Nonpeptide Arginine Vasopressin Antagonists for Both V_<1A> and V_2 Receptors : Synthesis and Pharmacological Properties of 2-Phenyl-4'-[(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide Derivatives

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概要

• 論文の詳細を見る

• A series of compounds structurally relate to 4'-[(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V_<1A> and V_2 receptors. The introduction of a phenyl or a 4-substituted phenyl group into the ortho position of the benzoyl moiety resulted in an increase in both binding affinity and antagonistic activity. The 2-(4-methylphenyl) derivative (1g) exhibited high antagonistic activities for both V_<1A> (8.6-fold) and V_2 (38-fold) receptors and high oral activity (8.6-fold) compared with the 2-methyl lead compound (1a). Datail of the synthesis and the pharmacological properties of this series are presented.

• 公益社団法人日本薬学会の論文
• 1997-11-15

著者

• TANAKA Akihiro

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

• Tanaka A

  Yamanouchi U.k. Ltd. Surrey Gbr

• 増田 明

  富山医科薬科大学麻酔科

• SHIMADA Yoshiaki

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

• MATSUHISA Akira

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

• KIKUCHI Kazumi

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

• YATSU Takeyuki

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

• Kikuchi Kazumi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Yatsu Takeyuki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Matsuhisa Akira

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Matsuhisa Akira

  Gastrointestinal Research Laboratories Institute For Drug Discovery Research Yamanouchi Pharmaceutic

• Tanaka Akihiro

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Yanagisawa Isao

  Corporate Planning Dept.

• Shimada Yoshiaki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Yatsu Takeyuki

  Astellas Pharma Inc. Ibaraki Jpn

• Tahara Atsuo

  Drug Discovery Research Astellas Pharma Inc.

• Matsuhisa Akira

  Institute For Drug Discovery Research Astellas Pharma Inc.

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