product name Flumazenil
Description: Flumazenil (also known as RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses. Flumazenil is a specific benzodiazepine receptor antagonist primarily administered by injection. It is the only benzodiazepine receptor antagonist on the market today. Flumazenil is of benefit in patients who become excessively drowsy after benzodiazepines are used for either diagnostic or therapeutic procedures.
References: Clin Pharm. 1993 Sep;12(9):641-56; quiz 699-701; Psychopharmacology (Berl). 2000 Jan;148(1):24-32.
303.29
Formula
C15H14FN3O3
CAS No.
78755-81-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (16.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
RO 15-1788
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19421743
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In vitro activity: Kinase Assay: Cell Assay: |
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| In Vivo | Flumazenil interacts at the central benzodiazepine receptor to antagonize or reverse the behavioral, neurologic, and electrophysiologic effects of benzodiazepine agonists and inverse agonists. Flumazenil is of some benefit in hepatic encephalopathy, but until well-designed clinical trials are conducted, hepatic encephalopathy must be considered an investigational indication for flumazenil. Flumazenil has been shown to reverse sedation caused by intoxication with benzodiazepines alone or benzodiazepines in combination with other agents, but it should not be used when cyclic antidepressant intoxication is suspected. Flumazenil (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test. Flumazenil (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats. Flumazenil (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. Flumazenil slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test. Flumazenil (3.0 mg/kg) blocks the changes withdrawal from chronic ethanol treatment, which leads to a decrease in open arm time and percent open arm entries. |
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| References | Clin Pharm. 1993 Sep;12(9):641-56; quiz 699-701; Psychopharmacology (Berl). 2000 Jan;148(1):24-32; Eur J Pharmacol. 1995 Jul 25;281(1):113-5. |
