Table 2 Functional properties of expressed wild type and mutated GABAA receptor subunits.
From: α subunits in GABAA receptors are dispensable for GABA and diazepam action
Subunit combination | Etomidate (nA; 50 µM) | GABA (nA; 10 mM) | EC50 (µM) | DZ potentiation (%) | Homology to mutated residues |
|---|---|---|---|---|---|
β2 | 4 ± 1 (4) | −4 ± 1 (4) | — | — | — |
γ2 | 0 ± 0 (5) | −4 ± 1 (5) | — | — | — |
β2γ2 | 946 ± 8 (4) | 131 ± 19 (13) | 75 ± 5 (5) | 216 ± 30 (15) | — |
β2Y62Lγ2 | 13 ± 3 (11) | 53 ± 8 (17) | 228 ± 50 (7) | 121 ± 12 (5) | α1F64, γ2F77 |
β2T202Aγ2 | 8 ± 2 (5) | 5 ± 0 (5) | — | — | α1T206, γ2S217 |
β2T202Sγ2 | 380 ± 77 (5) | 203 ± 18 (5) | 3130 ± 260 (4) | 100 ± 7 (4) | α1T206, γ2S217 |
β2Y205Sγ2 | 0 ± 0 (5) | 0 ± 0 (16) | — | — | α1Y209, γ2Y220 |
β2Y205Qγ2 | 6 ± 2 (5) | 1 ± 0 (4) | — | — | α1Y209, γ2Y220 |
γ2F77Yβ2 | 193 ± 25 (4) | 148 ± 23 (11) | 72 ± 15 (5) | 5 ± 2 (5) | α1F64, β2Y62 |
γ2S217Aβ2 | 141 ± 31 (5) | 100 ± 25 (13) | 133 ± 20 (3) | 185 ± 23 (4) | α1T206, β2T202 |
γ2Y220Sβ2 | 76 ± 17 (5) | 10 ± 1 (12) | — | — | α1Y209, β2Y205 |
γ2Y220Qβ2 | 777 ± 113 (5) | 127 ± 40 (6) | 367 ± 139 (3) | 127 ± 11 (6) | α1Y209, β2Y205 |