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Elucidation of molecular pharmacological profile of mu opioid receptor agonists, and clinical applications thereof

Research Project

Project/Area Number 17K11105
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Anesthesiology
Research InstitutionUniversity of Toyama

Principal Investigator

Yamazaki Mitsuaki  富山大学, 学術研究部医学系, 教授 (70158145)

Co-Investigator(Kenkyū-buntansha) 成田 年  星薬科大学, 薬学部, 教授 (40318613)
Project Period (FY) 2017-04-01 – 2020-03-31
Project Status Completed (Fiscal Year 2019)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Keywordsμオピオイド受容体作動薬 / TRV130 / βアレスチン / 薬理学的プロファイル / オピオイド鎮痛薬 / Ligand-biased efficacy / cAMP / β-arrestin / μオピオイド受容体
Outline of Final Research Achievements

Increasing action of β-arrestin recruitment with fentanyl and methadone was increased by combination of loperamide and oxycodone. On the other hand, β-arrestin recruitment increasing action by fentanyl was remarkably decreased by hydromorphone together with fentanyl. After calculating the side effect coefficient based on constipation and painkilling strength of each strong opioid, and then analyzing the correlation of the bias coefficient by each strong opioid, no significant differences were observed between these coefficients. After performing comparison between morphine and TRV130 about painkilling, constipation, vomiting, nausea and spontaneous momentum, big differences were not recognized between two drugs.

Academic Significance and Societal Importance of the Research Achievements

本研究では、オピオイド受容体作動薬の薬理学的プロファイルを検討した。この研究成果から、オピオイド製剤の適正使用の理解が深まり、オピオイド使用に関するアルゴリズムの確立に寄与できたものと思われる。そして、オピオイドの適正使用や効率的なオピオイドスイッチングに有用な情報を与える事が出来るものと考える。

Report

(4 results)
  • 2019 Annual Research Report   Final Research Report ( PDF )
  • 2018 Research-status Report
  • 2017 Research-status Report
  • Research Products

    (2 results)

All 2019

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (1 results) (of which Invited: 1 results)

  • [Journal Article] ペンタゾシンおよびブプレノルフィン注射薬連用による偽依存から,フェンタニル貼付薬へのオピオイドスイッチングとミルタザピン内服薬併用により自宅退院に至った症例2019

    • Author(s)
      竹村佳記,青木優太,伊東久勝,堀川英世,服部瑞樹,山崎光章
    • Journal Title

      日本ペインクリニック学会誌

      Volume: 26 Pages: 48-52

    • NAID

      130007610628

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed
  • [Presentation] 痛みのテーラーメイド医療の実現を目指す:患者個別の“痛み関連シグナル”の多次元解析.2019

    • Author(s)
      竹村佳記,成田 年,山崎光章.
    • Organizer
      第41回日本疼痛学会
    • Related Report
      2019 Annual Research Report
    • Invited

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Published: 2017-04-28   Modified: 2021-02-19  

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