Aprepitant

一种止吐药和NK1拮抗剂（Ki=3nM；对于人类受体，IC50=0.09nM）；对NK1受体的选择性优于NK3受体（对于人类NK3，Ki=454.1nM）；在1mg/kg剂量下可防止P物质诱发的血浆外渗到豚鼠食道；减少NK1激动剂诱发的沙鼠脚部拍打。An antiemetic and NK1 antagonist (Ki = 3 nM; IC50 = 0.09 nM for the human receptor); selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3); prevents substance P-induced plasma extravasation into the esophagus of guinea pigs at 1 mg/kg; reduces NK1-agonist-induced foot tapping in gerbils.