Table 1.
Analysis of biological activity at the rat 5-HT2A receptor. Ki values for [3H]-ketanserin competition displacement assays in NIH-3T3 cells expressing the rat 5-HT2A receptor and functional potency for stimulating inositol phosphate accumulation in the same cells.
| Drug | clog P | 5-HT2AKi, nM (SEM) | n | EC50, nM (SEM) | Intrinsic Activity % 5-HT (SEM) | n |
|---|---|---|---|---|---|---|
| 1 | 2.45 | 13 (6.0) | 2 | 22 (3.8) | 73 (5) | 3 |
| 2 | 2.65 | 1.0 (0.12) | 5 | 13 (1.9) | 88 (4) | 3 |
| 3a | 3.46 | 4.5 (0.76) | 3 | 241 (46) | 61 (9) | 3 |
| 3b | 3.77 | 3.1 (0.55) | 4 | 258 (45) | 72 (2) | 3 |
| 4a | 2.90 | 11 (1.4) | 3 | 9.4 (1.2) | 61 (6) | 3 |
| 4b | 3.21 | 3.6 (0.73) | 6 | 19 (1.9) | 86 (7) | 5 |
| 5a | 2.90 | 8.4 (0.35) | 3 | 146 (30) | 64 (12) | 3 |
| 5b | 3.21 | 5.3 (0.57) | 7 | 78 (11) | 74 (8) | 4 |
| 6 | 3.77 | 1.0 (0.12) | 5 | 13 (1.9) | 102 (6) | 3 |