Flumazenil

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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 (5)
Reviews
Literature

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 Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 303.29
Formula C15H14FN3O3
Storage Desiccate 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solubility Soluble to 25 mM in DMSO and to 5 mM in ethanol with gentle warming

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.3 mL 16.49 mL 32.97 mL
5 mM 0.66 mL 3.3 mL 6.59 mL
10 mM 0.33 mL 1.65 mL 3.3 mL
50 mM 0.07 mL 0.33 mL 0.66 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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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

5 Citations for Flumazenil

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

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

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

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


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