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Description: Netupitant (also known as CID-6451149) is a novel, potent, selective and orally bioavailable neurokinin 1 (NK1) receptor antagonist with with Ki of 0.95 nM. It has potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV).
References: Hoffmann T, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1; 16(5):1362-5; Stathis M, et al. Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Eur J Pharmacol. 2012 Aug 15; 689(1-3):25-30..
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