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.

在动物研究中,Flupirtine可以抑制由于各种刺激而诱导的神经痛反应,同时对海马和纹状体神经元损伤也具有保护作用.在大鼠实验中,Flupirtine能够放松肌肉.

Flupirtine能够阻断NMDA和gp120 HIV-1诱导的大鼠皮层神经元细胞死亡。Flupirtine浓度为1 μM和10 μM 时,可以降低TRAIL调节的人类活脑组织培养死亡；浓度为10 μM作用于10 mM L-谷氨酸处理的PC 12培养中,可以显著降低非受体-调节的坏死细胞死亡；浓度为1或5μg/mL时,通过作用于初级神经元细胞,从而阻断β-淀粉样蛋白(25-35)诱导的凋亡；浓度为1-10 mM时,通过降低钙离子浓度,而保护初级神经细胞免受谷氨酸钠诱导的毒性。

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)