Flumazenil

Catalog No.S1332 Synonyms: RO 15-1788

Flumazenil Chemical Structure

Molecular Weight(MW): 303.29

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

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Biological Activity

Description Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Targets
GABAA receptor [1]
In vivo Flumazenil interacts at the central benzodiazepine receptor to antagonize or reverse the behavioral, neurologic, and electrophysiologic effects of benzodiazepine agonists and inverse agonists. Flumazenil is of some benefit in hepatic encephalopathy, but until well-designed clinical trials are conducted, hepatic encephalopathy must be considered an investigational indication for flumazenil. Flumazenil has been shown to reverse sedation caused by intoxication with benzodiazepines alone or benzodiazepines in combination with other agents, but it should not be used when cyclic antidepressant intoxication is suspected. [1] Flumazenil (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test. [2] Flumazenil (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats. [3] Flumazenil (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. Flumazenil slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test. [4] Flumazenil (3.0 mg/kg) blocks the changes withdrawal from chronic ethanol treatment, which leads to a decrease in open arm time and percent open arm entries. [5]

Protocol

Solubility (25°C)

In vitro DMSO 5 mg/mL (16.48 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 303.29
Formula

C15H14FN3O3

CAS No. 78755-81-4
Storage powder
Synonyms RO 15-1788

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02899156 Recruiting Delirium University of California, Davis March 2016 Phase 4
NCT02690389 Completed Acupuncture|General Anaesthesia|Sedation Dr. Yin Liu|Sichuan Cancer Hospital and Research Institute January 2015 --
NCT02048969 Recruiting Hepatic Encephalopathy|Liver Cirrhosis Yale University June 2014 Phase 1|Phase 2
NCT01651520 Recruiting Multiple Sclerosis Assistance Publique - Hôpitaux de Paris March 2013 --
NCT01904487 Terminated Alcoholism Rajesh Narendran|University of Pittsburgh April 2011 Phase 1
NCT02157428 Completed Adverse Effect of Other General Anesthetics University of Sao Paulo January 2011 --

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