| 名稱 | Flupirtine maleate |
| 描述 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 體外活性 | 在動物研究中,Flupirtine可以抑制由于各種刺激而誘導(dǎo)的神經(jīng)痛反應(yīng),同時(shí)對海馬和紋狀體神經(jīng)元損傷也具有保護(hù)作用.在大鼠實(shí)驗(yàn)中,Flupirtine能夠放松肌肉. |
| 體內(nèi)活性 | Flupirtine能夠阻斷NMDA和gp120 HIV-1誘導(dǎo)的大鼠皮層神經(jīng)元細(xì)胞死亡。Flupirtine濃度為1 μM和10 μM 時(shí),可以降低TRAIL調(diào)節(jié)的人類活腦組織培養(yǎng)死亡；濃度為10 μM作用于10 mM L-谷氨酸處理的PC 12培養(yǎng)中,可以顯著降低非受體-調(diào)節(jié)的壞死細(xì)胞死亡；濃度為1或5μg/mL時(shí),通過作用于初級神經(jīng)元細(xì)胞,從而阻斷β-淀粉樣蛋白(25-35)誘導(dǎo)的凋亡；濃度為1-10 mM時(shí),通過降低鈣離子濃度,而保護(hù)初級神經(jīng)細(xì)胞免受谷氨酸鈉誘導(dǎo)的毒性。 |
| 存儲條件 | Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 250 mg/mL (594.69 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (23.79 mM), Solution.
10% DMSO+90% Saline : < 10 mg/mL (23.79 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
Ethanol : 4.21 mg/mL (10.01 mM), Sonication is recommended.
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| 關(guān)鍵字 | 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 |
| 相關(guān)產(chǎn)品 | glycine | L-Glutamic acid | Tetraethylammonium chloride | Urethane | 2,2,2-Trichloroethanol | N-Methylsarcosine | 1,8-Cineole | Cesium chloride | Indole-2-carboxylic acid | Decanoic Acid | 4-Aminopyridine | Carbamazepine |
| 相關(guān)庫 | 神經(jīng)保護(hù)化合物庫 | 經(jīng)典已知活性庫 | 抗癌上市藥物庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 臨床失敗化合物庫 | 膜蛋白靶向化合物庫 | 神經(jīng)退行性疾病化合物庫 | 免疫/炎癥分子化合物庫 | 疼痛相關(guān)化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |