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 CAS: 78755-81-4
• Peso molecular: 303.29
• MDL number: MFCD00242764
• UNSPSC Code: 12352200
• NACRES: NA.77

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
• SMILES string: Fc1cc2c(cc1)[n]3c(c(nc3)C(=O)OCC)CN(C2=O)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.

Biochem/physiol Actions

Primary Target
GABA_A

Packaging

Packaged under inert gas

Preparation Note

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

Slight warming is required for complete solubilization.

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

Disclaimer

Toxicity: Standard Handling (A)

Información de seguridad

• Clase de almacenamiento: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable