EFFECT OF A NEW POTENT H-2-BLOCKER, 3-[[[2-[(DIAMINOMETHYLENE)AMINO]-4-THIAZOLYL]METHYL]-THIO]-N-2-SULFAMOYLPROPIONAMIDINE (YM-11170) ON GASTRIC-SECRETION INDUCED BY HISTAMINE AND FOOD IN CONSCIOUS DOGS

  • 1 January 1982
    • journal article
    • research article
    • Vol. 256  (1) , 49-58
Abstract
The inhibitory effect of a new H2-receptor antagonist YM-11170 on gastric acid response to histamine and food was compared with that of cimetidine in the conscious dog with a Heidenhain pouch. When given i.v. at a steady state of gastric secretion by continuous infusion of histamine, YM-11170 was 42 times more potent and 1.3 times longer-lasting (P < 0.05) than cimetidine in reducing the total acid output. The higher potency of YM-11170 than that of cimetidine was also demonstrated in oral antisecretory tests with histamine. The oral ED50 relative to i.v. ED50 as an indirect indication of absorption rate of the drugs was 2.9 for YM-11170 and 2.7 for cimetidine. The secretory response to food stimulation was also antagonized by oral administration of YM-11170 with 40 times greater potency than that of cimetidine. The antisecretory effects of the drugs on the histamine-induced gastric secretion were characterized by a marked decrease in the secretory volume. No behavioral change was observed in association with the H2-blockers. Evidently, YM-11170 is a very potent inhibitor of gastric acid secretion whose absorption rate from the gastrointestinal tract is similar to that of cimetidine.

This publication has 0 references indexed in Scilit: