Table 2.
Parameters derived from Pro-substituted GlyR expressed in oocytes using nonsense suppression.
| Site | Substitution | pEC50, M | EC50, μM | nH | n |
|---|---|---|---|---|---|
| P30( α1β1L) | Pro | 3.948 ± 0.04 | 113 | 2.9 ± 1.2 | 6 |
| CFP | 3.825 ± 0.06 | 150 | 2.8 ± 0.7 | 6 | |
| TFP | 4.013 ± 0.05 | 97 | 2.7 ± 1.3 | 5 | |
| Pip | 4.439 ± 0.03 * | 36 | 2.7 ± 0.7 | 4 | |
| 2MeP | 3.434 ± 0.06 * | 368 | 1.6 ± 0.3 | 5 | |
| 3MeP | 5.046 ± 0.05 * | 8.9 | 3.0 ± 2.7 | 4 | |
| Vah | 4.684 ± 0.03 * | 21 | 3.8 ± 0.5 | 4 | |
| P96 (loopA) | Pro | 3.951 ± 0.04 | 112 | 2.7 ± 1.1 | 5 |
| CFP | 3.840 ± 0.05 | 145 | 3.2 ± 0.7 | 4 | |
| TFP | 3.898 ± 0.03 | 127 | 2.9 ± 0.7 | 4 | |
| Pip | 3.667 ± 0.02 * | 215 | 2.9 ± 0.3 | 4 | |
| 2MeP | 3.596 ± 0.03 * | 254 | 2.8 ± 0.5 | 4 | |
| 3MeP | 3.289 ± 0.02 * | 514 | 3.0 ± 0.2 | 4 | |
| Vah | 4.029 ± 0.05 | 94 | 1.5 ± 0.3 | 4 | |
| P146 (CysL) | Pro | 4.052 ± 0.02 | 89 | 2.5 ± 0.4 | 6 |
| CFP | 4.350 ± 0.03 * | 45 | 3.7 ± 0.6 | 6 | |
| TFP | 3.806 ± 0.05 * | 156 | 2.3 ± 0.4 | 5 | |
| Pip | 4.279 ± 0.11 * | 53 | 1.9 ± 0.7 | 5 | |
| 2MeP | 3.568 ± 0.04 * | 270 | 2.2 ± 0.5 | 6 | |
| 3MeP | ND | ||||
| Vah | NR | 6 | |||
| P230 (M1) | Pro | 3.922 ± 0.06 | 119 | 2.5 ± 0.9 | 4 |
| CFP | 4.131 ± 0.04 | 74 | 1.4 ± 0.2 | 4 | |
| TFP | 3.904 ± 0.06 | 125 | 3.0 ± 1.4 | 4 | |
| Pip | 4.166 ± 0.08 | 68 | 1.1 ± 0.2 | 4 | |
| 2MeP | 3.751 ± 0.08 | 177 | 1.6 ± 0.5 | 4 | |
| 3MeP | 4.471 ± 0.08 * | 34 | 1.1 ± 0.4 | 4 | |
| Vah | 4.015 ± 0.02 | 97 | 2.6 ± 0.4 | 4 |
pEC50 = −log EC50; nH = Hill coefficient. Data = mean ± SEM. * = significantly different to WT, p < 0.05. NR = non-responsive; ND = not determined.