Antisecretory and Antiulcer Effects of YM020, a New H^+, K^+-ATPase Inhibitor, in Rats and Dogs

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概要

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• We examined the effects of YM020 (3-cyanomethyl-2-methyl-8-[(3-methyl-2-butenyl)oxy]-imidazo[1, 2-α]pyridine), a novel H<SUP>+</SUP>, K<SUP>+</SUP>-ATPase inhibitor, on gastric acid secretion and experimental gastroduodenal lesions in rats and dogs. Intraduodenal, subcutaneous and oral YM020 inhibited basal gastric acid secretion in pylorus-ligated rats with ED<SUB>50</SUB> values of 9.1, 9.1 and 9.5 mg/kg, respectively. Oral pretreatment with YM020 5 hr before ligation still suppressed acid secretion, with a potency a little less than that of omeprazole. In anesthetized dogs, intravenous YM020 inhibited histamine-, methacholine- and pentagastrin-induced gastric acid secretion with ED<SUB>50</SUB> values of 0.05, 0.01 and 0.08 mg/kg, respectively. In Heidenhain pouch dogs, although oral YM020 (3 mg/kg) inhibited histamine-induced acid secretion, acid output returned to control levels faster than in dogs treated with omeprazole. Oral YM020 inhibited the formation of water-immersion restraint stress-, indomethacin-, absolute ethanol-, 0.7 N hydrochloric acid- and cysteamine-induced gastric or duodenal lesions with ED<SUB>50</SUB> values of 2.9, 4.3, 2.0, 11.7 and 8.4 mg/kg, respectively. Moreover, subcutaneous YM020 also suppressed the formation of ethanol- and HCl-induced gastric lesions. These results suggest that YM020 has an antisecretory effect almost the same as or 2 to 3 times weaker than those of omeprazole and that its duration is not as long as that of omeprazole in rats and dogs. Furthermore, YM020 possesses a cytoprotective effect and the mechanism of YM020 may be different to that of omeprazole.

• 社団法人 日本薬理学会の論文
• 1995-01-01

著者

• Miyata K

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Miyata K

  Yamanouchi Pharmaceutical Co. Ltd. Tsukuba City Jpn

• Miyata Keiji

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

• Miyata Keiji

  Inflammation Research Pharmacology Laboratories Institute For Drug Discovery Research Yamanouchi Pha

• Ohta Masato

  Pharmaceutical Research Center Meiji Seika Kaisha Ltd.

• Yanagisawa I

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Yanagisawa Isao

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

• Yanagisawa Isao

  山之内製薬

• Ohta Miyako

  Division Of Biological Chemistry And Biologicals National Institute Of Health Sciences

• Miyata K

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

• Kamato Takeshi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd

• Miyata K

  Inflammation Research Pharmacology Laboratories Institute For Drug Discovery Research Yamanouchi Pha

• OHTA Mitsuaki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• Miyata K

  Hitachi Research Laboratory Hitachi Ltd.

• YUKI Hidenobu

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• SHIKAMA Hisataka

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd

• Shikama Hisataka

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd

• Yuki Hidenobu

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Miyata Keiji

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

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