Flumazenil

Pricing Availability   Qty
Cat.No. 1328 - Flumazenil | C15H14FN3O3 | CAS No. 78755-81-4
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)
Datasheet
Citations (7)
Reviews (2)
Literature (7)

Biological Activity

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

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

M. Wt 303.29
Formula C15H14FN3O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 78755-81-4
PubChem ID 3373
InChI Key OFBIFZUFASYYRE-UHFFFAOYSA-N
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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25

Preparing Stock Solutions

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:

References

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.

View Related Products by Product Action

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

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

Joensuu et al (2014) Gene expression alterations in the cerebellum and granule neurons of Cstb(-/-) mouse are associated with early synaptic changes and inflammation. PLoS One 9 e89321 PMID: 24586687

Brodnik et al (2018) Local GABAA receptor mediated suppression of DA release within the nucleus accumbens. ACS Chem Neurosci 17 1978 PMID: 30253088


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.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%

Have you used Flumazenil?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


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.


Ion Channel

Ion Channel Product Listing

A collection of around 500 products for ion channel research, the listing includes research tools for the study of:

  • Ligand-gated ion channels
  • Voltage-gated ion channels
  • Other Ion Channels
Pain

Pain Research Product Guide

A collection of over 280 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
GABA Receptors

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

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.

Epilepsy

Epilepsy Poster

Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Schizophrenia

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.