Receptor binding profiles of TASP0434299 to G protein–coupled receptors, transporters, and ion channels
Values are expressed as the mean of the percent inhibition of control-specific binding at 1 μM of TASP0434299 performed in duplicate.
| Target | Species | Source | Radioligand | Inhibition at 1 μM |
|---|---|---|---|---|
| % | ||||
| α1A | Rat | Salivary glands | [3H]prazosin | −9.4 |
| α1B | Human | Recombinant (CHO cells) | [3H]prazosin | 8.1 |
| α1D | Human | Recombinant (CHO cells) | [3H]prazosin | −7.6 |
| α2A | Human | Recombinant (CHO cells) | [3H]RX821002 | −0.6 |
| α2B | Human | Recombinant (CHO cells) | [3H]RX821002 | −3.1 |
| α2C | Human | Recombinant (CHO cells) | [3H]RX821002 | −11.1 |
| β1 | Human | Recombinant (HEK-293 cells) | [3H](−)CGP12177 | −5.3 |
| β2 | Human | Recombinant (CHO cells) | [3H](−)CGP12177 | 15.1 |
| β3 | Human | SK-N-MC cells | [125I]CYP(+0.1 µM(−)propranolol) | −1.1 |
| AT1 | Human | Recombinant (HEK-293 cells) | [125I][Sar1,Ile8]-AT-II | −5.7 |
| AT2 | Human | Recombinant (HEK-293 cells) | [125I]CGP42112A | −0.2 |
| BZD (central) | Rat | Cerebral cortex | [3H]flunitrazepam | −15.2 |
| BZD (peripheral) | Rat | Heart | [3H]PK11195 | −5.0 |
| CRF1 | Human | Recombinant (CHO cells) | [125I]sauvagine | 4.2 |
| D1 | Human | Recombinant (CHO cells) | [3H]SCH23390 | −3.2 |
| D2L | Human | Recombinant (HEK-293 cells) | [3H]methyl-spiperone | 5.0 |
| D3 | Human | Recombinant (CHO cells) | [3H]methyl-spiperone | −10.9 |
| D4.4 | Human | Recombinant (CHO cells) | [3H]methyl-spiperone | 3.2 |
| D5 | Human | Recombinant (GH4 cells) | [3H]SCH23390 | 9.0 |
| ETA | Human | Recombinant (CHO cells) | [125I]endothelin-1 | 8.6 |
| ETB | Human | Recombinant (CHO cells) | [125I]endothelin-1 | 14.0 |
| GABAA1 | Human | Recombinant (CHO cells) | [3H]muscimol | 3.4 |
| GABAB(1b) | Human | Recombinant (CHO cells) | [3H]CGP54626 | 0.8 |
| AMPA | Rat | Cerebral cortex | [3H]AMPA | −13.1 |
| Kainite | Rat | Cerebral cortex | [3H]kainic acid | −2.2 |
| NMDA | Rat | Cerebral cortex | [3H]CGP39653 | −2.9 |
| H1 | Human | Recombinant (HEK-293 cells) | [3H]pyrilamine | −6.5 |
| H2 | Human | Recombinant (CHO cells) | [125I]APT | −6.2 |
| H3 | Human | Recombinant (CHO cells) | [3H]Nα-methyl-histamine | 10.0 |
| H4 | Human | Recombinant (HEK-293 cells) | [3H]histamine | −5.3 |
| M1 | Human | Recombinant (CHO cells) | [3H]pirenzepine | −9.9 |
| M2 | Human | Recombinant (CHO cells) | [3H]AF-DX384 | −14.8 |
| M3 | Human | Recombinant (CHO cells) | [3H]4-DAMP | −10.1 |
| M4 | Human | Recombinant (CHO cells) | [3H]4-DAMP | 14.4 |
| M5 | Human | Recombinant (CHO cells) | [3H]4-DAMP | −4.5 |
| δ2 (DOP) | Human | Recombinant (CHO cells) | [3H]DADLE | −4.5 |
| κ (KOP) | Rat | Recombinant (CHO cells) | [3H]U69593 | −8.4 |
| μ (MOP) | Human | Recombinant (HEK-293 cells) | [3H]diprenorphine | −12.8 |
| NOP (ORL1) | Human | Recombinant (HEK-293 cells) | [3H]nociception | −6.6 |
| 5-HT1A | Human | Recombinant (HEK-293 cells) | [3H]8-OH-DPAT | −8.2 |
| 5-HT1B | Rat | Cerebral cortex | [125I]P450 (+ 30 µM isoproterenol) | −26.0 |
| 5-HT1D | Rat | Recombinant (CHO cells) | [3H]serotonin | −3.0 |
| 5-HT2A | Human | Recombinant (HEK-293 cells) | [3H]ketanserin | −3.7 |
| 5-HT2B | Human | Recombinant (CHO cells) | [3H]mesulergine | −6.5 |
| 5-HT2C | Human | Recombinant (HEK-293 cells) | [3H]mesulergine | −4.6 |
| 5-HT3 | Human | Recombinant (CHO cells) | [3H]BRL43694 | −2.0 |
| 5-HT4e | Human | Recombinant (CHO cells) | [3H]GR113808 | −1.3 |
| 5-HT5a | Human | Recombinant (HEK-293 cells) | [3H]LSD | 0.2 |
| 5-HT6 | Human | Recombinant (CHO cells) | [3H]LSD | −2.2 |
| 5-HT7 | Human | Recombinant (CHO cells) | [3H]LSD | 2.2 |
| Sigma 1 | Human | Jurkat cells | [3H](+)pentazocine | −25.5 |
| Norepinephrine transporter | Human | Recombinant (CHO cells) | [3H]nisoxetine | −7.9 |
| Dopamine transporter | Human | Recombinant (CHO cells) | [3H]BTCP | 11.4 |
| 5-HT transporter | Human | Recombinant (CHO cells) | [3H]imipramine | 0.3 |
AF-DX384, N-[2-[2-[(dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide; AMPA, 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid; APT, 4-amino-N-[2-[[(cyanoamino)[[3-[3-(1-piperidinylmethyl)phenoxy]propyl]imino]methyl]amino]ethyl]benzamide; AT, angiotensin receptor; AT-II, angiotensin II; BRL43694, granisetron; BTCP, N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine; BZD, benzodiazepine receptor; (−)CGP12177, (−)4-[3-(tert-butylamino)-2-hydroxypropoxy]-1,3-dihydrobenzimidazol-2-one; CGP39653, d,l-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid; CGP42112A, Nα-nicotinoyl-Tyr-(Nα-CBZ-Arg)-Lys-His-Pro-Ile; CGP54626, [S-(R*,R*)]-[3-[[1-(3,4-dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid; CHO, Chinese hamster ovary; CYP, cyanopindolol; DADLE, [d-Ala2, d-Leu5]enkephalin; 4-DAMP, 1,1-dimethyl-4-diphenylacetoxypiperidinium iodide; DOP, delta opioid receptor; ET, endothelin receptor; GR113808, 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester; HEK, human embryonic kidney; 5-HT, serotonin receptor; KOP, kappa opioid receptor; LSD, lysergic acid diethylamide; MOP, mu opioid receptor; NMDA, N-methyl-D-aspartate; NOP, nociceptin/orphanin FQ receptor; 8-OH-DPAT, 1,1-dimethyl-4-diphenylacetoxypiperidinium iodide; ORL, opioid receptor-like; PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide; RX821002, 2-(2,3-dihydro-2-methoxy-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole; SCH23390, 7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine; U69593, N-methyl-2-phenyl-N-[(5S,7R,8R)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide.