SR 95531 hydrobromide, Tocris Bioscience™

SR 95531 hydrobromide is a selective, competitive GABAA receptor antagonist and allosteric inhibitor (IC50 = 200 nM). SR 95531 displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM. Unlike Bicuculline (Cat. No. 0130), SR 95531 selectively antagonizes GABA-induced Cl- currents with little action on Pentobarbitone -induced currents (Cat. No. 4579). SR 95531 can act as an agonist at high concentrations (>100 μM) and is a weak agonist at GABAA receptors with α1β2(Y157S)γ2L subunits. SR 95531 also acts as a competitive antagonist of recombinant glycine receptors and exhibits greater potency at glycine receptors containing β subunits.