Affinity of APD791 and its major metabolites for human 5-HT2A, 5-HT2B, and 5-HT2Creceptors using radioligand competition binding assays
| Receptor | Ki | ||
|---|---|---|---|
| APD791 | APD791-M1 | APD791-M2 | |
| nM ± S.E.M. (n) | |||
| Human 5-HT2A | 4.9 ± 0.42 (26) | 1.8 ± 0.25 (2) | 2.2 ± 0.5 (5) |
| Rat 5-HT2A | 3435 ± 686 (7) | 729 (1) | 334 (1) |
| Rabbit 5-HT2A | 3.6 (1) | 1.1 (1) | 1.1 (1) |
| Dog 5-HT2A | 5.5 ± 1.3 (6) | 4.6 (1) | 1.2 (1) |
| Monkey 5-HT2A | 1.2 ± 0.3 (2) | 1.7 ± 0.1 (2) | 2.1 ± 0.3 (2) |
| Human 5-HT2B | >10,000 (20) | >10,000 (2) | 6812 ± 855 (2) |
| Human 5-HT2C | >10,000 (24) | 5874 ± 289 (2) | 2347 ± 307 (2) |