Summary of GABA and FLZM concentration response data for wild-type and mutant receptors
Data represent mean ± S.D. nH values are calculated Hill coefficients.
Receptor | GABA EC50 | nH | n | EC50 mut/EC50 αβγ | FLZM EC50 | nH | n | EC50 mut/EC50 αβγ |
|---|---|---|---|---|---|---|---|---|
| μM | μM | |||||||
| α1β2γ2 | 17.4 ± 7.0 | 1.6 ± 0.3 | 4 | 1 | 0.47 ± 0.15 | 1.3 ± 0.3 | 5 | 1 |
| α1D97Cβ2γ2 | 168.8 ± 73.5 | 0.94 ± 0.2 | 4 | 9.7* | 0.56 ± 0.12 | 1.1 ± 0.1 | 3 | 1.2 |
| α1T98Cβ2γ2 | N.E. | N.E. | ||||||
| α1F99Cβ2γ2 | 50.6 ± 0.5 | 1.1 ± 0.1 | 3 | 2.9 | 0.43 ± 0.12 | 1.6 ± 0.2 | 3 | 0.91 |
| α1F100Cβ2γ2 | N.E. | N.E. | ||||||
| α1H101Cβ2γ2 | 50.5 ± 26.1 | 1.56 ± 0.3 | 7 | 2.9 | 9.0 ± 0.13 | 1.8 ± 0.1 | 3 | 19.1* |
| α1N102Cβ2γ2 | 410 ± 305 | 0.56 ± 0.2 | 7 | 23.6* | 2.6 ± 0.95 | 1.0 ± 0.2 | 3 | 5.5* |
| α1G103Cβ2γ2 | 10.9 ± 5.6 | 1.3 ± 0.3 | 4 | 0.6 | 0.27 ± 0.03 | 1.2 ± 0.4 | 4 | 0.57 |
| α1K104Cβ2γ2 | 13.3 ± 6.7 | 0.96 ± 0.2 | 3 | 0.8 | 0.40 ± 0.18 | 1.3 ± 0.5 | 5 | 0.85 |
| α1K105Cβ2γ2 | 23.2 ± 3.5 | 1.3 ± 0.1 | 3 | 1.3 | 0.29 ± 0.10 | 1.1 ± 0.2 | 3 | 0.62 |
| α1S106Cβ2γ2 | 4.9 ± 1.8 | 1.3 ± 0.1 | 3 | 0.3** | 0.44 ± 0.14 | 1.5 ± 0.2 | 3 | 0.94 |