SKF83959

Research use only, not for human use.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.

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 : 100 mg/mL (314.65 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years