TABLE 2.
KD-SR | koff-SR | kon-SR | EC50-GABA | kon-GABA | kon-THIP | |
---|---|---|---|---|---|---|
nM | s−1 | M−1·s−1 | mM | M−1·s−1 | ||
α1β2 | 124 | 10 ± 1 | (8.2 ± 0.7) × 107 | 6 | (2.2 ± 0.4) × 107 | (5.5 ± 0.7) × 106 |
α1β2-GKER | 69 | 7 ± 1 | (9.7 ± 0.8) × 107 | 8 | (2.0 ± 0.2) × 107 | N.A. |
α1β2R207A | 230 | 23 ± 2* | (9.9 ± 1.0) × 107 | 139 | (3.8 ± 0.4) × 106* | (1.9 ± 0.7) × 105* |
α1R67Aβ2-GKER | 26 | 12 ± 2 | (4.5 ± 0.6) × 108* | 1100 | (1.4 ± 0.1) × 106* | (5.6 ± 1.7) × 105* |
α1R132Aβ2-GKER | 542 | 63 ± 9* | (1.2 ± 0.2) × 108 | 31 | (1.7 ± 0.4) × 107 | N.A. |
N.A., not available.
Differences between mutants and their appropriate control (see Results) were calculated using one-way ANOVA with post-hoc Tukey test at p < 0.05 (Prism 4). GABA unbinding rates were also estimated using a kinetic model (see Fig. 7).