Kinetics of antisecretory action of a new H2-antagonist, YM-11170, in conscious dogs

• Published in: European journal of pharmacology Vol. 91; no. 4; p. 371
• Main Authors: Takeda, M, Takagi, T, Maeno, H
• Format: Journal Article
• Language: English
• Published: Netherlands 05.08.1983
• Subjects: Animals; Atropine - pharmacology; Cimetidine - pharmacology; Dimaprit; Dogs; Famotidine; Gastric Acid - metabolism; Gastric Mucosa - drug effects; Gastric Mucosa - metabolism; Histamine H2 Antagonists - pharmacology; Kinetics; Male; Methacholine Chloride; Methacholine Compounds - pharmacology; Pentagastrin - pharmacology; Thiazoles - pharmacology; Thiourea - pharmacology
• ISSN: 0014-2999
• DOI: 10.1016/0014-2999(83)90160-7

The antisecretory property of YM-11170 was compared with that of cimetidine and atropine in the Heidenhain pouch dog. YM-11170 inhibited competitively dimaprit-induced gastric acid secretion in doses of 33 and 100 nmol/kg per h and its antisecretory potency was 148 times more pronounced than that of cimetidine. The secretory action of pentagastrin and methacholine was also inhibited by YM-11170 and cimetidine with doses similar to those required for the inhibition of dimaprit action although the inhibition by the H2-antagonists was not of the surmountable type. Atropine inhibited gastric secretion stimulated by methacholine and pentagastrin more strongly than that stimulated by dimaprit. It is concluded that YM-11170 is a competitive antagonist of dimaprit-induced gastric secretion in vivo and that the activity of the H2-antagonists in blocking gastric H2-receptors may reflect their inhibitory effect on the acid response to pentagastrin and methacholine.