TABLE 1.
Predicted physicochemical properties and in vitro function data on dopamine D3 receptor of NGB 2904, JJC 4-077, CJB 090, and PG 01037
| Parameter | NGB 2904 | JJC 4-077 | CJB 090 | PG 01037 |
|---|---|---|---|---|
| IC50 (nM)a | 14.4 ± 0.5 | 42.0 ± 1.3 (26)b | 6.3 ± 1.7 (30)b | 3.0 ± 0.7 |
| D2 Kin (nM)a | 112 ± 22 | 168 ± 29 | 24.8 ± 8.6 | 93 ± 12 |
| D3 Kin (nM)a | 2.0 ± 0.4 | 1.5 ± 0.1 | 0.4 ± 0.02 | 0.7 ± 0.1 |
| Molecular mass (Da) | 619.32 | 583.38 | 556.26 | 572.35 |
| cLogP | 7.00 | 6.55 | 5.36 | 5.32 |
a
From Grundt et al., (2007).
b
Partial agonist activity: EC50 (% stimulation).