Diazepam and DOV 51892 potentiation of GABA-gated currents mediated by different GABAA receptor constructs
Values represent either the mean ± S.E.M. (potentiation) or mean (95% confidence interval) (EC50) of results from five to nine oocytes.
| Compound | Construct | Potentiation | Emax/Diazepam Emax | EC50 |
|---|---|---|---|---|
| % | μM | |||
| Diazepam | α1β2γ2S | 104 ± 3 | 1.00 | 0.28 (0.21-0.38) |
| α2β2γ2S | 135 ± 3 | 1.00 | 0.053 (0.047-0.059) | |
| α3β2γ2S | 166 ± 2 | 1.00 | 0.074 (0.068-0.080) | |
| α5β2γ2S | 77 ± 2 | 1.00 | 0.069 (0.062-0.076) | |
| DOV 51892 | α1β2γ2S | 152 ± 7 | 1.46 | 0.80 (0.70-0.90) |
| α2β2γ2S | 93 ± 7 | 0.69 | 1.57 (1.2-2.0) | |
| α3β2γ2S | 77 ± 2 | 0.46 | 2.0 (1.7-2.4) | |
| α5β2γ2S | 74 ± 2 | 0.96 | 3.8 (3.1-4.7) |