Effects of TU-199, a novel H+ , K+ -ATPase inhibitor, on gastric acid secretion and gastroduodenal ulcers in rats

• Published in: Japanese Journal of Pharmacology 1994, Vol.64 (suppl.1), p.281-281
• Main Authors: Uchiyama, Kazuyuki, Nakamura, Ryuta, Ishikawa, Masami, Sekido, Shozaburo
• Format: Article
• Language: eng ; jpn
• ISSN: 0021-5198
• DOI: 10.1016/S0021-5198(19)50756-9

TU-199, 5-methoxy-2- 「 「(4-methoxy-3, 5-dimethyl-2-pyridyl )methyl」 sulfinyl」 -imidazo「4,5-b」pyridine is a newly synthesized H^+ ,K^+ -ATPase inhibitor. We investigated the inhibitory effects of TU-199 on gastric H^+ , K^+ -ATPase activity, gastric acid secretion, gastric or duodenal ulcers and compared with those of omeprazole (OPZ). TU-199 inhibited hog and dog gastric H^+ , K^+ -ATPase activity (IC_50：8.4 and 7.0 μM, respectively), its potency was almost equal to that of OPZ. In pylorus ligated rats, TU-199 inhibited gastric acid secretion in a dose-dependent manner (ED_50 ：3.0mg/kg, p.o.). TU-199 also prevented gastric ulcer formations induced by water-immersion stress, pylorus ligation, indomethacin, HCl-aspirin and HCl-EtOH, and mepirizole-induced duodenal ulcer in rats. Although TU-199 was equivalent to QPZ in inhibiting H ,K -ATPase activity, these antisecretory and antiulcer effects of this agent were more potent than those of OPZ. These results suggest that TU-199 may be useful for peptic ulcer therapy.