SKF 83959 (hydrobromide)

SKF83959 hydrobromide is a potent and selective dopamine D₁-like receptor partial agonist. SKF83959 hydrobromide K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression^[1][2][3][4]. IC50 & Target:Ki: 1.18 nM (D₁ receptor)^[3].
Ki: 7.56 nM (D₅ receptor)^[3].
sigma (σ)-1^[4] In Vitro: SKF83959 hydrobromide (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 hydrobromide (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]. In Vivo: SKF83959 hydrobromide (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 hydrobromide (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade^[1].
SKF83959 hydrobromide has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice^[1].