Metabolic Studies on CS-359,a New β-Adrenergic Blocking Agent. I. Isolation and Identification of the Urinary Metabolites of CS-359
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概要
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On the basis of the spectral examinations of the isolated materials and direct comparisons with chemically synthesized samples, the main metabolites of 5-methyl-8-(2-hydroxy-3-t-butylaminopropoxy) coumarin (CS-359) in excreta of rats and dogs were established as the 5-hydroxymethyl and 5-carboxyl compounds, resulting from oxidation of the 5-methyl group of the parent compound. 8-Oxyacetic acid was also identified as a minor metabolite. Thin-layer chromatograms of the samples from urine and feces exhibited the similar pattern, irrespective of animal species or routes of administrations. Results from fractionation by AcOEt extraction and paper electrophoresis suggested that both neutral and acidic metabolites may be miner components. Experiments on enzymatic hydrolysis indicated that neither giucerchide (s) nor sulfate (s) occurred in significant amounts in excreta. Possible metabolic pathways of CS-359 are presented.
- 公益社団法人日本薬学会の論文
- 1975-06-25
著者
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佐藤 裕信
Central Research Laboratories Sankyo Co. Ltd.
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田中 頼久
三共(株)分析代謝研究所
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岡田 稔
Third Institute of New Drug Research Otsuka Pharmaceutical Co., Ltd.,
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下地 康雄
Research Institute, Sankyo Co., Ltd.,
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林 了三
三共(株)分析代謝研究所
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田中 頼久
Central Research Laboratories, Sankyo Co., Ltd.
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林 了三
Central Research Laboratories, Sankyo Co., Ltd.
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岡田 稔
Central Research Laboratories, Sankyo Co., Ltd.
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中沢 忠正
Central Research Laboratories, Sankyo Co., Ltd.
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下地 康雄
Central Research Laboratories, Sankyo Co., Ltd.
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岡田 稔
Third Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.
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下地 康雄
Research Institute Sankyo Co. Ltd.
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中沢 忠正
Central Research Laboratories Sankyo Co. Ltd.
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Okada Minoru
Third Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.
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