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Cat. No. Name Size Price Add Cart
KI0941Flumazenil25 mg$154
Flumazenil500 mg$752

Chemical Characteristic

Product NameFlumazenil
SynonymsRo 15-1788
CAS No.78755-81-4
Molecular Weight 303.29
FormulaC15H14FN3O3
Chemical NameEthyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Smilesn12c(CN(C(=O)c3c1ccc(c3)F)C)c(nc2)C(=O)OCC
Chemical Structure

Biological activities

Flumazenil is a specific benzodiazepine antagonist. Transfected with α1β2γ2S subunits of GABAA receptors to flumazenil (in the presence of 1 µM GABA) can enhance the maximum number of [3H]TBOB binding sites, without affecting their affinity. Besides, the IC50 of flumazenil is 87.1 nM and 71.3 µM for high and low affinity (IC50H, IC50L), respectively.[1] Flumazenil is used acutely to reverse the adverse effects of excessive sedation with benzodiazepines, and also used for the chronic treatment of hepatic encephalopathy. Chronic exposure of HEK 293 cells to flumazenil enhances basal [3H]flunitrazepam binding. [2] After chronic (14 days) flumazenil treatment can increase the binding of convulsant TBPS in cerebral cortex of rat. The chronic flumazenil treatment increases the specific [3H]flunitrazepam binding in cerebral cortex of rat.[2]

Protocols

Flumazenil is dissolved in ethanol at the 1 mM concentration.[2]

References

[1] Pericic D, et al. Chronic treatment with flumazenil enhances binding sites for convulsants at recombinant 122S GABAA receptors. Biomed Pharmacother. 2005, 59 (7): 408-414.
[2] Pericic D, et al. Chronic exposure of cells expressing recombinant GABAA receptors to benzodiazepine antagonist flumazenil enhances the maximum number of benzodiazepine binding sites. Life Sci. 2004, 76(3): 303-317.

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