Formulation: A solid
Formal Name: 8-bromo-11,12,13,13aS-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid, 1,1-dimethylethyl ester
Purity: ≥98%
Formula Markup: C19H20BrN3O3
Formula Weight: 418,3
Shelf life (days): 1460
CAS Number: 84379-13-5
Notes: Bretazenil is a positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity.{48491} It 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).{48491} Bretazenil inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM).{48492} It inhibits tonic convulsions induced by pentylenetetrazol (PTZ; Item No. 18682) and maximal electroshock (MES) in rats (ED50s = 0.07 and 0.48 mg/kg, respectively). Bretazenil (5-30 mg/kg) increases the number of open arm entries and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.{48493}
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