Flumazenil

For research use only. Not for therapeutic Use.

  • CAT Number: A000422
  • CAS Number: 78755-81-4
  • Molecular Formula: C15H14FN3O3
  • Molecular Weight: 303.30
  • Purity: ≥95%
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Flumazenil (Cat No.: A000422) is a benzodiazepine antagonist used to reverse the sedative effects of benzodiazepines during anesthesia or in cases of overdose. It works by competitively inhibiting benzodiazepine binding at the GABA-A receptor, rapidly restoring consciousness and respiratory function. Administered intravenously, flumazenil acts within minutes but has a short duration, often requiring repeated dosing. Side effects may include nausea, dizziness, agitation, or seizures, particularly in patients with long-term benzodiazepine use or mixed drug overdoses. It is used with caution in such cases.


CAS Number 78755-81-4
Synonyms

78755-81-4; Anexate; Flumazepil; Romazicon; Lanexat

Molecular Formula C15H14FN3O3
Purity ≥95%
Target Neuronal Signaling
Solubility Limited solubility
Storage -20°C
Overview of Clinical Research

Flumazenil is a&nbsp;<span style=”font-family:arial,helvetica,sans-serif;”><span style=”font-size:12px;”><span style=”font-variant-ligatures: normal; orphans: 2; widows: 2;”>GABA-A receptor antagonist used as antidote for&nbsp;benzodiazepine overdoses.&nbsp;</span><span style=”font-variant-ligatures: normal; orphans: 2; widows: 2;”>Coeruleus has patents pending for flumazenil in world including Japan in 2020.</span></span></span>

IUPAC Name ethyl 8-fluoro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
InChI InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3
InChIKey OFBIFZUFASYYRE-UHFFFAOYSA-N
SMILES CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)F)C
Reference

1: Bernik M, Ramos RT, Hetem LAB, Graeff F. Effect of single doses of pindolol and d-fenfluramine on flumazenil-induced anxiety in panic disorder patients. Behav Brain Res. 2017 Nov 4. pii: S0166-4328(17)30453-9. doi: 10.1016/j.bbr.2017.11.002. [Epub ahead of print] PubMed PMID: 29113874.<br />
2: Goh ET, Andersen ML, Morgan MY, Gluud LL. Flumazenil versus placebo or no intervention for people with cirrhosis and hepatic encephalopathy. Cochrane Database Syst Rev. 2017 Aug 10;8:CD002798. doi: 10.1002/14651858.CD002798.pub4. Review. PubMed PMID: 28796283.<br />
3: Goh ET, Andersen ML, Morgan MY, Gluud LL. Flumazenil versus placebo or no intervention for people with cirrhosis and hepatic encephalopathy. Cochrane Database Syst Rev. 2017 Jul 26;7:CD002798. doi: 10.1002/14651858.CD002798.pub3. Review. Update in: Cochrane Database Syst Rev. 2017 Aug 10;8:CD002798. PubMed PMID: 28745801.<br />
4: Parthvi R, Mehra S. Flumazenil for Mixed Drug Overdose. Am J Ther. 2017 Jul 6. doi: 10.1097/MJT.0000000000000620. [Epub ahead of print] PubMed PMID: 28708699.<br />
5: Lopes Alves I, V&aacute;llez Garc&iacute;a DV, Parente A, Doorduin J, da Silva AMM, Koole M, Dierckx R, Willemsen A, Boellaard R. Parametric Imaging of [(11)C]Flumazenil Binding in the Rat Brain. Mol Imaging Biol. 2017 Jun 19. doi: 10.1007/s11307-017-1098-2. [Epub ahead of print] PubMed PMID: 28631142.<br />
6: Tamburin S, Faccini M, Casari R, Federico A, Morbioli L, Franchini E, Bongiovanni LG, Lugoboni F. Low risk of seizures with slow flumazenil infusion and routine anticonvulsant prophylaxis for high-dose benzodiazepine dependence. J Psychopharmacol. 2017 Oct;31(10):1369-1373. doi: 10.1177/0269881117714050. Epub 2017 Jun 14. PubMed PMID: 28613124.<br />
7: Ishibashi K, Miura Y, Matsumura K, Kanemasa Y, Nakamichi K, Saijo M, Toyohara J, Ishii K. PET Imaging of (18)F-FDG, (11)C-methionine, (11)C-flumazenil, and (11)C-4DST in Progressive Multifocal Leukoencephalopathy. Intern Med. 2017;56(10):1219-1223. doi: 10.2169/internalmedicine.56.8080. Epub 2017 May 15. PubMed PMID: 28502940; PubMed Central PMCID: PMC5491820.<br />
8: Cimolai N. Zopiclone overdose and flumazenil rescue. CMAJ. 2017 Apr 24;189(16):E613. doi: 10.1503/cmaj.732933. PubMed PMID: 28438958; PubMed Central PMCID: PMC5403648.<br />
9: Wallace IR, Campbell EC, Trimble M. Use of a flumazenil infusion to treat chlordiazepoxide toxicity. Acute Med. 2017;16(1):30-34. PubMed PMID: 28424803.<br />
10: Parente A, V&aacute;llez Garc&iacute;a D, Shoji A, Lopes Alves I, Maas B, Zijlma R, Dierckx RA, Buchpiguel CA, de Vries EF, Doorduin J. Contribution of neuroinflammation to changes in [(11)C]flumazenil binding in the rat brain: Evaluation of the inflamed pons as reference tissue. Nucl Med Biol. 2017 Jun;49:50-56. doi: 10.1016/j.nucmedbio.2017.03.001. Epub 2017 Mar 18. PubMed PMID: 28364664.

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