5.05991

Flumazenil

• Sinônimo(s): Flumazenil, GABA _A Receptor Antagonist, Flumazenil, Ro 15-1788, GABA_A Receptor Antagonist, Flumazenil, Ro 15-1788
• Fórmula empírica (Notação de Hill): C₁₅H₁₄FN₃O₃
• Número CAS: 78755-81-4
• Peso molecular: 303.29
• Número MDL: MFCD00242764
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥99% (HPLC)
• Nível de qualidade: 100
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 25 mM
• temperatura de armazenamento: 2-8°C
• 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
• chave InChI: OFBIFZUFASYYRE-UHFFFAOYSA-N

Descrição

Descrição geral

A competitive blocker of benzodiazepine activation of inhibitory GABAergic synpases (ID50 = 200 µg/kg/i.p). Binds to the benzodiazepine site of GABA_A receptors. Enhances GABA_A-receptor mediated currents and antagonizes the enhancing effects of benzodiapine agonist flurazepam. Exhibits fast association and dissociation from the benzodiazepine binding site. Permeates the blood brain barrier, however, the level of uptake may depend on efflux effects of p-glycogprotein transporter.

A competitive blocker of benzodiazepine activation of inhibitory GABAergic synpases (ID50 = 200 mg/kg/i.p). Binds to the benzodiazepine site of GABA_A receptors. Enhances GABA_A-receptor mediated currents and antagonizes the enhancing effects of benzodiapine agonist flurazepam. Exhibits fast association and dissociation from the benzodiazepine binding site. Permeates the blood brain barrier, however, the level of uptake may depend on efflux effects of p-glycogprotein transporter.

Ações bioquímicas/fisiológicas

Primary Target
GABA_A

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Nota de preparo

Slight warming is required for complete solubilization.

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Froklage, F.E., et al. 2012. EJNMMI Research.2, 12.
Li, J., et al. 2006. Neuropharmacol.51, 168.
Weiss, M., et al. 2002. Neurochem. Res.27, 1605.
Atack, J., et al. 1999. Neuropsychopharmacol.20, 255.
Votey, S.R., et al. 1991. Ann. Emerg. Med.20, 181.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable