Studies on Analgesic Oligopeptides. VI. : Further Studies of Synthesis and Biological Properties of Tripeptide Alkylamides, Try-D-Arg-Phe-X

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概要

• 論文の詳細を見る

• Nine analogs based on a structure of Tyr-D-Arg-Phe-X (X=alkylamides or alkylhydrazide containing electoron-withdrawing atoms or groups) were newly synthesized and their biological properties were examined by the opioid receptor binding properties of μ-, δ- and κ-receptors, guinea-pig ileum (GPI) assay and analgesic activity in the tail pinch test after subcutaneous administration in mice. Analogs with X=NHCH_2CF_3,Sar-ol, or NH(CH_2)_2CN showed potent activities in the GPI and analgesic assays and high affinity for μ-receptor. An analog with X=taurinamide was found to possess 4-fold higher μ-receptor selectivity than that of [D-Ala^2,MePhe^4,Gly-ol^5]enkephalin (DAGO). The receptor binding properties of previously reported analogs [Chem. Pharm. Bull., 33,1528 (1985); ibid., 33,4865 (1985); ibid., 36,4834 (1988)] were also examined for overall discussion of the structure-activity relationships of this series of tripeptide amides.

• 社団法人日本薬学会の論文
• 1990-08-25

著者

• 鈴木 謙次

  東北薬科大学

• 安保 明博

  Tohoku College of Pharmacy

• 佐々木 有亮

  Tohoku College of Pharmacy

• 鈴木 謙次

  Tohoku College of Pharmacy

• 河野 弘之

  Tohoku College of Pharmacy

• 大久保 恭仁

  Tohoku College of Pharmacy

• 藤田 浩毅

  Tohoku College of Pharmacy

• 日野 正孝

  Zenyaku Kogyo Co., Ltd.,

• 日野 正孝

  Zenyaku Kogyo Co. Ltd.

• 大久保 恭仁

  東北薬大

• 大久保 恭仁

  東北薬科大学 放射薬品

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