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Submit ReviewFlumazenil
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)
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 |
| 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 for Flumazenil
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25 |
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 |
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Product Datasheets for Flumazenil
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:
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
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
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
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.
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
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!
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