5.05991

Flumazenil

• Synonym(e): Flumazenil, GABA _A Receptor Antagonist, Flumazenil, Ro 15-1788, GABA_A Receptor Antagonist, Flumazenil, Ro 15-1788
• Empirische Formel (Hill-System): C₁₅H₁₄FN₃O₃
• CAS-Nummer: 78755-81-4
• Molekulargewicht: 303.29
• MDL-Nummer: MFCD00242764
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥99% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 25 mM
• Lagertemp.: 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
• InChIKey: OFBIFZUFASYYRE-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Primary Target
GABA_A

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Angaben zur Herstellung

Slight warming is required for complete solubilization.

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable