5.05991

Flumazenil

• Sinónimos: Flumazenil, GABA _A Receptor Antagonist, Flumazenil, Ro 15-1788, GABA_A Receptor Antagonist, Flumazenil, Ro 15-1788
• Fórmula empírica (notación de Hill): C₁₅H₁₄FN₃O₃
• Número de CAS: 78755-81-4
• Peso molecular: 303.29
• MDL number: MFCD00242764
• UNSPSC Code: 12352200

Propiedades

• assay: ≥99% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 25 mM
• storage temp.: 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
• InChI key: OFBIFZUFASYYRE-UHFFFAOYSA-N

Descripción

General description

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.

Biochem/physiol Actions

Primary Target
GABA_A

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Preparation Note

Slight warming is required for complete solubilization.

Reconstitution

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

Other Notes

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.

Legal Information

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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable