Table 2. Binding affinities for D2, D3, 5-HT1A, 5-HT2A, 5-HT2C and H1 receptors of compounds 7–26 and reference antipsychotics.a .
| Compound | Binding data of compounds, Ki±SEM (nM) | |||||
| D2 | 5HT1A | 5HT2A | D3 | 5HT2C | H1 | |
| 7 | >10000b | >10000b | 373.9±33.0 | – | – | – |
| 8 | >10000b | >10000b | >10000b | – | – | – |
| 9 | >10000b | >10000b | >10000b | – | – | – |
| 10 | >10000b | >10000b | >10000b | – | – | – |
| 11 | 2568.5±321.3 | 19.0±2.3 | 61.4±5.8 | – | – | – |
| 12 | 2968.5±381.1 | 18.9±1.6 | 11.3±1.2 | – | – | – |
| 13 | 96.7±9.5 | >10000 | 17.2±1.6 | – | – | – |
| 14 | 14.8±1.8 | 6.8±0.7 | 0.22±0.02 | 218.6±35.2 | 19.4±98.6 | 13.2±3.4 |
| 15 | 125.8±13.5 | 14.2±1.3 | 27.2±2.8 | – | – | – |
| 16 | 18.3±1.6 | 10.5±1.2 | 6.6±0.8 | 15.5±1.9 | 501.5±56.2 | 18.9±2.1 |
| 17 | 487.2±46.3 | >10000 | 50.8±5.3 | – | – | – |
| 18 | 94.5±8.9 | 51.0±4.9 | 24.7±2.8 | – | – | – |
| 19 | >10000 | >10000 | >10000 | – | – | – |
| 20 | 125.3±12.4 | 14.8±1.5 | 15.8±1.3 | – | – | – |
| 21 | 137.5±13.6 | 345.8±35.9 | 113.9±12.1 | – | – | – |
| 22 | 23.0±2.6 | 4.6±0.8 | 1.1±0.1 | 7.7±0.6 | 860.7±86.2 | >10000b |
| 23 | >10000 | 449.6±49.8 | 54.1±6.9 | – | – | – |
| 24 | 91.0±11.2 | 96.6±10.3 | 50.3±6.5 | – | – | – |
| 25 | >10000 | >10000 | 389.8±36.5 | – | – | – |
| 26 | 260.3±32.1 | 60.6±8.6 | 59.2±7.6 | – | – | – |
| risperidone | 3.7±0.3 | 180±15 | 0.18±0.02 | 9.7±0.9 | 14.5±2.2 | 21.7±2.7 |
| clozapine | 128.7±1.9 | 141.6±1.6 | 11.6±1.3 | 239.8±29.6 | 16.2±2.7 | 3.8±0.5 |
a
Ki values are taken from three experiments, expressed as means ±SEM.
b
The Ki values were not calculated because the inhibition percentages at 10 µM were too low.