Preferred Label : Grapiprant;
NCIt synonyms : N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide;
NCIt definition : An orally bioavailable antagonist of the prostaglandin E receptor subtype 4 (EP4),
with potential analgesic, immunomodulating and antineoplastic activities. Upon administration
of grapiprant, this agent selectively binds to and inhibits the binding of prostaglandin
E2 (PGE2) and prevents the activation of the EP4 receptor. This inhibits PGE2-EP4
receptor-mediated signaling and prevents proliferation in tumor cells in which the
PGE2-EP4 signaling pathway is over-activated. In addition, EP4 receptor inhibition
modulates the immune system by preventing both interleukin-23 (IL-23) production and
the IL-23-mediated expansion of Th17 cells. As EP4 is expressed by peripheral sensory
neurons, blockade of EP4-mediated signaling may induce an analgesic effect. EP4, a
prostanoid receptor subtype, is a G protein-coupled receptor that is expressed in
certain types of cancers; it promotes tumor cell proliferation and invasion.;
UNII : J9F5ZPH7NB;
InChIKey : HZVLFTCYCLXTGV-UHFFFAOYSA-N;
CAS number : 415903-37-6; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 415903-37-6
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G-SRS /a ;
Molecule name : RQ-07; AAT-007; RQ-00000007; AT-001; CJ-023,423; CJ 023,423;
Origin ID : C124131;
UMLS CUI : C4278621;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
