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.