Table 1. Pharmacological evaluation of the expressed recombinant receptors.
Receptor | GABA EC50 (µM) mean ± SD | n | PCCP− IC50 (µM) mean ± SD | n | Picrotoxin IC50 (µM) mean ± SD | n |
α1β2γ2 | 31.3±6.5 | 3 | 2.58±0.75 | 3 | 2.02±0.89 | 6 |
α1A253Cβ2γ2 | 30.6±6.4 | 3 | 2.63±0.31 | 3 | 1.79±0.15 | 3 |
α1V256Cβ2γ2 | 2.91±7.4 | 4 | 62.2±22.4 | 4 | 0.74±0.36 | 4 |
α1T260Cβ2γ2 | 44.1±6.4 | 4 | 0.85±0.46 | 4 | 1.31±0.41 | 3 |
α1T261Cβ2γ2 | 111±1 | 3 | 46.4±7.25 | 3 | 1.31±0.71 | 3 |
α1L263Cβ2γ2 | open ch. | 3 | 4.47±1.36 | 3 | 1.10±0.21 | 3 |
α1T264Cβ2γ2 | 126±24 | 4 | 3.15±0.48 | 3 | 1.03±0.35 | 3 |
α1T267Cβ2γ2 | 32.2±11.9 | 3 | 0.77±0.11 | 3 | 0.83±0.48 | 3 |
EC50 for GABA, IC50 for PCCP−, and IC50 for picrotoxin are given for wild type and mutant receptors.