Aprepitant
NK-1 antagonist / Potent human neurokinin-1 (NK-1) antagonist.1 It is an FDA approved medication for the treatment of chemotherapy-induced and postoperative nausea and vomiting.2 Aprepitant is also a selective activator of the K2P channel TRAAK.3 It also has been shown to have multiple anticancer effects.4
Biochemicals & reagents
170729-80-3
MK-0869; ONO-7436; L-754,030
Hale et al. (1998), Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1receptor antagonist; Med. Chem. 41 4607 Rapoport and Smit (2017); Clinical pharmacology of neurokinin-1 receptor antagonists for the treatment of nausea and vomiting associated with chemotherapy, Expert Opin. Drug Saf., 16 697 McCoull et al. (2022); Aprepitant is a novel, selective activator of the K2P channel TRAAK, Biochem. Biophys. Res. Commun., 588 41 Muñoz and Coveñas (2020); The Neurokinin-1 Receptor Antagonist Aprepitant: An Intelligent Bullet against Cancer?, Cancer (Basel), 12 2682
-20°C
TARGET: GPCR; Ion channel; Cytochrome/MDR -- PATHWAY: Cation channel; Lipid signaling; JNK pathway; JAK/STAT; Cell migration -- RESEARCH AREA: Neuroscience; Immunology -- DISEASE AREA: Cancer; Inflammation