BMS 470539 (hydrochloride)

一种MC1R激动剂；在B16/F10小鼠黑色素瘤细胞和过表达人类MC1R的CHO细胞中诱导cAMP积累（EC50分别为11.6和16.8nM）；抑制小鼠LPS诱导的TNF-α产生（ED50=10μmol/kg，皮下注射）；减少小鼠模型中的LPS诱导的白细胞浸润和爪肿胀，分别用于肺炎和迟发型超敏反应；减少小鼠模型中的视网膜损伤，针对链脲佐菌素诱导的糖尿病视网膜病变；在小鼠帕金森病模型中，20mg/kg剂量增加纹状体多巴胺水平并减少纹状体α-突触核蛋白聚集体数量。An MC1R agonist; induces cAMP accumulation in B16/F10 murine melanoma cells and in CHO cells overexpressing human MC1R (EC50s = 11.6 and 16.8 nM, respectively); inhibits LPS-induced TNF-α production in mice (ED50 = 10 μmol/kg, s.c.); reduces LPS-induced leukocyte infiltration and paw swelling in mouse models of lung inflammation and delayed-type hypersensitivity, respectively; decreases retinal damage in a mouse model of streptozotocin-induced diabetic retinopathy; increases striatal dopamine levels and decreases the number of striatal α-synuclein aggregates in a mouse model of Parkinson's disease at 20 mg/kg.