Studies on a New 1,5-Benzothiazepine Derivative (CRD-401). IV. Coronary Vasodilating Effect and Structure-Activity Relationship
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概要
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The coronary vasodilating action of 1,5-benzothiazepine derivatives and the structureactivity relationship were examined in the anesthetized dog. 2-(4-Methoxyphenyl), 3-acyloxy or alkyloxy, 5-dimethylaminoethyl and 7-hydrogen moieties were important for vasodilation. The action of the derivatives was found to be stereospecific for the d-cis-isomer. Based on these findings, it can be concluded that d-3-acetoxy-cis-2,3-dihydro-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one hydrochloride (CRD-401) was the most potent compound among the derivatives tested. The metabolites of dl-isomer of CRD-401,i.e. deacetyl and deacetyl-O- or N-demethyl compounds, were less active and less toxic than the parent compound.
- 公益社団法人日本薬学会の論文
- 1973-01-25
著者
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清本 昭夫
Research Laboratories, Tanabe Seiyaku, Co., Ltd.
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清本 昭夫
Research Laboratories Tanabe Seiyaku Co. Ltd.
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長尾 拓
Department Of Toxicology And Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo
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長尾 拓
The Biological Research Laboratory, Tanabe Seiyuku, Co., Ltd.
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佐藤 匡徳
The Biological Research Laboratory, Tanabe Seiyuku, Co., Ltd.
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中島 宏通
The Biological Research Laboratory, Tanabe Seiyuku, Co., Ltd.
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清本 昭夫
The Biological Research Laboratory, Tanabe Seiyuku, Co., Ltd.
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中島 宏通
The Biological Research Laboratory Tanabe Seiyuku Co. Ltd.
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佐藤 匡徳
The Biological Research Laboratory Tanabe Seiyuku Co. Ltd.
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