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SKF83959
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SKF83959图片
CAS NO:80751-85-5
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

SKF83959 is a potent and selective dopamineD1-likereceptor partial agonist. SKF83959Kivalues for ratD1,D5, D2and D3receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator ofsigma (σ)-1receptor. 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].

IC50& Target[3][4]

D1Receptor

1.18 nM (Ki)

Sigma 1 Receptor

 

D5Receptor

7.56 nM (Ki)

D2Receptor

920 nM (Ki)

D3Receptor

399 nM (Ki)

体外研究
(In Vitro)

SKF83959 (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 (0.1~10 μM; PC12 cell) changes the EC50value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM[2].

体内研究
(In Vivo)

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.
分子量

317.81

Formula

C18H20ClNO2

CAS 号

80751-85-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.