Effect of the novel histamine H2-antagonist 5,6-dimethyl-2-[4-[3-(1- piperidinomethyl)phenoxy]-(z)-2-butenylamino]-4(1H)-pyrimidine dihydrochloride on histamine-induced gastric acid secretion in Heidenhain pouch dogs.
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| Abstract |
Effects of IGN-2098 (5,6-dimethyl-2-[4-[3-(1-piperidinomethyl)phenoxy]- (z)-2-butenylamino]-4(1H)-pyrimidone dihydrochloride, CAS 126869-04-3) a novel histamine H2-antagonist, on histamine-induced gastric acid secretion were investigated in Heidenhain pouch dogs in comparison with those of famotidine, roxatidine acetate HCl and cimetidine. Orally administered IGN-2098 (0.03-1.0 mg/kg), famotidine (0.01-0.3 mg/kg), roxatidine acetate HCl (0.1-1.0 mg/kg) and cimetidine (0.3-3.0 mg/kg) showed dose-dependent inhibition on histamine-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 effective 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 and is a useful antisecretory drug for the treatment of peptic ulcer disease.
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| Authors | M Uchida, S Ohba, Y Ikarashi, N Misaki, O Kawano |
| Journal | Arzneimittel-Forschung (Arzneimittelforschung) Vol. 43 Issue 8 Pg. 873-6 (Aug 1993) ISSN: 0004-4172 [Print] Germany |
| PMID | 8105784 (Publication Type: Comparative Study, Journal Article) |
| Chemical References |
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