化合物SKF83959 T60835

Product Introduction
Bioactivity


英文名: SKF83959

描述: SKF83959 是苯并氮平类化合物，是一种具有选择性和有效性的多巴胺D1受体部分激动剂，对大鼠D1，D5，D2和D3受体的Ki 值分别为 1.18, 7.56, 920 和 399 nM。SKF83959 是 sigma (σ)-1受体的有效变构调节剂，可改善认知功能障碍，用于研究抑郁症和阿尔茨海默病。

体外活性: SKF83959 (0.1-30 micromol/L) improved H2O2-reduced cell viability in a dose-dependent manner. Moreover, SKF83959 treatment significantly inhibited H2O2-activated glycogen synthase kinase-3beta (GSK-3beta) which was associated with the drug's neuroprotective effect. Moreover, the application of either SKF83959 or a pharmacological inhibitor of GSK-3beta attenuated the inhibition by H2O2 on the expression of inducible NO synthase and the production of NO. In addition, SKF83959 also effectively decreased the level of lipid peroxidation and increased the activity of GSH-peroxidase altered by H2O2. These results suggest that SKF83959 exerts its neuroprotective effect through both receptor-dependent and independent mechanisms: Inhibition of GSK-3beta and consequently increasing the expression of inducible NO synthase via putative PI-linked DAR; and its anti-oxidative activity which is independent of DAR.[5]

体内活性: SKF83959 (0.5, 1 mg/kg; i.p.; 1 h; Male ICR male mice) alleviates scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test.[1]SKF83959 (1 mg/kg; i.p.; 30 minutes; Male ICR male mice) memory-enhancing effects are hindered by the blockade of the brain-derived neurotrophic factor system.[1]SKF83959 exhibits anti-amnesic activities and reinstates the scopolamine-induced decrease in the BDNF signaling pathway in the hippocampus of mice.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 90 mg/mL (283.19 mM)


相关产品: LP-211 | SCH-23390 hydrochloride | Pimozide-d4 | L-DOPA | Methiothepin mesylate | Methyldopa | Aripiprazole Lauroxil | Penfluridol | SCH-23390 maleate | Clozapine

相关库: Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Bioactive Compound Library

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