GABA EC50 values and SR-95531 apparent KI values for introduced cysteines in the loop E region of the GABAA receptor
GABA EC50 values and SR-95531 apparent KI values were measured using two-electrode voltage clamp as described under Materials and Methods. All EC50 and apparent KI values are expressed as the average of at least three independent experiments ± S.D.
Receptor | EC50 | n | mut/wt | KI | n | mut/wt |
|---|---|---|---|---|---|---|
| μM | nM | |||||
| α1βγ2 | 13.1 ± 3.7 | 4 | 1 | 110 ± 24 | 4 | 1 |
| α1M113Cβγ2 | 18.4 ± 8.3 | 4 | 1.4 | 89.5 ± 5.5 | 3 | 0.8 |
| α1P114Cβγ2 | 70.8 ± 20.5 | 4 | 5.4** | 355.0 ± 67.4 | 3 | 3.2* |
| α1N115Cβγ2 | 41.6 ± 10.4 | 3 | 3.2 | 92.5 ± 16.4 | 3 | 0.8 |
| α1K116Cβγ2 | 18.9 ± 12.0 | 4 | 1.4 | 92.0 ± 21.7 | 3 | 0.8 |
| α1L117Cβγ2 | 2100 ± 272 | 5 | 160.6** | 385 ± 256 | 3 | 3.5* |
| α1L118Cβγ2 | 320 ± 93.5 | 3 | 24.5** | 83.7 ± 17.5 | 3 | 0.8 |
| α1R119Cβγ2 | 3400 ± 910 | 3 | 260.5** | 450 ± 135 | 3 | 4.0** |
| α1I120Cβγ2 | 170 ± 61 | 3 | 13.1** | 170 ± 100 | 3 | 1.6 |
| α1T121Cβγ2 | 11.5 ± 1.4 | 3 | 0.9 | 51.5 ± 5.0 | 3 | 0.5* |
| α1E122Cβγ2 | 36.2 ± 11.5 | 6 | 2.8 | 63.3 ± 13.1 | 3 | 0.6 |
| α1D123Cβγ2 | 69.1 ± 24.5 | 3 | 5.3** | 155 ± 17.5 | 3 | 1.4 |
| α1G124Cβγ2 | 550 ± 120 | 3 | 42** | 1155 ± 245 | 3 | 10.4** |
| α1T125Cβγ2 | 28.0 ± 5.6 | 3 | 2.1 | 85.7 ± 11.7 | 3 | 0.8 |
| α1L126Cβγ2 | 49.3 ± 11.6 | 5 | 3.8* | 101 ± 1.26 | 3 | 0.9 |
| α1L127Cβγ2 | 190 ± 18 | 3 | 14.5** | 167 ± 57 | 4 | 1.5 |
| α1Y128Cβγ2 | 372 ± 31 | 3 | 28.4** | 737 ± 99 | 3 | 6.7** |
| α1T129Cβγ2 | 1330 ± 329 | 8 | 102** | 235 ± 102 | 3 | 2.1 |
| α1M130Cβγ2 | 86.2 ± 25.8 | 5 | 6.6** | 70.7 ± 2.8 | 3 | 0.64 |
| α1R131Cβγ2 | 883 ± 358 | 6 | 67.4** | 937 ± 279 | 3 | 8.5** |
| α1L132Cβγ2 | 86 ± 33.5 | 4 | 6.6** | 299 ± 56 | 3 | 2.7 |