L-732,138

L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor). It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 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. It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.). L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic...