Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA A receptor antagonist, which negatively modulates the action of GABA on GABA A receptors. Picrotoxinin inhibits α 1 β 2 γ 2L GABA A receptor with an IC 50 of 1.15 μM.
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