Description
SR 95531 is a derivative of γ-
aminobutyric acid (GABA) that acts as an antagonist of GABA
A receptors (K
i = 74-
150 nM). When administered intravenously, it elicits seizures in mice. SR 95531 differs in action from bicuculline in that it antagonizes GABA-
induced chloride currents but not those induced by pentobarbitone. It is effective against GABA
A receptor isoforms from mice, rats, and humans.
Biological Activity
Selective, competitive GABA A receptor antagonist. Displaces [ 3 H]-GABA from rat brain membranes with a K i of 150 nM. Unlike bicuculline, selectively antagonizes GABA-induced Cl - currents with little action on pentobarbitone-induced currents. Also acts as a low affinity glycine receptor antagonist.
