5.05991

Flumazenil

• Sinonimo/i: Flumazenil, GABA _A Receptor Antagonist, Flumazenil, Ro 15-1788, GABA_A Receptor Antagonist, Flumazenil, Ro 15-1788
• Formula empirica (notazione di Hill): C₁₅H₁₄FN₃O₃
• Numero CAS: 78755-81-4
• Peso molecolare: 303.29
• Numero MDL: MFCD00242764
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥99% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 25 mM
• Temperatura di conservazione: 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; OFBIFZUFASYYRE-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Primary Target
GABA_A

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Nota sulla preparazione

Slight warming is required for complete solubilization.

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable