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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
Technical Data for Flumazenil
|Storage||Store at +4°C|
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.
|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|
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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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
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
Brodnik et al (2018) Local GABAA receptor mediated suppression of DA release within the nucleus accumbens. ACS Chem Neurosci 17 1978 PMID: 30253088
Zhu (2018) Structure of a human synaptic GABAA receptor. Nature 559 67 PMID: 29950726
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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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.
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
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
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.
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 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.
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 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.