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.
D000818:Animals; D052160:Benzothiazoles; D002927:Cimetidine / Q000494:pharmacology; D003864:Depression, Chemical; D005744:Gastric Acid / Q000378:metabolism*; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D011708:Pylorus / Q000502:physiology; D011899:Ranitidine / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013844:Thiazoles / Q000494:pharmacology*
D052160:Benzothiazoles; D006635:Histamine H2 Antagonists; D013844:Thiazoles; D002927:Cimetidine; C050409:Wy 45086; C050410:Wy 45253; D011899:Ranitidine