Synthesis and Pharmacological Evaluation of 2-(3-Piperidyl)-1,2,3,4-tetrahydroisoquinoline Derivatives as Specific Bradycardic Agents

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概要

• 論文の詳細を見る

• Novel 1,2,3,4-tetrahydroisoquinoline derivatives hearing directly a cyclic amine at the 2-position were prepared and examined for their bradycardic activities in isolated right atria and in anesthetized rats. The structure-activity relationships (SAR) study revealed that the 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinoline skeleton is essential for the appearance of potent in vitro activity, and that the presence of at least one methoxy group at the 6- or 7-position of the 1,2,3,4-tetrahydroisoquinoline ring is important to exert potent in vitro activity. In vivo tests of selected compounds demonstrated that 2-(l-henzyl-3-piperidyl)-6,7-dimethoxy-1,2,3,4-tetrahydroiso- quinoline (6c) exhibited potent bradycardic activity with negligible influence on mean blood pressure in rats, although its potency is a half of that of Zatebradine.

• 公益社団法人日本薬学会の論文
• 2003-04-01

著者

• 渡辺 敏子

  School Of Pharmaceutical Sciences Toho University

• Tanaka A

  Faculty Of Pharmaceutical Sciences Tokyo University Of Science

• Watanabe Toshifumi

  Pharmaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemical Industries

• Yanagisawa I

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Yanagisawa Isao

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

• Yanagisawa Isao

  山之内製薬

• Watanabe T

  Chiba Univ. Chiba Jpn

• Watanabe Toshiko

  Faculty Of Pharmaceutical Sciences Chiba University

• Watanabe Toshiko

  Graduate School Of Pharmaceutical Sciences Chiba University

• Watanabe Toshihiro

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• KAKEFUDA Akio

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• Kakefuda Akio

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Taguchi Y

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• TAGUCHI Yasuko

  Institute for Drug, Discovery Research, Yamanouchi Pharmaceutical Co. Ltd.

• MASUDA Noriaki

  Institute for Drug, Discovery Research, Yamanouchi Pharmaceutical Co. Ltd.

• TANAKA Akihiro

  Yamanouchi U. K. Ltd.

• Masuda N

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

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