SKF83959

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SKF83959 是一种有效的选择性多巴胺 D1-like 受体部分激动剂。SKF83959 Ki 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 D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 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.

SKF83959 (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 (0.1~10 μM; PC12 cell) changes the EC50 value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM.

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

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GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

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80751-85-5

317.81

C18H20ClNO2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (314.65 mM; 超声助溶 )

ClC1=C2C(C(CN(C)CC2)C3=CC(C)=CC=C3)=CC(O)=C1O

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(-20℃)

With Ice Pack

≥ 2 years