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Aprepitant

CAS No. : 170729-80-3

MCE 国际站：Aprepitant

产品活性：Aprepitant (MK-0869) 是选择性和高亲和力的神经激肽1受体拮抗剂，K_d 值为86 pM。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Anti-infection

作用靶点：Neurokinin Receptor  |  Bacterial  |  HIV  |  Antibiotic

In Vitro: Aprepitant decreases the metabolic activity with an estimated IC₅₀ value of 20 µM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 µM) induces p53 accumulation and expression of pro-apoptotic p53 target genes. Aprepitant (1, 5, 10 µM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC₉₀ value of aprepitant is equivalent to 10 μM, and the IC₅₀ value is about 5 μM.

In Vivo: Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B. burgdorferi. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, prevents B. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced reductions in astrocyte activity/numbers. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls.

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