Synthesis and Structure-Activity Relationship of 2-(4-Benzhydryl-1-piperazinyl)-1-phenylethanols as New Calcium Blockers
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概要
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A series of 2-(4-benzhydryl-1-piperazinyl)-1-phenylethanols (4) was synthesized and evaluated for calcium entry-blocking activity, assessed as inhibitory activity on calcium current in rat hippocampal pyramidal neurons by using a patch-clamp technique (10^<-5> M), and cerebral visodilating activity, assessed in terms of increase of vertebral blood flow after intravenous administration (1 mg/kg) in anesthetized dogs. Alkoxy substituents on the phenyl ring of the phenylethanol moiety conferred potent calcium entry-blocking activity and potent cerebral vesodilating activity.Among these compounds, 4i (NC-1100) was selected as the best analog. Some pharmacological properties of 4i are presented.
- 公益社団法人日本薬学会の論文
- 1995-02-15
著者
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三宅 雅久
日本ケミファ(株)研究開発本部企画調査部
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西岡 浩一郎
日本ケミファ(株)研究開発本部企画調査部研究所
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西岡 浩一郎
日本ケミファ 研
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野村 豊
Department Of Applied Chemistry Faculty Of Engineering Saitama University
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野平 博之
Department Of Applied Chemistry Faculty Of Engineering Saitama University
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山川 富雄
Research Laboratories, Nippon Chemiphar Co., Ltd.,
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西岡 浩一郎
Research Laboratories, Nippon Chemiphar Co., Ltd.,
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大村 知広
Research Laboratories, Nippon Chemiphar Co., Ltd.,
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三宅 雅久
Research Laboratories, Nippon Chemiphar Co., Ltd.,
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真崎 光夫
Research Laboratories, Nippon Chemiphar Co., Ltd.,
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山川 富雄
Research Laboratories Nippon Chemiphar Co. Ltd.
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Miyake Norihisa
Research Laboratories Nippon Chemiphar Co. Ltd.
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大村 知広
Research Laboratories Nippon Chemiphar Co. Ltd.
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真崎 光夫
Research Laboratories Nippon Chemiphar Co. Ltd.
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