TABLE 2
Affinity constants (IC50corr) of SB269,652 for wild-type D3 and D2 and chimeric dopamine D3/D2 receptors in transiently transfected COS-7 cells
The amount of cDNA transiently transfected into COS-7 cells was 4 μg in each case. The concentration of [3H]nemonapride in displacement experiment was 2 nM. IC50corr = IC50 corrected for [3H]nemonapride occupancy. Data are the mean ± S.E.M. of at least three experiments, each performed in triplicate.
| [3H]Nemonapride Kd | SB269,652 | Wild-Type and Chimeric Receptors | ||
|---|---|---|---|---|
| IC50corr | Inhibition | |||
| nM | nM | % | ||
| D2 wild type | 0.03 ± 0.004 | 8.23 ± 0.71 | 8.1 ± 7.5 |  |
| D3 wild type | 0.04 ± 0.010 | 0.69 ± 0.13 | 80.1 ± 2.7 |  |
| Chimera A | 0.03 ± 0.003 | 9.12 ± 1.42 | 13.8 ± 3.2 |  |
| Chimera B | 0.04 ± 0.010 | 5.92 ± 0.63 | 44.1 ± 1.8 |  |
| Chimera C | 0.03 ± 0.003 | 5.86 ± 0.32 | 47.9 ± 1.7 |  |
| Chimera D | 0.04 ± 0.002 | 6.09 ± 0.42 | 52.5 ± 1.7 |  |
| Chimera E | 0.03 ± 0.010 | 0.31 ± 0.02 | 91.6 ± 2.8 |  |
| Chimera F | 0.03 ± 0.003 | 0.21 ± 0.01 | 80.1 ± 2.5 |  |
| Chimera G | 0.04 ± 0.010 | 5.98 ± 0.17 | 31.3 ± 2.6 |  |
| Chimera H | 0.06 ± 0.010 | 7.07 ± 0.69 | 79.6 ± 1.7 |  |
| Chimera I | 0.04 ± 0.010 | 1.38 ± 0.10 | 89.9 ± 1.3 |  |