Table 4.
The maximal effects (Emax) and potencies (EC50 and IC50) of compounds determined in an assay of D3R activation.a
| compound | D3R GPA GαoA agonism | D3R GPA GαoA antagonism | |||
|---|---|---|---|---|---|
| pEC50 ± SEM | EC50 (nM) | Emax ± SEM (%) | pIC50 ± SEM | IC50 (nM) | |
| cariprazine | 8.72 ± 0.14 | 1.89 | 45.1 ± 1.6 | 8.70 ± 0.32 | 2.02 |
| 13a | 8.80 ± 0.20 | 1.60 | 49.3 ± 2.3 | 8.34 ± 0.23 | 4.62 |
| 11b | ND | ND | ND | 7.44 ± 0.25 | 36.00 |
| 13b | ND | ND | ND | 8.73 ± 0.16 | 1.87 |
| 6c | 8.79 ± 0.14 | 1.64 | 95.4 ± 3.8 | - | - |
| 13c | 8.54 ± 0.16 | 2.87 | 104.8 ± 4.8 | - | - |
| 11d | ND | ND | ND | 7.47 ± 0.15 | 33.63 |
| 13d | ND | ND | ND | 8.49 ± 0.24 | 3.21 |
| 6e | ND | ND | ND | 7.87 ± 0.13 | 13.41 |
| 7e | ND | ND | ND | 7.70 ± 0.19 | 19.85 |
| 13e | ND | ND | ND | 7.76 ± 0.13 | 17.45 |
| 21a | 8.22 ± 0.20 | 6.07 | 73.2 ± 4.9 | - | - |
| 22a | 7.70 ± 0.13 | 19.91 | 41.5 ± 1.9 | 7.92 ± 0.35 | 12.12 |
| 22b | 7.80 ± 0.28 | 16.02 | 33.0 ± 2.9 | 7.89 ± 0.37 | 12.93 |
| Quinpirole | 8.59 ± 0.06 | 2.59 | 100.1 ± 1.7 | - | - |
| Haloperidol | - | - | - | 8.60 ± 0.08 | 2.54 |
a
Compounds were tested in an amplified GαoA G protein (GPA GαoA) activation assay as agonists and antagonists. ND indicates no agonist response detected, ‘-’ indicates compound not tested. Data represent the mean ± SEM of three independent experiments performed in duplicate.