Table 2.
Binding Affinity Constants of Compounds to Dopamine, 5HT and Histamine Receptors.
| Compds | Binding (Ki±SEM) Data of Synthetic Compounds at Selected Receptors (nM) | ||||||
|---|---|---|---|---|---|---|---|
| D2 | D3 | D4 | 5HT1A | 5HT2A | 5HT2C | H1 | |
| Cloz(1)a | 130 | 240 | 54 | 140 | 8.9 | 17.0 | 1.8 |
| Hal (2) a | 1.4 | 2.5 | 3.3 | 3600 | 120 | 4700 | 440 |
| 10b | 155 | 600 | 2100 | ND | ND | ND | ND |
| 11b | 170 | 220 | 520 | ND | ND | ND | ND |
| 12 | 98.0±15.3 | 244.1±106.0 | 6.53±0.76 | 30.5±5.0 | 22.0±4.0 | 4132±1081 | 911.8±152.0 |
| 13 | 43.3±13.3 | 158.8±35.1 | 6.6±0.6 | 117.4±32.6 | 23.6±2.7 | 1425±207 | 188.6±16.0 |
| 14 | 178.4±29.2 | 548.1±246.0 | 41.8±9.0 | 2332±470 | 194.8±53.0 | 3513±912 | 1014±206 |
ND = Not Determined.; Hal = Haloperidol; Cloz = Clozapine
a
Data for compounds 1 & 2 were obtained from ref. 12b.
b
Data from Pfizer Global Research and Development Laboratories by A. W. Schmidt.