pirenzepine>1000
Muscarinic-M2[3H]AF-DX 384>1000
Muscarinic-M3[3H]4-DAMP>1000
Muscarinic-M4[3H]4-DAMP>1000
Muscarinic-M5[3H]4-DAMP>1000
Alpha-1a[3H]Prazosin>1000
Alpha-1b[3H]Prazosin890
Alpha-1d[3H]Prazosin>1000
Alpha-2a[3H]Rauwolscine>1000
Alpha-2b[3H]Rauwolscine597
Alpha-2c[3H]Rauwolscine342
Serotonin 5-HT-1A[3H]8-OH-DPAT>1000
Serotonin 5-HT-1B[125I]CYP>1000
Serotonin 5-HT-2A[3H]ketanserin>1000
Serotonin 5-HT-2C[3H]mesulergine>1000
Serotonin 5-HT-3[3H]BRL 43694>1000
Serotonin 5-HT-6[3H]LSD>1000
Serotonin 5-HT-7[3H]LSD>1000
Adenosine A1[3H]CCPA>1000
Adenosine A2[3H]CGS 21680>1000
Adenosine A3[3H]AB-MECA>1000
Beta-1[3H](−)-CGP 12177>1000
Beta-2[3H](−)-CGP 12177>1000
Beta-3[125I]CYP>1000
Dopamine D1[3H]SCH 23390>1000
Dopamine D2[3H]Spiperone>1000
Dopamine D3[3H]Spiperone>1000
Dopamine D4.4[3H]Spiperone>1000
Dopamine D5[3H]SCH 23390>1000
GABAA [3H]Muscimol>1000
GABAB [3H]GABA (+50 mM isoguvacine to block GABAA)>1000
Histamine-H3[3H](R)-α-Me-histamine>1000
Sigma[3H]Di(2-tolyl)guanidine (DTG)>1000
AT1[3H]A II>1000
ANP[125I]ANP>1000
V1[3H]V1 antagonist>1000
B2[3H]NPC 17731>1000
CCK A[3H]Devazepide>1000
Endothelin A[125I]Endothelin-1>1000
Glucagon[125I]Glucagon>1000
Somatostatin[125I]Tyr11-Somatostatin>1000
Y1[125I]Peptide YY>1000
Y2[125I]Peptide YY>1000
Neurokinin 1[3H][Sar9,Met(O2)11]-SP>1000
Neurokinin 2[125I]NKA>1000
Neurokinin 3[3H]Senktide>1000
Neurotensin[125I]Neurotensin>1000
Calcium channel (Type L)[3H]D 888>1000
Chloride ionophore[3H]TBPS>1000
Potassium (voltage-dependent)[125I]Charybdotoxin>1000
Phencyclidine[3H]TCP>1000
Sodium channel 1[3H]Saxitoxin>1000
Sodium channel 2[3H]Batrachotoxinin>1000
Benzodiazepine (peripheral)[3H]PK11195>1000
Benzodiazepine (central)[3H]Flunitrazepam>1000
Glycine, Strychnine[3H]Strychnine>1000
AMPA[3H]AMPA>1000
Kainate[3H]Kainic acid>1000
MK-801[3H]MK-801>1000
N-Methyl-d-aspartate[3H]CGP 39653>1000
Norepinephrine uptake[3H]Desmethylimipramine>1000
Serotonin uptake[3H]Paroxetine>1000
GABA uptake[3H]GABA>1000
Choline uptake[3H]Choline chloride>1000
Dopamine uptake[3H]BTCP>1000
ADO uptake[3H]NBTI>1000
PDE I–IV[3H]cAMP>1000
PDE V[3H]cGMP>1000
Monoamine oxidase AKynuramine>1000
Monoamine oxidase BBenzylamine>1000
COX-1Indomethacin>1000
COX-2Nimesulfide>1000

These in vitro assays were conducted by Cerep to assess the potential interaction of ABT-594 with other receptor, enzyme and uptake systems.