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Flumazenil

Catalog No. T1240 CAS 78755-81-4

Synonyms: Ro 15-1788

Flumazenil (Ro 15-1788) antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. Flumazenil is an imidazobenzodiazepine derivative, effective in reversing benzodiazepine-induced activities.

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Flumazenil, CAS 78755-81-4

Pack Size	Availability	Price/USD
10 mg	In stock	$ 43.00
25 mg	In stock	$ 72.00
50 mg	In stock	$ 108.00
100 mg	In stock	$ 147.00
500 mg	In stock	$ 363.00
1 mL * 10 mM (in DMSO)	In stock	$ 30.00

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Purity: 100%

Purity: 99.91%

Biological Description

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Description

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.

Synonyms	Ro 15-1788
Molecular Weight	303.29
Formula	C15H14FN3O3
CAS No.	78755-81-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (16.48 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Hoffman EJ, et al. Clin Pharm, 1993, 12(9), 641-656. 2. Belzung C, et al. Psychopharmacology (Berl), 2000, 148(1), 24-32. 3. Fernández-Guasti A, et al. Eur J Pharmacol. 1995 Jul 25;281(1):113-5. 4. Löscher W,et al. Br J Pharmacol. 1994 Dec;113(4):1349-57. 5. Moy SS, et al. Psychopharmacology (Berl), 1997, 131(4), 354-360.

Citations

1. Ekiciler A, Chen W L K, Bo Y, et al.Quantitative Cytochrome P450 3A4 Induction Risk Assessment Using Human Hepatocytes Complemented with Pregnane X Receptor-Activating Profiles.Drug Metabolism and Disposition.2023, 51(3): 276-284.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Compound Library FDA-Approved Drug Library ReFRAME Related Library

Related Products

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(E)-GABAB receptor antagonist 1 Dihydroxyaflavinine Oxiracetam Tetrahydromagnolol NEO 376 Vigabatrin Hydrochloride α-Thujone γ-Acetylenic GABA hydrochloride

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Keywords

Flumazenil 78755-81-4 Membrane transporter/Ion channel Neuroscience GABA Receptor Ro 15-1788 inhibit Inhibitor γ-Aminobutyric acid Receptor Gamma-aminobutyric acid Receptor inhibitor

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