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Flumazenil

Name: Flumazenil
Brand: Selleck Chemicals
SKU: S1332
Rating: 5 (3 reviews)

Synonyms: RO 15-1788

Catalog No.S1332 Purity:99.98%

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

Flumazenil Chemical Structure

CAS No. 78755-81-4

Purity & Quality Control

Batch: Purity: 99.98%

99.98

Flumazenil Related Products

Related Targets	GABAA receptor GABAB receptor	Click to Expand
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Signaling Pathway

GABA Receptor Signaling Pathway

Biological Activity

Description

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

Targets

GABAA receptor ^[1]

In Vivo
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06275594	Not yet recruiting	Midazolam\|Remimazolam	Yeungnam University Hospital	March 1 2024	Phase 2
NCT05939674	Recruiting	Flumazenil Adverse Reaction\|Remimazolam\|Hip Joint\|Elderly Patients	Pusan National University Yangsan Hospital	September 19 2023	Not Applicable
NCT05841667	Recruiting	Adult\|Middle Aged\|Elective Surgical Procedures	Korea University Guro Hospital	September 6 2023	--
NCT05220462	Recruiting	Tooth Extraction	Guy''s and St Thomas'' NHS Foundation Trust	March 9 2022	Phase 3
NCT05025410	Completed	Myoma;Uterus\|Polyp Endometrium\|Unspecified Condition Associated With Female Genital Organs and Menstrual Cycle	Seoul National University Bundang Hospital	November 1 2021	--

References

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Chemical Information & Solubility

Molecular Weight	303.29	Formula	C₁₅H₁₄FN₃O₃
CAS No.	78755-81-4	SDF	Download Flumazenil SDF
Smiles	CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)F)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 9 mg/mL ( (29.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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