Inhibition of gastric acid secretion by H2-receptor antagonists

Wy-45,086 and Wy-45,253, synthesized as potential antiulcer agents, were shown by in vitro and in vivo evaluation to have potent H2-receptor antagonist activity (respective pA2's of 8.1 and 7.6), and to have gastric acid antisecretory activity (respective ED50's of 1 and 2 mg/kg in the pylorus-ligated rat and of 1 and 1.4 mg/kg in dogs prepared with innervated gastric pouches). Both compounds were significantly more potent than ranitidine and cimetidine.