Synthesis of the Optically Active trans-Isomers of Diltiazem and Their Cardiovascular Effects and Ca-Antagonistic Activity
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概要
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Optically active trans-isomers of diltiazem were synthesized and their cardiovascular effects were evaluated in anesthetized dogs and in isolated guinea pig hearts.Both (+)-2 (2R, 3S) and (-)-2 (2S, 3R) were much less active than diltiazem (1,2D, 3S) with short duration of action. No substantial enantiomeric difference in activity was seen between them. Their Ca-antagonistic activities on Ca^<2+>-induced contractions in K^+ -depolarized canine basilar arteries were also examined.Absolute stereochemistry of (+)-2 was determined to be 2R, 3S by X-ray crystallographic analysis.
- 1992-06-25
著者
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井上 博純
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd, .
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武田 幹男
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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岡村 公生
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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伊達 忠正
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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長尾 拓
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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青江 啓一
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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釘田 博至
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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長尾 拓
Biological Research Laboratory:tanabe Seiyaku Co. Ltd. :(present Adress)department Of Toxicology And
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田中 崇嗣
Organic Chemistry Research Laboratory
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村田 栄
Biological Research Laboratory
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山口 孝司
Biological Research Laboratory
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吉川 公平
Biological Research Laboratory
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中島 滋代
Biological Research Laboratory
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村田 栄
Pharmacological Research Laboratory Tanabe Seiyaku Co. Ltd.
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岡村 公生
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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田中 崇嗣
Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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釘田 博至
田辺製薬有機研究所
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田中 崇嗣
Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.
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武田 幹男
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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釘田 博至
Organic Chemistry Research Laboratory:tanabe Seiyaku Co. Ltd.
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伊達 忠正
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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青江 啓一
Organic Chemistry Research Laboratory:tanabe Seiyaku Co. Ltd.
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吉川 公平
Biological Research Laboratory:tanabe Seiyaku Co. Ltd.
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井上 博純
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd .
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釘田 博至
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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山口 孝司
Biological Research Laboratory:tanabe Seiyaku Co. Ltd.
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中島 滋代
Biological Research Laboratory:tanabe Seiyaku Co. Ltd.
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