Pharmacological studies of 2-(3-(3-(1-piperidinylmethyl)-phenoxy)propylamino)-4 (3H)-quinazolinone (NO-794), a new histamine H2-receptor antagonist.
The pharmacological profile of a new histamine H2-receptor antagonist, 2-(3-(3-(1-piperidinylmethyl)phenoxy)propylamino)-4 (3H)-quinazolinone (NO-794), was studied. NO-794 was a potent and selective histamine H2-receptor antagonist in the guinea-pig atria and gastric mucosal cells. NO-794 (1 X 10(-5) M) did not interact with H1-, muscarinic and beta 1-receptors. In guinea-pig atria, antagonism of NO-794 was unsurmountable. The onset of action of NO-794 was slow, and this antagonism was apparently irreversible not only on the guinea-pig atria but also on the gastric mucosal cells. In addition, NO-794 inhibited gastric acid secretion in pylorus ligated rats when administered intraduodenally. These results indicate that NO-794 is a powerful and unique histamine H2-receptor antagonist and may be useful in the treatment of peptic ulcer.
D000818:Animals; D000242:Cyclic AMP / Q000096:biosynthesis; D005744:Gastric Acid / Q000187:drug effects / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D006635:Histamine H2 Antagonists; D066298:In Vitro Techniques; D008026:Ligation; D008297:Male; D050198:Phenoxypropanolamines; D011708:Pylorus; D011799:Quinazolines / Q000494:pharmacology*; D052999:Quinazolinones; D011899:Ranitidine / Q000494:pharmacology
D006635:Histamine H2 Antagonists; D050198:Phenoxypropanolamines; D011799:Quinazolines; D052999:Quinazolinones; C050470:NO 794; D011899:Ranitidine; D000242:Cyclic AMP