Table 1. The Affinity of the Dopamine Receptor Antagonists and Agonists on D2L Wild-Type and D2L F3906.52W Receptora.
| compound | Ki measured | Ki for D2L wild-type (nM) | Ki for D2L F3906.52W (nM) | Kimut/Ki |
|---|---|---|---|---|
| Antagonists | ||||
| spiperone | Ki | 0.09 (0.08−0.12)b (−1.05)c | 0.14 (0.08−0.19)b (−1.16)c | 1.6 |
| haloperidol | Ki | 0.41 (0.24−0.69)b (−0.84)c | 0.60 (0.52−0.69)b (−1.04)c | 1.5 |
| nemonapride | Ki | 0.14 (0.10−0.18)b (−0.84)c | 1.5 (1.2−1.8)b (−0.98)c | 11 |
| Agonists | ||||
| dopamine | K0.5 | 450 (380−660)b (−0.43)c | >20 000 | >44 |
| Khigh | 8.4 (4.6−25)b (31%)d | |||
| Klow | 2000 (1400−2800)b | >20 000 | >10 | |
| 7-OH-DPAT | K0.5 | 69 (49−98)b (−0.40)c | 2200 (1600−3200)b (−0.45)c | 32 |
| Khigh | 1.1 (0.45−2.5)b (39%)d | 21 (11−41)b (28%)d | 19 | |
| Klow | 190 (110−340)b | 5600 (3700−8500)b | 29 | |
| quinpirole | K0.5 | 610 (460−790)b (−0.44)c | 2500 (1700−3700)b (−0.56)c | 4 |
| Khigh | 13 (6.9−25)b (31%)d | 22 (11−41)b (25%)d | 1.7 | |
| Klow | 2100 (1500−3200)b | 5000 (3200−7500)b | 2.3 | |
a
The affinities of investigated substances were determined on membrane preparations of stably transfected CHO cells expressing either D2L wild-type or D2L F3906.52W receptor using [3H]spiperone displacement study. Data are derived from normalized curves of 3-4 experiments done in triplicate. The factor Kimut/Ki indicates the changes in the affinity.
b
95% confidence interval.
c
Hill slope.
d
Fraction of high-affinity sites.