Table II.
Peak currents (nA) |
EC50 (μM) |
Hill coefficient, n |
τ (s) |
|||||
---|---|---|---|---|---|---|---|---|
Receptor | GABA | Muscimol | GABA | Muscimol | GABA | Muscimol | GABA | Muscimol |
WT ρ1 | 237–169 | 298–161 | 0.89 ± 0.01 | 1.05 ± 0.02 | 2.04 ± 0.06 | 1.53 ± 0.05 | 37.80 ± 10.06 | 5.97 ± 2.24 |
R158D | No response | No response | N/A | N/A | N/A | N/A | N/A | N/A |
R158A | 333–157 | 348–61 | 208.9 ± 19.66 | 110.2 ± 6.65 | 1.20 ± 0.10 | 1.41 ± 0.12 | 1.04 ± 0.36 | 1.17 ± 0.44 |
D204R | 484–201 | 266–127 | 2.75 ± 0.13 | 5.3 ± 0.19 | 1.87 ± 0.08 | 1.36 ± 0.05 | 7.25 ± 1.83 | 1.81 ± 0.29 |
D204A | 1003–530 | 51–28 | 12.4 ± 0.28 | 8.5 ± 0.52 | 1.53 ± 0.08 | 1.29 ± 0.09 | 1.89 ± 0.22 | 2.34 ± 0.54 |
R158D– D204R | No response | No response | N/A | N/A | N/A | N/A | N/A | N/A |
The above data are the averages obtained from five or more different oocytes from two or more different batches. Dose-response data (mean ± SD for four to eight determinations in two to three experiments) for the wild-type (WT) human ρ1 GABAC receptor as well as the mutant receptors are obtained by fitting of the Hill equation. Peak amplitudes of responses to GABA and muscimol for each mutant receptor are normalized to the saturating response obtained at the highest concentration of the respective agonist. τ values obtained by fitting a simple exponential to the recovery phase of the membrane current responses to the agonist concentrations in the range EC30–E70.