Affinity of SL65.0155 for human recombinant 5-HT receptor subtypes
| Receptor | Cell Type | Ligand and Concentration | Affinity of SL65.0155 | |
|---|---|---|---|---|
| nM | Ki, nM | |||
| 5-HT1A | CHO | 8-OH-DPAT | 0.3 | 1,020 |
| 5-HT1B | CHO | GR 125743 | 0.5 | 5,500 |
| 5-HT1D | CHO-K1 | 5-CT | 0.5 | 7,990 |
| 5-HT2A | CHO | Ketanserin | 2 | 1,320 |
| 5-HT2B | CHO-K1 | LSD | 1.2 | 1,560 |
| 5-HT2C | CHO | Mesulergine | 0.7 | 4,780 |
| 5-HT3 | HEK-293 | GR 65630 | 0.69 | >10,000 |
| 5-HT4(e) | CHO | GR 113808 | 0.2 | 0.6 |
| 5-HT5A | HEK-293 | LSD | 1 | >10,000 |
| 5-HT6 | HEK-293 | LSD | 2 | 2,580 |
| 5-HT7 | CHO | LSD | 4 | 3,260 |
| Transporter | HEK-293 | RTI-55 | 0.15 | 905 |
All binding studies were carried out by Cerep except for 5-HT1D, 5-HT3, and the 5-HT transporter, which were carried out by MDS Panlabs (see www.mdsps.com and www.cerep.com for further experimental details). The cell type used for expression is indicated. All ligands were tritiated except RTI-55, which was iodinated.
GR 125743,N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-methyl-4-(4-pyridyl) benzamide; GR 65630, 3-(5-methyl-1H-imidazol-4-yl)-1-(1-methyl-1H-indol-3-yl)-1-propanone; RTI-55, 3 β-(4-iodophenyl) tropane-2 β-carboxylic acid methyl ester; 8-OH-DPAT, 8-hydroxy-aminotetralin; 5-CT, 5-carboxytryptamine, LSD, lysergic acid diethylamide; HEK, human embryonic kidney.