| Name | Flupirtine maleate |
| Description | Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener. |
| Cell Research | For measurement of viability and generation of reactive oxygen intermediates, PC12 cells are seeded in 24- or 96-well plates coated with poly-L-lysine at 105 cells/mL. Drugs are dissolved in PBS (pH 7.4), or ethanol and filtered sterile. At the end of each experiment cells are trypsinized and pelleted together with cells of the culture supernatant. After staining for 10 min with 0.2% Trypan blue solution live (unstained) and dead (Trypan blue positive) cells are counted in a hemocytometer chamber. In addition, cellular viability is evaluated by the reduction of MTT to formazan. After 2 hours incubation with MTT (0.5 mg/ml) at 37 °C, cells are lysed in DMSO. Extinction at 570 nm is determined on a plate photometer. For staining of surviving adherent cells, plates are incubated for 10 min with 0.5% crystalviolet dissolved in 20% methanol. Plates are rinsed with water and stained cells are lysed in 50% ethanol, 0.1 M sodiumcitrate before determining extinction at 550 nm. (Only for Reference) |
| In vitro | Flupirtine was able to block NMDA and gp120 HIV-1-induced cell death in rat cortical neurons.Flupirtine at concentrations of 1 μM and 10 μM reduced TRAIL-regulated death of human living brain tissue in culture; a concentration of 10 μM in 10 mM L-glutamic acid-treated PC 12 cultures significantly reduced non-receptor- regulated necrotic cell death; a concentration of 1 or 5 μg/mL blocked β-amyloid (25-35)-induced apoptosis by acting on primary neuronal cells; and a concentration of 1-10 mM protected primary neuronal cells from monosodium glutamate-induced toxicity by lowering calcium ion concentration. |
| In vivo | Flupirtine was able to block NMDA and gp120 HIV-1-induced cell death in rat cortical neurons.Flupirtine at concentrations of 1 μM and 10 μM reduced TRAIL-regulated death of human living brain tissue in culture; a concentration of 10 μM in 10 mM L-glutamic acid-treated PC 12 cultures significantly reduced non-receptor- regulated necrotic cell death; a concentration of 1 or 5 μg/mL blocked β-amyloid (25-35)-induced apoptosis by acting on primary neuronal cells; and a concentration of 1-10 mM protected primary neuronal cells from monosodium glutamate-induced toxicity by lowering calcium ion concentration. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 250 mg/mL (594.69 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.76 mM), Sonication is recommended.
Ethanol : 4.21 mg/mL (10.01 mM), Sonication is recommended.
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| Keywords | stroke | PotassiumChannel | Potassium Channel | non-opioid | NMDAR | NMDA receptor | Neuroprotective | KcsA | Katadolon Maleate | Ionotropic glutamate receptors | Inhibitor | inhibit | iGluR | Flupirtine maleate | Flupirtine | centrally | brain,?penetrant | analgesic | acting |
| Inhibitors Related | Urethane | Decanoic Acid | N-Methylsarcosine | L-Glutamic acid | 1,8-Cineole | Tetraethylammonium bromide | Indole-2-carboxylic acid | Chenodeoxycholic acid | L-Glutamic acid monosodium salt | Chlorzoxazone | Memantine | Memantine hydrochloride |
| Related Compound Libraries | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
