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Description
Overview
A competitive blocker of benzodiazepine activation of inhibitory GABAergic synpases (ID50 = 200 µg/kg/i.p). Binds to the benzodiazepine site of GABAA receptors. Enhances GABAA-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.
Catalogue Number
505991
Brand Family
Calbiochem®
Synonyms
GABAA Receptor Antagonist, Flumazenil, Ro 15-1788
References
References
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.
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.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
12-September-2013 JSW
Synonyms
GABAA Receptor Antagonist, Flumazenil, Ro 15-1788
Description
A competitive blocker of benzodiazepine activation of inhibitory GABAergic synpases (ID50 = 200 mg/kg/i.p). Binds to the benzodiazepine site of GABAA receptors. Enhances GABAA-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.
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
78755-81-4
Chemical formula
C₁₅H₁₄FN₃O₃
Structure formula
Purity
≥99% by HPLC
Solubility
DMSO (25 mM). Slight warming is required for complete solubilization.
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.