EFFECT OF THE NOVEL HISTAMINE H-2-ANTAGONIST THYL)PHENOXY]-(Z)-2-BUTENYLAMINO]-4(1H)-PYRIMIDONE DIHYDROCHLORIDE ON HISTAMINE-INDUCED GASTRIC-ACID SECRETION IN HEIDENHAIN POUCH DOGS

Effects of IGN-2098 thyl)phenoxy]-(z)-2-butenylamino]-4(1H)-pyrimidone dihydrochloride, CAS 126869-04-3) a novel histamine H-2-antagonist, o n histamine-induced gastric acid secretion were investigated in Heiden hain pouch dogs in comparison with those of famotidine, roxatidine ace tate HCI and cimetidine. Orally administered IGN-2098 (0.03-1.0 mg/kg) , famotidine (0.01-0.3 mg/kg), roxatidine acetate HCI (0.1 - 1.0 mg/kg ) and cimetidine (0.3-3.0 mg/kg) showed dose-dependent inhibition on h istamine-induced gastric acid secretion, and ED50 values of IGN-2098, famotidine, roxatidine acetate HCl and cimetidine were 0.077, 0.024, 0 .200 and 0.585 mg/kg, respectively. IGN-2098 was effective even at 6 h after administration and ED50 value was 0.315 mg/kg. IGN-2098 was eff ective also by intravenous route. The inhibitory effect of IGN-2098 on histamine-induced gastric secretion was not affected by the repeated administration of IGN-2098 (1 mg/kg b.i.d. for 14 days). These results show that IGN-2098 is a potent and long acting antisecretory agent an d is a useful antisecretory drug for the treatment of peptic ulcer dis ease.