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Description: Benzodiazepine antagonist
Alternative Names: Ro 15-1788
Chemical Name: 8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, ethyl ester
Purity: ≥99% (HPLC)
Citations (7)
Reviews (2)
Literature (2)

Biological Activity for Flumazenil

Flumazenil is a benzodiazepine antagonist, non-selective for α1, α2, α3 or α5-containing GABAA receptors. Centrally active upon systemic administration in vivo. Also inhibits repressor element-1 silencing transcription factor (REST) by targeting degradation.

Compound Libraries for Flumazenil

Flumazenil is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Flumazenil

M. Wt 303.29
Formula C15H14FN3O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 78755-81-4
PubChem ID 3373
Smiles CCOC(=O)C1=C2CN(C)C(=O)C3=CC(F)=CC=C3N2C=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Flumazenil

Solvent Max Conc. mg/mL Max Conc. mM

Preparing Stock Solutions for Flumazenil

The following data is based on the product molecular weight 303.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 13.19 mL 65.94 mL 131.89 mL
1.25 mM 2.64 mL 13.19 mL 26.38 mL
2.5 mM 1.32 mL 6.59 mL 13.19 mL
12.5 mM 0.26 mL 1.32 mL 2.64 mL

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Product Datasheets for Flumazenil

Certificate of Analysis / Product Datasheet
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References for Flumazenil

References are publications that support the biological activity of the product.

Atack et al (1999) Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for α1 versus α2 and α3 subunit-containing GABAA receptors. Neuropsychopharmacology 20 255 PMID: 10063485

Dobl (1999) New insights into the mechanism of action of hypnotics. J.Psychopharmacol. 13 S11 PMID: 10667451

Polc et al (1981) Electrophysiological studies on the specific benzodiazepine antagonist Ro 15-1788. Naunyn Schmiedebergs Arch.Pharmacol. 316 317 PMID: 7196507

If you know of a relevant reference for Flumazenil, please let us know.

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View all GABAA Receptor Benzodiazepines

Keywords: Flumazenil, Flumazenil supplier, Benzodiazepine, antagonists, GABAA, Receptors, Ro151788, repressor, element-1, silencing, transcription, factor, REST, inhibitors, inhibits, Ro, 15-1788, Other, Transcription, Factors, 1328, Tocris Bioscience

7 Citations for Flumazenil

Citations are publications that use Tocris products. Selected citations for Flumazenil include:

Heidelberg et al (2013) SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with β3 and γ2 subunits. J Pharmacol Exp Ther 347 235 PMID: 23902941

Leppä et al (2011) Removal of GABA(A) receptor γ2 subunits from parvalbumin neurons causes wide-ranging behavioral alterations. PLoS One 6 e24159 PMID: 21912668

Linden et al (2011) Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci 5 3 PMID: 21270945

Carlile et al (2012) An anxiolytic-like effect of hyperbaric oxygen in the mouse light/dark exploration test. Life Sci 90 267 PMID: 22154905

Do you know of a great paper that uses Flumazenil from Tocris? Please let us know.

Reviews for Flumazenil

Average Rating: 5 (Based on 2 Reviews.)

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Antagonism of Flumazenil to effects of Phenazepam.
By Anonymous on 04/14/2020
Assay Type: In Vitro
Species: Other

Flumazenil (FMZ) was used to block action of other benzodiazepine ligand of GABA-A receptor (Phenazepam, PNZ) on decay kinetics of spontaneous inhibitory currents recorded from brain neurons of Prussian carp (Carassius gibelio). FMZ demonstrated competitive antagonism to PNZ in this research, both in vivo (behavioral tests) and in vitro (whole-cell voltage-clamp recordings, see example illustration).

Soluble in DMSO, but requires sonication.

PMID: 29191862
review image

Flumazenil and in vivo chloride signals.
By Anonymous on 05/23/2019
Assay Type: In Vivo
Species: Mouse

used with fiber photometry to validate a chloride sensor in vivo. response to footshock was measured at baseline and then at 15 min intervals post injection

injected 15mg/kg i.p at a concentration of.8mg/ml in 5% DMSO in saline

review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

GABA Receptors Scientific Review

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.