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NCI Drug Dictionary


An orally active, benzodiazepine type, selective cholecystokinin B receptor (CCKBR; CCK2R; gastrin receptor) antagonist with potential gastric acid reducing and antiproliferative activity. Upon administration of netazepide, this agent selectively binds to and blocks the CCKBR, thereby preventing the binding of gastrin and cholecystokinin. This may prevent gastric neuroendocrine enterochromaffin-like (ECL) cell-induced secretion of histamine, ultimately preventing gastric acid secretion from adjacent parietal cells. In addition, YF476 may inhibit ECL cell proliferation and ECL-derived gastric carcinoids. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
Synonyms:CCK-B/gastrin receptor antagonist YF476
cholecystokin 2 (CCK(2)) receptor antagonist YF476
cholecystokinin B receptor antagonist YF476
Code names:YF476
Chemical structure:1-((3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-3-(3-(methylamino)phenyl)urea