L-732,138

L-732,138 is a neurokinin-1 (NK₁) receptor antagonist (IC₅₀ = 1.6 nM in CHO cells expressing the human receptor).¹ 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.² It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID₅₀ = 8 mg/kg, i.p.).¹ L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.³

WARNING This product is not for human or veterinary use.

1. MacLeod, A.M., Merchant, K.J., Brookfield, F., et al. Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. J. Med. Chem. 37(9), 1269-1274 (1994).

2. Muñoz, M., Rosso, M., González-Ortega, A., et al. The NK-1 receptor antagonist L-732,138 induces apoptosis and counteracts substance P-related mitogenesis in human melanoma cell lines. Cancers (Basel) 2(2), 611-623 (2010).

3. Cahill, C.M., and Coderre, T.J. Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre- or post-treatment with a neurokinin-1 antagonist. Pain 95(3), 277-285 (2002).