Pharmacological studies of 2-(3-(3-(1-piperidinylmethyl)-phenoxy)propylamino)-4 (3H)-quinazolinone (NO-794), a new histamine H2-receptor antagonist.

Abstract

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.

• Authors: M Oshita, K Morikawa, T Aratani, H Kato, Y Ito
• Journal: Japanese journal of pharmacology (Jpn J Pharmacol) Vol. 42 Issue 2 Pg. 229-35 (Oct 1986) ISSN: 0021-5198 [Print] Japan
• PMID: 2879057 (Publication Type: Journal Article)

Chemical References

• Histamine H2 Antagonists
• Phenoxypropanolamines
• Quinazolines
• Quinazolinones
• NO 794
• Ranitidine
• Cyclic AMP

Topics

• Animals
• Cyclic AMP (biosynthesis)
• Gastric Acid (drug effects, metabolism)
• Gastric Mucosa (drug effects, metabolism)
• Guinea Pigs
• Heart Rate (drug effects)
• Histamine H2 Antagonists
• In Vitro Techniques
• Ligation
• Male
• Phenoxypropanolamines
• Pylorus
• Quinazolines (pharmacology)
• Quinazolinones
• Ranitidine (pharmacology)