Background:

6-methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.

6-methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors. 6-Methylflavone enhances the normal response to GABA at recombinant α1β2γ2L and α1β2 GABAA receptors (P<0.0001) at concentrations from 1 to 100 μM. 6-Methylflavone (60 μM) shifts the GABA dose-response curve to the left (n=4, F=16.38, P=0.0004), decreasing the mean EC50 at α1β2γ2L GABAA receptors by 33±5.4%[1].

[1]. Hall BJ, et al. Flumazenil-independent positive modulation of gamma-aminobutyric acid action by 6-methylflavone at human recombinant alpha1beta2gamma2L and alpha1beta2 GABAA receptors. Eur J Pharmacol. 2004 Apr 26;491(1):1-8.