| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (118.94 mM), Sonication is recommended.
Ethanol : 4.2 mg/mL (10 mM)
|
| Keywords | centrally | acting | brain,?penetrant | Flupirtine maleate | KcsA | Flupirtine | Neuroprotective | Inhibitor | inhibit | Ionotropic glutamate receptors | stroke | non-opioid | Katadolon Maleate | Flupirtine Maleate | Potassium Channel | analgesic | iGluR | NMDAR |
| Inhibitors Related | Minoxidil sulfate | L-Glutamic acid | glycine | Halothane | L-Glutamic acid monosodium salt | Riluzole | Cloperastine hydrochloride | O-Phospho-L-serine | Indapamide |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
