Flumazenil

For research use only.

Catalog No.S1332 Synonyms: RO 15-1788

2 publications

Flumazenil Chemical Structure

Molecular Weight(MW): 303.29

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

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 67 In stock
USD 97 In stock
USD 227 In stock
USD 590 In stock
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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
in solvent
Synonyms RO 15-1788
Smiles CCOC(=O)C1=C2CN(C)C(=O)C3=CC(=CC=C3[N]2C=N1)F

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03825601 Not yet recruiting Diagnostic Test: PET with [11C]Flumazenil Multiple Sclerosis|Relapsing-Remitting Multiple Sclerosis Institut National de la Santé Et de la Recherche Médicale France February 1 2019 Not Applicable
NCT03440112 Recruiting Drug: Flumazenil|Drug: Placebo Parkinson Disease Nicolaas Bohnen MD PhD|National Institute of Neurological Disorders and Stroke (NINDS)|University of Michigan January 29 2018 Phase 1|Phase 2
NCT04308954 Recruiting Drug: [18F]flumazenil Fragile X Syndrome (FXS)|Idiopathic Intellectual Developmental Disorder (IDD) Stanford University November 1 2016 Phase 1
NCT02048969 Withdrawn Drug: Flumazenil|Drug: Placebo Hepatic Encephalopathy|Liver Cirrhosis Yale University June 2014 Phase 1|Phase 2
NCT01904487 Completed Radiation: [11C]flumazenil|Drug: Tiagabine Alcoholism Rajesh Narendran|University of Pittsburgh April 19 2011 Phase 1

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