Flumazenil, GABAA receptor antagonist

Product Details

Formal Name: 8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, ethyl ester

Alternate Names: Ro 1722; Ro 15-1788

Molecular Formula: C₁₅H₁₄FN₃O₃

Formula Weight: 303.30

CAS Number: 78755-81-4

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 8 mg/ml).

Storage: -20°C

Stability: ≥ 2 years.

Applications

GABAA receptor antagonist

Functions

GABAA receptor, and benzodiazepine, antagonist (radioligand binding assay in rat cortical synaptosomes, IC50 = 2 nM. Panspecific for α1, α2, α3, or α5-containing GABAA receptors. When used at 10 µM in HEK-293 cells, flumazenil reduces α4β2δ GABAA receptor at the cell surface, likely through an increase in its endocytosis and lysosomal degradation. Used to study GABAA signaling, and develop new benzodiazepines. Reduces withdrawal sequelae in benzodiazepine dependence. Reverses the toxic effects, including coma and respiratory depression of zolpidem intoxication4 and gabapentin-induced coma.

Application Procedures

First dissolved in DMSO (up to 8 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)