Preferred Label : Tradipitant;
NCIt definition : An orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor;
NK1R; NK-1R) antagonist with potential anti-emetic, anti-pruritic and anti-inflammatory
activities. Upon oral administration, tradipitant competitively binds to and blocks
the activity of the NK1R in the central nervous system (CNS), thereby inhibiting the
binding of the endogenous ligand and neuropeptide, substance P (SP; neurokinin-1;
NK1). This inhibits SP/NK1-mediated signal transduction and may prevent both SP-induced
emesis and pruritis. In addition, inhibition of SP/NK1R signaling also reduces neurogenic
inflammation which is triggered by the release of neuropeptides, such as substance
P, from nerve cells. NK1R is a G protein-coupled receptor (GPCR) that preferentially
binds to SP, a neuropeptide secreted by neuronal cells and inflammatory cells.;
UNII : NY0COC51FI;
InChIKey : CAVRKWRKTNINFF-UHFFFAOYSA-N;
CAS number : 622370-35-8;
Molecule name : LY-686017; VLY-686;
NCI Metathesaurus CUI : CL554039;
Origin ID : C152707;
UMLS CUI : C4519147;
Semantic type(s)
- concept_is_in_subset
