Table 3.
Receptor | ent-9 | ent-7 |
---|---|---|
α 1 β 2 γ 2L | 9.2 ± 5.2** | 7.8 ± 3.9** |
α1(Q241L)β2γ2L | 1.3 ± 0.1**, ** | 1.3 ± 0.3*, ** |
α1(S240L)β2γ2L | 9.4 ± 2.9**, # | 7.6 ± 3.8*, # |
α1(W245L)β2γ2L | 0.9 ± 0.1#, ** | 1.0 ± 0.1 #,** |
The data give the mean (±S.D.) effect of 20 μM ent-9 or ent-7 on peak currents elicited by GABA at a concentration (5 μM for wild-type; 10 μM for mutants) producing 11-17% of maximal current. Number of cells was 4-7 at each receptor-compound combination. Receptors were expressed in HEK 293 cells. Statistical analysis applies to comparison with no effect (using paired two-sample t-test) and comparison with potentiation observed at the wild-type receptor (ANOVA with Bonferroni post-hoc correction). (
, not significant;
, p<0.05;
, p<0.01)