Inhibition of dimaprit- and pentagastrin-induced gastric acid secretion in cats by the new histamine H2 antagonist, CM 57755.
The antisecretory effects of CM 57755, a new histamine-H2 receptor antagonist, have been compared with those of cimetidine on gastric acid secretion induced by intravenous infusions of dimaprit or pentagastrin into conscious cats with chronically implanted gastric fistulae. Intravenous infusion of CM 57755 induced a parallel shift to the right of the dimaprit dose-response curve. The potency of CM 57755 was comparable with that of cimetidine as shown by similar doses causing a 5-fold displacement to the right of the dimaprit dose-response curve (4.9 mumol kg-1 h-1 for CM 57755 and 4.7 mumol kg-1 h-1 for cimetidine). Unlike that with dimaprit, the acid secretion stimulated by increasing doses of pentagastrin was inhibited by CM 57755 with depression of the maximal effect, indicating non-competitive antagonism. In a second series of experiments the time course of the anti-secretory action of intragastrically administered CM 57755 was studied from the gastric acid secretion induced by constant infusion of dimaprit. At equieffective doses, CM 57755 caused more sustained inhibition than cimetidine.
D000818:Animals; D002415:Cats; D002927:Cimetidine / Q000494:pharmacology; D017259:Dimaprit; D005744:Gastric Acid / Q000378:metabolism*; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000494:pharmacology; D010418:Pentagastrin / Q000037:antagonists & inhibitors*; D013890:Thiourea / Q000037:antagonists & inhibitors*
D006635:Histamine H2 Antagonists; D009536:Niacinamide; D002927:Cimetidine; C041784:ramixotidine; D010418:Pentagastrin; D013890:Thiourea; D017259:Dimaprit