Table 2.
Inhibition constants (pKi) of selected standard ligands determined in radioligand displacement experiments. pKi values were determined at receptors fused to the C-terminal fragment of the Emerald luciferase using whole cells and at wild-type receptors using homogenates. Data represent mean pKi ± SEM determined in three independent experiments, each performed in triplicate.
| cpd | D2longR | D3R | D4.4R | ||||
|---|---|---|---|---|---|---|---|
| ELucC Fusion Protein | wt | ELucC Fusion Protein | wt | ELucC Fusion Protein | wt | ||
| aripiprazole | 9.25 ± 0.16 | 8.32 ± 0.02 | 8.9 ± 0.24 | 7.85 ± 0.08 | 7.64 ± 0.15 | 7.85 ± 0.08 | |
| quinpirole | 7.29 ± 0.07 | hi | 7.90 ± 0.10 | 7.63 ± 0.05 | 8.00 ± 0.08 | 6.58 ± 0.01 | 8.00 ± 0.08 |
| lo | 6.11 ± 0.02 | ||||||
| haloperidol | 9.45 ± 0.05 | 9.58 ± 0.13 | 8.27 ± 0.08 | 8.93 ± 0.02 | 8.27 ± 0.02 | 8.93 ± 0.02 | |
| nemonapride | 9.95 ± 0.13 | 9.76 ± 0.08 | 9.76 ± 0.06 | 9.33 ± 0.02 | 9.69 ± 0.08 | 9.33 ± 0.02 | |