Antisecretory effects of two new histamine H2-receptor antagonists.
N-(3-[3-(1-Piperidinylmethyl)phenoxy]propyl)acetoxyaceta mide hydrochloride (Hoe 760) and N-(3-[3-(1-piperidinylmethyl)phenoxy]propyl)glycolamine hydrochloride (Hoe 062) are highly specific H2-receptor antagonists. The compounds are equipotent after intragastrical or intravenous administration. The antagonists inhibited gastric acid secretion in the rat induced by all stimuli tested, carbachol, desglugastrin and histamine. In the Heidenhain pouch dog whose gastric acid secretion was stimulated by food or histamine the two receptor blockers proved to be 4-6 times more potent inhibitors than cimetidine.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D002927:Cimetidine / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D004285:Dogs; D005260:Female; D005502:Food; D005744:Gastric Acid / Q000378:metabolism*; D005753:Gastric Mucosa / Q000201:enzymology; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D008566:Membranes / Q000378:metabolism; D010477:Perfusion; D011708:Pylorus / Q000502:physiology; D051381:Rats; D011970:Receptors, Histamine H2 / Q000378:metabolism
D006635:Histamine H2 Antagonists; D011970:Receptors, Histamine H2; D002927:Cimetidine; D000242:Cyclic AMP; D000262:Adenylyl Cyclases