SKF83959 是一种有效的选择性多巴胺D1-like受体部分激动剂。SKF83959Ki对大鼠D1，D5，D2和D3的值分别为 1.18, 7.56, 920 和 399 nM。SKF83959 是一种有效的sigma (σ)-1受体变构调节剂。SKF83959 属于 benzazepine 家族，对认知功能障碍有改善作用。SKF83959 可用于研究阿尔茨海默病和抑郁症。

SKF83959 is a potent and selective dopamine D 1 -like receptor partial agonist. SKF83959 K i values for rat D 1, D 5, D 2 and D 3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression [1] [2] [3] [4].

SKF83959 (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 (0.1~10 μM; PC12 cell) changes the EC 50 value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM [2].

SKF83959 (0.5 and 1 mg/kg; i.p.; 1 hour) reverses the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test [1]. SKF83959 (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade [1]. SKF83959 has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice [1]. Animal Model: Male ICR male mice (8 weeks) [1] Dosage: 0.5 and 1 mg/kg Administration: I.p.; 1 hour Result: Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test. Animal Model: Male ICR male mice (8 weeks) [1] Dosage: 1 mg/kg Administration: I.p.; 30 minutes Result: The memory enhancing effects were prevented by BDNF system blockade.

80751-85-5

C18H20ClNO2

317.81

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years