Flumazenil

Flumazenil is a GABAA receptor antagonist (IC50 = 2 nM in a radioligand binding assay using rat cortical synaptosomes). Flumazenil also acts as a partial agonist of GABAA receptors, decreasing the amplitude of electrically stimulated population spikes in rat hippocampal CA1 pyramidal neurons. It increases the number of entries into the open arms of the elevated plus maze in high-anxiety BALB/c, but not C57BL/6, mice when administered at doses ranging from 0.1 to 1,000 µg/kg. Flumazenil (5 and 10 mg/kg) prevents a reduction in burying behavior induced by the GABAA receptor positive allosteric modulator allopregnanolone (Cay-16930) in ovariectomized rats when administered at doses of 5 and 10 mg/kg. Formulations containing flumazenil have been used to reverse sedation induced by benzodiazepines and in the treatment of benzodiazepine overdose or withdrawal.Formal Name: 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, ethyl ester. CAS Number: 78755-81-4. Synonyms: Ro 1722, Ro 15-1788, Ro 41-8157. Molecular Formula: C15H14FN3O3. Formula Weight: 303.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 11 mg/ml, DMSO: 16 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 244 nm. SMILES: O=C(OCC)C1=C2CN(C)C(C(C=C(F)C=C3)=C3N2C=N1)=O. InChi Code: InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3. InChi Key: OFBIFZUFASYYRE-UHFFFAOYSA-N.