Effects of a New Histamine H2-Receptor Antagonist, Z-300, on Gastric Secretion and Gastro-Duodenal Lesions in Rats: Comparison with Roxatidine.
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概要
- 論文の詳細を見る
We examined the effects of a new compound, <I>N</I>-[3-[3-(piperidinomethyl)phenoxy]-propyl]-2-(2-hydroxyethyl-l-thio)acetamido·2-(4-hydroxy benzoyl)benzoate (Z-300), on the histamine H<SUB>2</SUB>-receptor, gastric secretion in rats and dogs, and acute gastro-duodenal lesions or chronic gastric ulcers in rats. Roxatidine acetate hydrochloride (roxatidine), a known histamine H<SUB>2</SUB>-receptor antagonist, was used as a reference compound. The pA<SUB>2</SUB> values for Z-300 and roxatidine for the isolated guinea pig atrium were 6.8 and 7.0, respectively. These agents at <10<SUP>-5</SUP> M did not affect the contraction of guinea pig ileum in response to carbachol. Z-300, administered either orally or parenterally, significantly inhibited the basal and histamine-stimulated gastric acid secretion in rats. Gastric acid secretion stimulated by histamine, pentagastrin or carbachol in Heidenhain pouch dogs was also significantly inhibited by the compound. The effect persisted for <7 hr in the case of histamine-stimulation. Oral Z-300 significantly protected the gastric mucosa from water-immersion stress-, indomethacin-, aspirin- and HCl·ethanol-induced lesions and protected the duodenal mucosa against mepirizole- and cysteamine-induced ulcers. These effects on gastric secretion and lesion formation were, as a whole, stronger than those observed with roxatidine. Z-300, but not roxatidine, significantly accelerated the spontaneous healing of acetic acid ulcers induced in rats and prevented the delay in ulcer healing caused by indomethacin. The mechanism of action of Z-300 on acute lesions and chronic ulcers appears to be mostly related to its potent antisecretory and mucosal-protective activities.
- 公益社団法人 日本薬理学会の論文
著者
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Okabe Susumu
Department Of Applied Pharmacology Kyoto College Of Pharmacy
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Igata Hideki
Department Of Cardiovascular Medicine Kyoto University Graduate School Of Medicine
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Kato Shinichi
Department Of Materials Science And Engineering Graduate School Of Engineering Nagoya University
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Shimosako Kenichi
Department Of Applied Pharmacology Kyoto Pharmaceutical University
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SEIKI Masao
Department of Geriatric Medicine, Faculty of Medicine, Kyoto University
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Seiki Masao
Department of Pharmacology, Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.
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Takagi Keiko
Department of Applied Pharmacology, Kyoto Pharmaceutical University
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Yamaji Yoshiaki
Department of Pharmacology, Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.
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Igata Hideki
Department of Applied Pharmacology, Kyoto Pharmaceutical University
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Kato Shinichi
Department of Applied Pharmacology, Kyoto Pharmaceutical University
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