Figure 6.

The flavan Fa173 acts as an antagonist of the loreclezole-induced enhancement of GABA currents. (A) Current traces (nA vs. min) illustrating the blockade that increasing concentrations of Fa173 exert over the potentiating action of loreclezole at α1β2γ2L receptors. (B) Current traces (nA vs. min) illustrating the blockade that increasing concentrations of Fa173 exert over the potentiating action of loreclezole at α1β2 receptors. Drug concentrations were 3 µM GABA and 10 µM loreclezole at α1β2γ2L and 1 µM GABA and 10 µM loreclezole at α1β2, equivalent to their corresponding EC₃ and EC₅₀, respectively. Horizontal bars represent drug application. (C) Concentration-response curves for Fa173 blockade of loreclezole-induced potentiation (IC₅₀ = 6.6 ± 0.2 µM and 3.8 ± 0.9 µM, maximal inhibition = 99 ± 11% and 94 ± 4%, n = 7 and 5, at α1β2γ2L and α1β2 receptors, respectively).