Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Flumazenil (Flumazepil, Anexate, Romazicon, Lanexat; Ro-15-1788; Ro-15 1788) is a specific and competitive GABAA receptor antagonist that has been used for 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.
ln Vivo |
The behavioral, neurological, and electrophysiological effects of benzodiazepine agonists and inverse agonists are neutralized or reversed by flumazenil through its interaction with central benzodiazepine receptors. Hepatic encephalopathy can benefit from flumazenil in certain cases, however until well planned clinical trials can be carried out, hepatic encephalopathy must be treated as an exploratory indication. Although flumazenil can restore the drowsiness brought on by benzodiazepines either by alone or in conjunction with other medications, it shouldn't be taken if cyclic antidepressant toxicity is suspected [1]. In the raised plus maze and light/dark test, flumazenil (1 mg/kg) significantly reduces anxiety in BALB/c mice [2]. In rats, the decrease in allopregnanolone can be successfully stopped by flumazenil (10 mg/kg) [3]. In mice, the anticonvulsant and side effects of diazepam are countered by flumazenil (5–20 mg/kg), but not by GYKI 52466. The anticonvulsant activity of NBQX was somewhat diminished by flumazenil in the MES model, but not in the PTZ trial [4]. Reduced open-arm time and open-arm entry percentage are the outcomes of long-term ethanol treatment because flumazenil (3.0 mg/kg) inhibits withdrawal alterations [5].
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References |
[1]. Hoffman EJ, et al. Flumazenil: a benzodiazepine antagonist. Clin Pharm. 1993 Sep;12(9):641-56; quiz 699-701
[2]. Belzung C, et al. Flumazenil induces benzodiazepine partial agonist-like effects in BALB/c but not C57BL/6 mice. Psychopharmacology (Berl). 2000 Jan;148(1):24-32. [3]. Fernandez-Guasti A, et al. Flumazenil blocks the anxiolytic action of allopregnanolone. Eur J Pharmacol. 1995 Jul 25;281(1):113-5. [4]. Loscher W, et al. Effects of the non-NMDA antagonists NBQX and the 2,3-benzodiazepine GYKI 52466 on different seizure types in mice: comparison with diazepam and interactions with flumazenil. Br J Pharmacol. 1994 Dec;113(4):1349-57. [5]. Moy SS, et al. Flumazenil blockade of anxiety following ethanol withdrawal in rats. Psychopharmacology (Berl). 1997 Jun;131(4):354-60 |
Molecular Formula |
C15H14FN3O3
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Molecular Weight |
303.29
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CAS # |
78755-81-4
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Related CAS # |
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SMILES |
FC1C([H])=C([H])C2=C(C=1[H])C(N(C([H])([H])[H])C([H])([H])C1=C(C(=O)OC([H])([H])C([H])([H])[H])N=C([H])N12)=O
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InChi Key |
OFBIFZUFASYYRE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3
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Chemical Name |
ethyl 8-fluoro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2972 mL | 16.4859 mL | 32.9717 mL | |
5 mM | 0.6594 mL | 3.2972 mL | 6.5943 mL | |
10 mM | 0.3297 mL | 1.6486 mL | 3.2972 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.