Synthesis and Antidiuretic Activities of Novel Glycoconjugates of Arginine-Vasopressin

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概要

• 論文の詳細を見る

• Arginine-vasopressin (AVP) was acylated with various acyl azides (2a-j) in pH 9.1 buffer to give AVP derivatives (11a-j) modified at the tyrosine side chain with a carbohydrate via a spacer arm. Glycoconjugates of AVP modified at the N-terminal amide (12a-e) were also synthesized from AVP and carboxylic acids (3a-e) using dicyclohexylcarbodiimide and 1-hydroxybenzotriazole as coupling agent. Analogues (11a-j) exhibited greater in vivo antidiuretic activity than AVP. AVP and glycoconjugates (12a-e) were stable in rat plasma. On the other hand, glycoconjugates (11a-i) were found to readily convert to AVP according to first order kinetics. Hence, 11a-j are considered to be prodrugs of AVP.

• 公益社団法人日本薬学会の論文
• 1998-10-15

著者

• 山田 治民

  (株) ディ・ディ・エス研究所

• Suzuki Kazutoshi

  放射線医学総合研究所分子イメージング研究センター

• Suzuki K

  Pharmaceutical Frontier Research Laboratories Japan Tobacco Inc.

• Yamada H

  Yamada Apiculture Center Inc.

• Suzuki Kenji

  Suntory Institute For Biomedical Research Wakayamadai

• Suzuki K

  Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)pharmaceutics Resear

• Suzuki Kokichi

  Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)pharmaceutics Resear

• Suzuki Kazutoshi

  Department Of Medical Imaging National Institute Of Radiological Sciences

• Suzuki Kazutoshi

  Clinical Neuroimaging Section Department Of Molecular Neuroimaging Molecular Imaging Center National

• Yamada H

  School Of Science And Technology Kwansei Gakuin University

• Ikeda Masahiro

  Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)new Product Research

• Suzuki K

  Molecular Imaging Center National Institute Of Radiological Sciences

• Yamada Harutami

  Drug Delivery System Institute Ltd.:(present Address)tanabe Seiyaku Co. Ltd.

• SUSAKI Hiroshi

  Noda Research Laboratories, Drug Delivery System Institute, Ltd.

• YAMADA Harutami

  Noda Research Laboratories, Drug Delivery System Institute, Ltd.

• WATANABE Hiroshi

  Noda Research Laboratories, Drug Delivery System Institute, Ltd.

• Susaki H

  Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)new Product Research

• Watanabe Hiroshi

  Noda Research Laboratories Drug Delivery System Institute Ltd.:(present Address)patent Department Me

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