Bretazenil

Bretazenil is a positive allosteric modulator of GABA_A 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 GABA_A 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

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1. Puia, G., Dučič, I., Vicini, S., et al. Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at γ-aminobutyric acid type A receptor. Proc. Natl. Acad. Sci. USA 89(8), 3620-3624 (1992).

2. Martin, J.R., Pieri, L., Bonetti, E.P., et al. Ro 16-6028: A novel anxiolytic acting as a partial agonist at the benzodiazepine receptor. Pharmacopsychiatry 21(6), 360-362 (1988).

3. Cole, J.C., and Rodgers, R.J. An ethological analysis of the effects of chlordiazepoxide and bretazenil (Ro 16-6028) in the murine elevated plus-maze. Behav. Pharmacol. 4(6), 573-580 (1993).