Conditionnement : 1mLx10mM(inDMSO)
Synonyms: Ro 15-1788
| Description | 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. |
| 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 |
| Smiles | CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(F)ccc-21 |
| Relative Density. | 1.39 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 20.625 mg/mL (68 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.59 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
|---|
