Table 1.
Summary of GABA and FLZM concentration response data for wildtype and mutant receptors.
| Receptor | GABA EC50 (μM) | nH | n | EC50 mut/EC50 αβγ | FLZM EC50 (μM) | nH | n | EC50 mut/EC50 αβγ |
|---|---|---|---|---|---|---|---|---|
| α1β2γ2 | 17.4 ± 7.0 | 1.6 +/− .3 | 4 | 1 | .47 ± .15 | 1.3 ± .3 | 5 | 1 |
| α1 D97C β2γ2 | 168.8 ± 73.5 | .94 ± .2 | 4 | 9.7 * | .56 ± .12 | 1.1 ± .1 | 3 | 1.2 |
| α1 T98C β2 γ2 | No expression | No Expression | ||||||
| α1 F99C β2 γ2 | 50.6 ± .5 | 1.1 ± .1 | 3 | 2.9 | .43 ± .12 | 1.6 ± .2 | 3 | 0.91 |
| α1 F100C β2γ2 | No expression | No Expression | ||||||
| α1 H101C β2 γ2 | 50.5 ± 26.1 | 1.56 ± .3 | 7 | 2.9 | 9.0 ± .13 | 1.8 ± .1 | 3 | 19.1 * |
| α1 N102C β2 γ2 | 410 ± 305 | .56 ± .2 | 7 | 23.6 * | 2.6 ± .95 | 1.0 ± .2 | 3 | 5.5 * |
| α1 G103C β2 γ2 | 10.9 ± 5.6 | 1.3 ± .3 | 4 | 0.6 | .27 ± .03 | 1.2 ± .4 | 4 | 0.57 |
| α1 K104C β2 γ2 | 13.3 ± 6.7 | .96 ± .2 | 3 | 0.8 | .40 ± .18 | 1.3 ± .5 | 5 | 0.85 |
| α1 K105C β2 γ2 | 23.2 ± 3.5 | 1.3 ± .1 | 3 | 1.3 | .29 ± .10 | 1.1 ± .2 | 3 | 0.62 |
| α1 S106C β2 γ2 | 4.9 ± 1.8 | 1.3 ± .1 | 3 | 0.3 ** | .44 ± .14 | 1.5 ± .2 | 3 | 0.94 |
Data represent mean ± SD. nH values are calculated Hill coefficients.
**
Statistically different from wild type (p < .001),
*
statistically different from wild type (p< .05)