Table 3.
Primary CNS receptor binding data of compound 1–11a
| Compound | Serotonin |
Dopamine |
Histamine |
Acetylcholine |
Opioid |
|
|---|---|---|---|---|---|---|
| 5-HT1A | 5-HT3 | D1 | H1 | M3 | Signal | |
| 1 | 62.3 | NAb | 50.3 | NA | NA | NA |
| 2 | NA | NA | 57.4 | 54.3 | NA | NA |
| 3 | NA | NA | NA | 56.3 | NA | NA |
| 4 | NA | NA | NA | NA | 55.1 | NA |
| 5 | NA | NA | 62.3 | NA | NA | NA |
| 6 | 50.0 | NA | 55.7 | NA | NA | NA |
| 7 | 61.9 | NA | NA | NA | NA | NA |
| 8 | NA | 57.0 | NA | NA | NA | NA |
| 9 | 60.4 | NA | NA | NA | NA | NA |
| 10 | NA | NA | NA | 52.3 | NA | NA |
| 11 | NA | NA | NA | 63.2 | NA | 59.1 |
a
Data represent mean percent inhibition (n = 4 determinations) for compound tested at receptor subtypes. Significant inhibition is considered >50%. All represent human receptors unless otherwise specified.
b
NA, not active