Studies on Antiulcer Agents. I. Synthesis and Pharmacological Properties of Ethyl 2-[(1H-Benzimidazol-2-yl)sulfinylmethyl]-4-dimethylamino-5-pyrimidinecarboxylate, a New H^+/K^+-ATPase Inhibitor Possessing Mucosal Protective Activity
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概要
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Ethyl 2-[(1H-benzimidazol-2-yl)sulfinylmethyl]-4-dimethylamino-5-pyrimidinecarboxylate (2) has been synthesized and evaluated for antiulcer properties. Compound 2 is a H^+/K^+-ATPase inhibitor that affords mucosal protection against absolute ethanol-induced gastric lesions in rats after oral and parenteral administrations. On the other hand, omeprazole, a representative H^+/K^+-ATPase inhibitor, showed mucosal protective action only after oral administration, indicating that it required gastric acid secretion to generate activity. The antiulcer activity of 2 in animal models, such as water-immersion stress-induced gastric ulcer in rats and acidified aspirin-induced gastric ulcer in rats, was three times higher than that of cimetidine.
- 社団法人日本薬学会の論文
- 1995-01-15
著者
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嶋村 浩
Research Laboratories, Morishita Pharmaceutical Co., Ltd.
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TANAKA Yasuko
Showa College of Pharmaceutical Sciences
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佐藤 誠
Research Institute, Daiichi Seiyaku Co., Ltd.,
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佐藤 誠
日本ヘキスト・マリオン・ルセル(株)研究開発本部開発研究所滋賀サイト
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Tanaka Y
Osaka University Of Pharmaceutical Science
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寺島 幸司
Research Laboratories, Roussel Morishita Co., Ltd.,
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川瀬 明人
Research Laboratories, Roussel Morishita Co., Ltd.,
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田中 裕二
Research Laboratories, Roussel Morishita Co., Ltd.,
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石塚 泰博
Research Laboratories, Roussel Morishita Co., Ltd.,
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上西 啓司
Research Laboratories, Roussel Morishita Co., Ltd.,
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木村 伊佐美
Research Laboratories, Roussel Morishita Co., Ltd.,
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Shimamura H
Research Laboratories Roussel Morishita Co. Ltd.
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嶋村 浩
Research Laboratories Roussel Morishita Co. Ltd.
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嶋村 浩
Research Laboratories Morishita Pharmaceutical Co. Ltd.
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Kimura Isami
Research Laboratories Roussel Morishita Co. Ltd.
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田中 裕二
Research Laboratories Roussel Morishita Co. Ltd.
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石塚 泰博
Research Laboratories Roussel Morishita Co. Ltd.
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木村 伊佐美
日本ヘキスト・マリオン・ルセル(株)研究開発本部開発研究所滋賀サイト
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上西 啓司
Research Laboratories Roussel Morishita Co. Ltd.
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川瀬 明人
Chugai Pharmaceutical Co. Ltd. Tokyo Jpn
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寺島 幸司
Research Laboratories Roussel Morishita Co. Ltd.
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川瀬 明人
Research Laboratories Roussel Morishita Co. Ltd.
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