SK609 (hydrochloride)

SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC₅₀ of 1109 nM. SK609 hydrochloride has the potential for parkinson research^[1]. In Vitro:In a Competitive inhibition affinity assay by SK609 hydrochloride to D3R, SK609 exhibits an EC₅₀ value of 1109 nM at D3R^[1].
SK609 hydrochloride activates Gi/o proteins and downstream ERK1/2 signaling but have no effects on D2R/ERK1/2. SK609 exhibits EC₅₀ values of 1.1 μM, 50.2 nM, and 14.4 μM for [³⁵S]GTPγS binding, ERK1/2 phosphorylation, and β-Arrestin recruitment respectively^[1].
In Vivo:Safety toxicology studies of SK609 hydrochloride in rats have shown the maximum tolerated dose of SK609 hydrochloride is 30 mg/kg and all the doses used in this study are well within the no-observed-adverse-effect level of SK609 hydrochloride^[1].
SK609 hydrochloride shows the maximum tolerated dose of SK609 hydrochloride is 30mg/kg in safety toxicology study within the no-observed-adverse-effect level of SK609 hydrochloride^[2].
In the cynomolgus macaques PK study, oral administration of SK609 hydrochloride (0.5, 2 and 4 mg/kg) is associated with mean C_max values of 13.7, 69.3 and 218 ng/ml respectively, occurring at (T_max) 4.1, 6.4 and 5.0 hours following administration and with corresponding AUC_(0-t) values of 171, 904 and 2938 h.ng/ml respectively^[3].
Following intravenous administration (2 mg/kg), SK609 hydrochloride has a mean terminal half-life of 7.9 h in plasma. SK609 hydrochloride (i.p.; 2, 4, 6, 8, 10, 20 mg/kg) significantly improves the performance of the impaired paw and also normalized the bilateral asymmetry associated with the hemiparkinson rat^[3].