Aprepitant (MK-0869; MK-869; L-754030; Emend; MK0869; MK869; L754030),又称阿瑞匹坦、阿瑞吡坦或阿瑞比坦,是治疗癌症化疗呕吐药物,是neurokinin-1 receptor选择性拮抗剂,IC50为0.1 nM,Kd值为86 pM。阿瑞匹坦通过阻止中枢神经系统内P物质与NK-1受体的结合表现出止呕作用。
参考文献
1.Martinez AN, et al. Aprepitant limits in vivo neuroinflammatory responses in a rhesus model of Lyme neuroborreliosis. J Neuroinflammation. 2017 Feb 15;14(1):37.
2.Bayati S, et al. Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. Eur J Pharmacol. 2016 Nov 15;791:274-283.
3.Mannangatti P, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl). 2017 Feb;234(4):695-705.
4.Barrett JS, et al. Pharmacologic rationale for the NK1R antagonist, aprepitant as adjunctive therapy in HIV. J Transl Med. 2016 May 26;14(1):148.
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