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SR-95531 C화학적 특성, 용도, 생산
개요
SR 95531 is a derivative of γ-aminobutyric acid (GABA) that acts as an antagonist of GABAA receptors (Ki = 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 GABAA receptor isoforms from mice, rats, and humans.
용도
Gabazine Hydrobromide is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites.
생물학적 활성
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.
