Bretazenil

A positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity; potentiates GABA-gated chloride currents in rat cortical neurons and in HEK293 cells expressing α1β1γ2 subunit-containing GABAA receptors (EC50s = 60 and 10 nM, respectively); inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM); inhibits PTZ- and MES-induced tonic convulsions in rats (ED50s = 0.07 and 0.48 mg/kg, respectively); increases the number of open arm entries and percentage of time spent in the open arms of the elevated plus maze in mice at 5-30 mg/kg