Flumazenil

SKU: orb1309273

Description

Flumazenil is a competitive antagonist at the central benzodiazepine receptor site on the GABA-A complex. It effectively reverses sedative, amnesic, and respiratory depressant effects of benzodiazepines in research settings, making it a valuable tool for in vivo and in vitro neuropharmacology studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 78755-81-4
• MW: 303.29
• Purity: >99.99% (May vary between batches)
• Formula: C₁₅H₁₄FN₃O₃
• SMILES: CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(F)ccc-21
• Target: GABA Receptor
• Solubility: DMSO:20.625 mg/mL (68 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.59 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vitro:
  Flumazenil (1 mg/kg) demonstrated significant anxiolytic effects in BALB/c mice during elevated plus-maze and light/dark box tests. At a dose of 3 mg/kg, Flumazenil prevented changes induced by chronic ethanol withdrawal in mice, observed as decreased open arm time and the percentage of open arm entries. In rats, Flumazenil (10 mg/kg) effectively counteracted the sedative action produced by tetrahydroprogesterone. Additionally, Flumazenil antagonized the effects of diazepam in mice at doses ranging from 5-20 mg/kg, yet showed no effect on the anticonvulsant and adverse reactions associated with GYKI52466. While minimally decreasing the anticonvulsant activity of NBQX in the MES model and not in the PTZ test, Flumazenil binds to central benzodiazepine (BZD) receptors, thus antagonizing or reversing the neuropsychological and electrophysiological effects of BZD inverse agonists and agonists. Flumazenil can reverse sedative toxic reactions caused by the combined use of BZDs and other drugs, but it is ineffective in the case of cyclic antidepressant overdose.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, GABAReceptor, GABAR, Gamma-aminobutyric acid Receptor, GABA Receptor, Flumazenil, inhibit, Ro 15-1788, γ-Aminobutyric acid Receptor

Compound Identifiers

PubChem CID

3373