Netupitant

NK1受体拮抗剂（Ki=0.95nM）；对人类NK1具有选择性，而对人类NK2和NK3以及大鼠NK1则无选择性（Kis=>1,500nM）；在纳摩尔范围内使用时，对NK1具有选择性，而对50G蛋白偶联受体、单胺转运体和离子通道则无选择性；降低豚鼠离体回肠对P物质的最大反应；在剂量为1-10mg/kg时抑制小鼠因P物质引起的抓挠、咬和舔行为；减少沙鼠因NK激动剂引起的脚部轻拍行为（ID50s=1.5mg/kg，腹腔注射，或0.5mg/kg，口服）。An NK1 receptor antagonist (Ki = 0.95 nM); selective for human NK1 over human NK2 and NK3 and rat NK1 (Kis = >1,500 nM); selective for NK1 over 50 G protein-coupled receptors, monoamine transporters, and ion channels when used in the nanomolar range; decreases the maximal response to substance P in isolated guinea pig ileum; inhibits substance P-induced scratching, biting, and licking in mice at doses of 1-10 mg/kg; decreases NK agonist-induced foot tapping in gerbils (ID50s = 1.5 mg/kg, i.p., or 0.5 mg/kg, oral).