Tafluprost (free acid)

一种FP受体激动剂（对人类受体的Ki=4nM），为PGF2α衍生物，且为tafuprost的活性代谢物；对FP受体选择性高于多巴胺受体和PGE2受体亚型EP1和EP2，以及32种神经受体和转运蛋白，在1µM时；在隔离的猫虹膜括约肌中诱导收缩（EC50=0.6nM）；在100µM时，增加HUVEC细胞的增殖、迁移、毛细血管形成以及COX-2水平。An FP receptor agonist (Ki = 4 nM for the human receptor), a PGF2α derivative, and an active metabolite of tafluprost; selective for the FP receptor over the dopamine receptor and PGE2 receptor subtypes EP1 and EP2, as well as a panel of 32 neurological receptors and transporters, at 1 µM; induces constriction in isolated cat iris sphincters (EC50 = 0.6 nM); increases the proliferation and migration of, capillary formation by, and COX-2 levels in, HUVECs at 100 µM.