Acid-Promoted Epimerization of Arbaprostil, 15(R)-15-Methylprostaglandin E2, Elicits Gastric Antisecretory Activities in Rats.
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概要
- 論文の詳細を見る
Gastric acid antisecretory activities of 15(R)-15-methylprostaglandin E<SUB>2</SUB> (arbaprostil) preincubated or not preincubated with 0.9% physiological saline, the pH of which was precisely adjusted to less than 4.30, were examined in pylorus-ligated rats, and compared with those of 15(S)-15-methylprostaglandin E<SUB>2</SUB> (15(S), epimer of arbaprostil). 15(S), unlike arbaprostil without preincubation, when s.c.-administered to rats significantly inhibited gastric acid secretion in a dose-dependent manner (30-300 μg/kg). However, arbaprostil preincubated at 37°C for 30 min with 0.9% saline, at pHs of 4.30, 2.75 and 1.20, respectively, showed the following order of pH-dependent antisecretory activities: 1.20 > 2.75 > 4.30. An increase in 15(S) formation from arbaprostil in a pH-dependent manner was also observed by radioisotopic experiments under the same incubation conditions using [<SUP>3</SUP>H]-labeled arbaprostil. The present result suggests that the gastric antisecretory effect of arbaprostil can be mainly explained in terms of the formation of 15(S) after oral administration.
- 公益社団法人 日本薬理学会の論文
著者
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TAKANASHI Hisanori
Department of Hospital Pharmacy
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Kawabe Yoshiki
Department Of Molecular Biology And Medicine Research Center For Advanced Science And Technology Uni
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AKIMA Michitaka
Departinent of Pharmacology, Research Laboratories, Chugai Pharmaceutical Co.
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Akima Michitaka
Department of Pharmacology, Exploratory Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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Kawabe Yoshiki
Department of Pharmacology, Exploratory Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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