Flumazenil (RO 15-1788)

Catalog No.S1332

For research use only.

Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

Flumazenil (RO 15-1788) Chemical Structure

CAS No. 78755-81-4

Selleck's Flumazenil (RO 15-1788) has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Flumazenil (RO 15-1788) 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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 303.29
Formula

C15H14FN3O3

CAS No. 78755-81-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)F)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05025410 Recruiting Drug: Remimazolam Myoma;Uterus|Polyp Endometrium|Unspecified Condition Associated With Female Genital Organs and Menstrual Cycle Seoul National University Bundang Hospital September 1 2021 --
NCT03825601 Unknown status 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
NCT04308954 Terminated 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|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) June 2014 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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