Table 4.
Binding Profile of Selected Synthetic Compounds and Their Comparison with Standard Agents
| Binding (Ki ± SEM) data of compounds at selected receptors (nM) | ||||||||
|---|---|---|---|---|---|---|---|---|
| Receptors | 16 | 18 | 19 | 23 | 24 | 25 | Cloz.* | Hal* |
| D2 | 37.0 ± 0.9 | 119 ± 0.9 | 98.0 ± 15.3 | 124 ± 10 | 183 ± 21 | 186 ± 16 | 130 | 0.89 |
| D4 | 7.4 ± 0.9 | 4.5 ± 0.9 | 6.5 ± 0.8 | 3.5 ± 0.2 | 5.7 ± 0.3 | 1.8 ± 0.1 | 54 | 10 |
| 5HT1A | 24.0 ± 0.9 | 25.0 ± 0.9 | 30.5 ± 5.0 | 1.1 ± 0.1 | 6.2 ± 0.5 | 3.6 ± 0.2 | 140 | 3600 |
| 5HT2A | 57.6 ± 2.8 | 46.0 ± 4.2 | 22.0 ± 4.0 | 50.0 ± 3.0 | 26.0 ± 1.0 | 18.0 ± 1.0 | 8.9 | 120 |
| 5HT2C | MP | MP | 4132 ± 1081 | MP | 8097 ± 495 | 8277 ± 497 | 17 | 4700 |
| 5HT7 | ND | ND | ND | 90.0 ± 4.0 | 291 ± 36 | 208 ± 33 | ND | ND |
| H1 | 62.9 ± 12.7 | 67.9 ± 9.7 | 912 ± 152 | 167 ± 24 | 212 ± 30 | 262 ± 23 | 1.8 | 440 |
| Alpha 2C | ND | ND | 80.0 ± 9.6 | 308.2 ± 24.4 | 45.1 ± 8.5 | 194.5 ± 8.5 | ND | ND |
| M1 | MP | MP | MP | MP | MP | MP | 1.8 | 1600 |
*
Cloz, Clozapine; Hal, Haloperidol; ND = Not determined; MP = Missed primary assay threshold of 50% inhibition,