Bretazenil

A positive allosteric modulator of GABAA receptors

Bretazenil is a positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity.1 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).1 Bretazenil inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM).2 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.3

418.3

≥98%

Ro 16-6028

BrC1=CC=CC(N2C([C@@]3([H])N4CCC3)=C(C(OC(C)(C)C)=O)N=C2)=C1C4=O

C19H20BrN3O3

84379-13-5

≥ 4 years

DMF: 30 mg/ml DMSO: 30 mg/ml Ethanol: 20 mg/ml PBS (pH 7.2): Partially soluble