Table 1.
Inhibition constants (Ki, nM)* of compounds on ligand binding to homogenates of brain tissue
| Compounds | vs[125I]4 | vs[125I]9 | Compounds | vs[125I]4 | vs[125I]9 |
|---|---|---|---|---|---|
| 14a -OMe | >8,000 | >4,000 | 14h- NH(CH CH F) | 217 ± 20 | 12 ± 3 |
| 14c -OH | 150 ± 30 | 9.0 ± 2.1 | 4 | 5.1 ± 1.2 | >1,000 |
| 14d -NO2 | >4,000 | 500 ± 30 | 9 | >5,000 | 5.0 ± 0.4 |
| 14e -NH2 | 375 ± 150 | 9.0 ± 3.2 | 7 | >3,000 | 1.2 ± 0.2 |
| 14f -NHMe | 122 ± 40 | 7.5 ± 2.5 | 8 | >10,000 | 2.8 ± 0.5 |
| 14g -NMe2 | >7,000 | 837 ± 80 | 10 | >8,000 | 152 ± 20 |
*
Values are the mean ± SEM of three independent experiments, each in duplicate.