L-732,138

NK1受体拮抗剂（在表达人类受体的CHO细胞中IC50=1.6nM）；对NK1受体的选择性优于NK2和NK3受体（两者的IC50s=>5,000nM）；抑制COLO858、MELHO和COLO679黑色素瘤细胞的生长（IC50s分别为44.6、76.3和64.2μM），并诱导这些细胞系的细胞凋亡；抑制豚鼠中P物质引起的血浆外渗（ID50=8mg/kg，腹腔注射）；减轻大鼠坐骨神经慢性压迫性损伤引起的神经性疼痛模型中的机械性异常疼痛和冷痛觉过敏。An NK1 receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor); selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both); inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines; inhibits plasma extravasation induced by substance P in guinea pigs (ID50 = 8 mg/kg, i.p.); attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.分子式C22H18F6N2O3分子量472.4CC(N[C@@H](CC1=CNC2=C1C=CC=C2)C(OCC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)=O