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. Author manuscript; available in PMC: 2015 Jan 9.
Published in final edited form as: J Med Chem. 2013 Dec 24;57(1):171–190. doi: 10.1021/jm401577c

Table 3.

Modulation of Rat Wild-Type and Mutant α1β2γ2L GABAA Receptor Function by Steroid Enantiomers ent-9 and ent-7a

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 #,**
a

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)