Table 2.
Affinity profile of M100907 derivatives at the 5-HT2AR, 5-HT2BR, 5-HT2CR.
| ID | Linker # | 5-HT2AR | 5-HT2BR | 5-HT2CR | |||
|---|---|---|---|---|---|---|---|
| pKi1 | Ki (nM) | pKi2 | Ki (nM) | pKi3 | Ki (nM) | ||
| 1 | -- | 8.54 | 3.0 | 6.2 | 612 | 7.4 | 41 |
| 2 | -- | N.T. | N.T. | N.T. | |||
| 3 | -- | N.T. | N.T. | N.T. | |||
| 4 | -- | 8.8 | 1.6 | 6.6 | 261 | 7.8 | 15 |
| 5a | 10 | 8.3 | 5.4 | 6.2 | 701 | 6.5 | 312 |
| 5b | 13 | 8.2 | 6.9 | N.D.5 | 6.3 | 472 | |
| 6a | 5 | 8.54 | 3.1 | 6.7 | 202 | 7.6 | 27 |
| 6b | 8 | 8.14 | 7.2 | 6.3 | 476 | 7.2 | 64 |
| 6c | 11 | 8.24 | 5.8 | 6.9 | 126 | 7.1 | 79 |
| 6d | 14 | 8.54 | 3.4 | 6.8 | 157 | 7.1 | 84 |
| 6e | 17 | 8.54 | 3.0 | 6.6 | 267 | 7.3 | 50 |
| 6f | 20 | 7.54 | 32 | 5.9 | 1399 | 6.3 | 245 |
| 6g | 23 | 8.44 | 4.4 | 6.6 | 238 | 7.0 | 101 |
Ki determinations were generously provided by the NIMH Psychoactive Drug Screening Program.
1
Determined by displacement of [3H] ketanserin (0.5 nM) relative to displacement by 10 μM clozapine;
2
Determined by displacement of [3H] LSD (1.0 nM) relative to displacement by 10 μM methysergide;
3
Determined by displacement of [3H] mesulergine (0.5 nM) relative to displacement by 10 μM chlorpromazine.
4
Determined in two independent assays; N.D. = Not determined; Displacement by 10 μM of methylsergide was < 50%. N.T.= Not tested in this assay