SKF 83959 

SKF83959 is a potent and selective dopamine D₁-like receptor partial agonist. SKF83959 K_i 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^[1][2][3][4].

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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

317.81

C₁₈H₂₀ClNO₂

80751-85-5

固体

White to light yellow

Room temperature in continental US; may vary elsewhere.

• [1]. Sheng G, et al. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia. Biol Pharm Bull. 2018;41(3):427-434.  [Content Brief]

  [2]. Jin LQ, et al. SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain. J Neurochem. 2003;85(2):378-386.  [Content Brief]

  [3]. Neumeyer JL, et al. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur J Pharmacol. 2003;474(2-3):137-140.  [Content Brief]

  [4]. Guo L, et al. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol Pharmacol. 2013;83(3):577-586.  [Content Brief]