Flumazenil

Biochem/physiol Actions

Primary TargetGABA_A

General description

A competitive blocker of benzodiazepine activation of inhibitory GABAergic synpases (ID50 = 200 µg/kg/i.p). Binds to the benzodiazepine site of GABA_A receptors. Enhances GABA_A-receptor mediated currents and antagonizes the enhancing effects of benzodiapine agonist flurazepam. Exhibits fast association and dissociation from the benzodiazepine binding site. Permeates the blood brain barrier, however, the level of uptake may depend on efflux effects of p-glycogprotein transporter.

A competitive blocker of benzodiazepine activation of inhibitory GABAergic synpases (ID50 = 200 mg/kg/i.p). Binds to the benzodiazepine site of GABA_A receptors. Enhances GABA_A-receptor mediated currents and antagonizes the enhancing effects of benzodiapine agonist flurazepam. Exhibits fast association and dissociation from the benzodiazepine binding site. Permeates the blood brain barrier, however, the level of uptake may depend on efflux effects of p-glycogprotein transporter.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Froklage, F.E., et al. 2012. EJNMMI Research.2, 12.Li, J., et al. 2006. Neuropharmacol.51, 168. Weiss, M., et al. 2002. Neurochem. Res.27, 1605. Atack, J., et al. 1999. Neuropsychopharmacol.20, 255.Votey, S.R., et al. 1991. Ann. Emerg. Med.20, 181.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Preparation Note

Slight warming is required for complete solubilization.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)