Lu AA33810

NPY受体Y5的拮抗剂（对于人类受体，Ki=1.5nM）；对Y5的选择性优于Y1、Y2和Y4（在表达大鼠受体的HEK293膜中，所有受体的Kis=>10µM）；与5-HT1A和5-HT2B受体结合（Kis分别为478和247nM）；抑制NPY诱导的钙动员和cAMP在表达大鼠Y5受体的COS-7和HEK293细胞中的积累；在10mg/kg剂量下，在社交探索测试中增加大鼠的社交互动时间，并在强迫游泳测试中减少不动时间。An antagonist of NPY receptor Y5 (Ki = 1.5 nM for the human receptor); selective for Y5 over Y1, Y2, and Y4 (Kis = >10 µM for all in HEK293 membranes expressing rat receptors); binds 5-HT1A and 5-HT2B receptors (Kis = 478 and 247 nM, respectively); inhibits NPY-induced calcium mobilization and cAMP accumulation in COS-7 and HEK293 cells expressing the rat Y5 receptor, respectively; increases social interaction time in a social exploration test, as well as decreases immobility time in the forced swim test, in rats at 10 mg/kg.分子式C19H25N3O2S3分子量423.6CS(NC[C@@H](CC1)CC[C@H]1NC2=NC3=C(S2)CCSC4=CC=CC=C34)(=O)=O