Kinetics of antisecretory action of a new H2-antagonist, YM-11170, in conscious dogs.
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.
D000818:Animals; D001285:Atropine / Q000494:pharmacology; D002927:Cimetidine / Q000494:pharmacology; D017259:Dimaprit; D004285:Dogs; D015738:Famotidine; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D016210:Methacholine Chloride; D008688:Methacholine Compounds / Q000494:pharmacology; D010418:Pentagastrin / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology*; D013890:Thiourea / Q000494:pharmacology
D006635:Histamine H2 Antagonists; D008688:Methacholine Compounds; D013844:Thiazoles; D016210:Methacholine Chloride; D015738:Famotidine; D001285:Atropine; D002927:Cimetidine; D010418:Pentagastrin; D013890:Thiourea; D017259:Dimaprit