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编 号:F605222
分子式:C18H20ClNO2
分子量:317.81
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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生物活性:
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.

体内研究:
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.

体外研究:
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.
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