Table 2.
Binding affinities of Ro15-1788, flurazepam, zolpidem, and DMCM for wild-type (α 1β 2γ 2) and mutant receptors
| Receptor | Ro15–1788 |
Flurazepam |
Zolpidem |
DMCM |
||||
|---|---|---|---|---|---|---|---|---|
| Ki | n | Ki | n | Ki | n | Ki | n | |
| αβγ | 5.1 ± 1.5 | 3 | 165 ± 23 | 5 | 108 ± 22 | 3 | 10.8 ± 2.4 | 3 |
| αβγW183C | 4.6 ± 0.4 | 3 | 117 ± 7 | 3 | 213 ± 57 | 3 | 5.5 ± 0.6 | 3 |
| αβγE189C | 7.7 ± 2.4 | 3 | 213 ± 40 | 3 | 198 ± 10 | 4 | 16.8 ± 3.5 | 3 |
| αβγR197C | 5.1 ± 1.0 | 4 | 68 ± 12* | 3 | 47 ± 7 | 3 | 20.4 ± 5.5 | 3 |
Ki values were determined by displacement of [3H] Ro15-1788 binding and represent the equilibrium dissociation constant (apparent affinity) of the unlabeled ligand. Data represent mean ± SD for n experiments. Values significantly different from WT receptors are indicated (*p < 0.05).