Binding profile of S32212 at multiple classes of 5-HT receptor, α/β-AR, dopamine receptor, histamine receptor, and muscarinic receptor
Standard procedures were used (see Millan et al., 2002). Data are means ± S.E.M. of pKi values, based on three to four determinations, each performed in triplicate.
| Receptor | Tissue | Radioligand | pKi |
|---|---|---|---|
| nM | |||
| h5-HT2C INI | HEK-293 cell line | [3H]Mesulergine (1.0) | 8.18 ± 0.07 |
| h5-HT2C VSV | CHO cell line | [3H]Mesulergine (1.0) | 8.05 ± 0.03 |
| hα2A-AR | CHO cell line | [3H]RX821,002 (1.0) | 7.21 ± 0.08 |
| hα2B-AR | CHO cell line | [3H]RX821,002 (2.0) | 8.24 ± 0.18 |
| hα2C-AR | CHO cell line | [3H]RX821,002 (1.0) | 7.44 ± 0.01 |
| h5-HT2A | CHO cell line | [3H]Ketanserin (0.5) | 8.24 ± 0.01 |
| h5-HT1A | CHO cell line | [3H]WAY100,635 (0.4) | 6.66 ± 0.11 |
| h5-HT1B | CHO cell line | [3H]GR125,743 (1.0) | 7.07 ± 0.19 |
| r5-HT1D | CHO cell line | [3H]5-HT (1.0) | 7.04 ± 0.10 |
| h5-HT2B | CHO cell line | [3H]Mesulergine (1.0) | 6.98 ± 0.01 |
| h5-HT3 | NIE-115 cell line | [3H]BRL43,694 (1.0) | <5 |
| h5-HT4 | CHO cell line | [3H]GR113,808 (0.1) | 6.21 ± 0.08 |
| h5-HT5A | CHO cell line | [3H]LSD (1.0) | 5.98 ± 0.03 |
| h5-HT6 | HEK-293 cell line | [3H]LSD (2.0) | 6.62 ± 0.05 |
| h5-HT7 | CHO cell line | [3H]LSD (4.0) | 6.22 ± 0.01 |
| hα1A-AR | CHO cell line | [3H]Prazosin (0.3) | 5.95 ± 0.11 |
| hα1B-AR | CHO cell line | [3H]Prazosin (0.3) | 5.81 ± 0.13 |
| hβ1-AR | HEK-293 cell line | [3H]CGP12177 (0.15) | 5.35 ± 0.01 |
| hβ2-AR | Sf9 cell line | [3H]CGP12177 (0.15) | <5 |
| hD1 | L cell line | [3H]SCH23390 (0.3) | 6.20 ± 0.01 |
| hD2L | CHO cell line | [3H]Spiperone (0.5) | 5.19 ± 0.07 |
| hD3 | CHO cell line | [3H]Spiperone (0.5) | 5.81 ± 0.03 |
| hSERT | HEK-293 cell line | [3H]Citalopram (2.0) | 5.65 ± 0.16 |
| hNAT | MDCK cell line | [3H]Nisoxetine (2.2) | <5 |
| hDAT | CHO cell line | [3H]GBR12935 (1.0) | 5.49 ± 0.09 |
| rMAO A | Rat cerebral cortex | [3H]Ro41-1049 (10.0) | <5 |
| rMAO B | Rat cerebral cortex | [3H]Ro19-6327 (15.0) | <5 |
| hH1 | CHO cell line | [3H]Pyrilamine (2.0) | <5 |
| hH2 | CHO cell line | [125I]Aminopotendine (1.0) | 6.46 ± 0.05 |
| hH3 | CHO cell line | [3H]N-methylhistamine | <6 |
| hM1 | CHO cell line | [3H]Pirenzepine (11) | 5.44 ± 0.06 |
| hM2 | CHO cell line | [3H]AFDX384 (4.6) | 5.44 ± 0.04 |
WAY100,635, N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-2-pyridinyl-trihydrochloride; GR125,743, N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-methyl-4-(4-pyridyl)benzamide; BRL43,694, N-(9-methyl-9-azabicyclo[3.3.1.]non-3-yl-1-methyl-1H-indazol-3-carboxamide; GR113,808, 1-methyl-1H-indole-3-carboxylic acid 1-[2-(methylsulfonamido)ethyl]piperidin-4-ylmethyl ester; LSD, d-lysergic acid diethylamide; CGP12177, 4-[3-[(1,1-dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one; SCH23390, (R)-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine; GBR12935, 1-(2-diphenylmethoxyethyl)-4-(3-phenylpropyl)piperazine; Ro41-1049, N-(2-aminoethyl)-5-(3-fluorophenyl)-4-thiazolecarboxamide; Ro19-6327, N-(2-aminoethyl)-5-chloro-pyridine-2-carboxamide; AFDX384, N-[2-[2-[(dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide.