Synthesis of Neurokinin B Analogs and Their Activities as Agonists and Antagonists(Organic,Chemical)

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概要

• 論文の詳細を見る

• Nine neurokinin B (NKB) related octapeptide analogs, substituted with Arg for His^3, or Gly, D-Trp, D-Ala or D-Phe for Phe^6, or Gly for Val^7, or D-Trp or D-Ala for Gly^8 in the original sequence, were synthesized by the solid-phase method. The biological activity of the synthetic analogs was assayed on isolated guinea-pig ileum and rat duodenum. None of the analogs possessed agonistic activity. In the guinea-pig ileum assay, [Arg^3, Gly6^, D-Ala^8]- and [Arg^3, Gly^6, D-Trp^8]-NKB (3-10) were found to act as fairly potent antagonists against NKB, but showed no antagonistic effect against substance P (SP) or neurokinin A (NKA). [Arg^3, D-Ala^6, D-Trp^8]- and [Arg^3, D-Trp^<6-8>, Gly^7]-NKB (3-10) showed antagonistic activities against NKB and SP, and NKB, SP and NKA, respectively, in the ileum assay, while the latter acted as an antagonist against NKB, but not against SP or NKA in the rat duodenum assay.

• 社団法人日本薬学会の論文
• 1987-08-25

著者

• OKIMURA Keiko

  Faculty of Pharmaceutical Sciences, Hokuriku University

• Kanazawa Kazushi

  Faculty Of Pharmaceutical Sciences Hokuriku University

• 黒沢 克郎

  Faculty Of Pharmaceutical Sciences Hokuriku University

• Kurosawa Katsuro

  School Of Pharmacy Hokuriku University

• Ohnishi Kuniharu

  Faculty Of Pharmaceutical Sciences Hokuriku University

• Ohki K

  Faculty Of Pharmaceutical Sciences Hokuriku University

• Okimura Keiko

  Shcool Of Pharmacy Hokuriku University

• Uchida Y

  Hokuriku Univ. Kanazawa Jpn

• HASHIMOTO TADASHI

  School of Pharmacy, Hokuriku University

• UCHIDA YOSHIKI

  School of Pharmacy, Hokuriku University

• Hashimoto T

  Hokuriku Univ. Kanazawa Jpn

• Uchida Yoshiki

  School Of Pharmacy Hokuriku University

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