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Fundamental Evaluation Aiming at the Development of Ultra-Short-Acting Non-Depolarizing Neuromuscular Blocking Drugs

Research Project

Project/Area Number 18K08832
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 55050:Anesthesiology-related
Research InstitutionJikei University School of Medicine

Principal Investigator

Sunaga Hiroshi  東京慈恵会医科大学, 医学部, 教授 (80317966)

Co-Investigator(Kenkyū-buntansha) 山川 健太郎  東京慈恵会医科大学, 医学部, 准教授 (80570192)
Project Period (FY) 2018-04-01 – 2024-03-31
Project Status Completed (Fiscal Year 2023)
Budget Amount *help
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2021: ¥390,000 (Direct Cost: ¥300,000、Indirect Cost: ¥90,000)
Fiscal Year 2020: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2019: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Keywords筋弛緩薬 / 開発 / 新規化合物 / 超短時間作用 / 超短時間作用型非脱分極性筋弛緩薬 / 合成
Outline of Final Research Achievements

This study aims to develop an ultra-short-acting non-depolarizing neuromuscular blocking drug by creating new compounds and testing their effects using small animals. First, we revealed that the non-depolarizing neuromuscular blocking drug rocuronium delays emergence from general anesthesia in a dose-dependent manner in rats. This possibly results from the direct action of intravenously administered rocuronium on the central nervous system, a side effect of neuromuscular blocking drugs that had not been sufficiently understood before. These findings were published in a journal. Considering these new findings, the chemical formulas of our original compounds were reviewed, and new compounds were subsequently synthesized. It was demonstrated that these new compounds have neuromuscular blocking potency and a short duration of action in rats. They were determined to possess novelty and inventiveness, leading to a patent application.

Academic Significance and Societal Importance of the Research Achievements

特許申請に至った新規筋弛緩薬は、作用の発現が速やかで、効果の制御が容易であり、拮抗薬なしに急速に回復し、蓄積作用がなく、有害作用もない(安全域が広い)などの特徴を備える可能性があり、全身麻酔の簡便性を高め、周術期の安全性向上に寄与することが期待される。また、筋弛緩薬が中枢神経に直接影響を与える可能性を示した知見は、新薬開発において考慮すべき重要な因子を追加する成果となった。

Report

(5 results)
  • 2023 Final Research Report ( PDF )
  • 2021 Research-status Report
  • 2020 Research-status Report
  • 2019 Research-status Report
  • 2018 Research-status Report
  • Research Products

    (3 results)

All 2022 2021 2018

All Journal Article (1 results) (of which Peer Reviewed: 1 results,  Open Access: 1 results) Presentation (1 results) (of which Int'l Joint Research: 1 results) Patent(Industrial Property Rights) (1 results)

  • [Journal Article] Intravenous infusion of rocuronium bromide prolongs emergence from propofol anesthesia in rats2021

    • Author(s)
      Suzuki Kaoru、Sunaga Hiroshi、Yamakawa Kentaro、Suga Yoshifumi、Kondo Ichiro、Tsubokawa Tsunehisa、Uezono Shoichi
    • Journal Title

      PLOS ONE

      Volume: 16 Issue: 2 Pages: e0246858-e0246858

    • DOI

      10.1371/journal.pone.0246858

    • Related Report
      2020 Research-status Report
    • Peer Reviewed / Open Access
  • [Presentation] Effect of rocuronium on emergence from propofol anesthesia in rats2018

    • Author(s)
      鈴木薫、須永宏、山川健太郎、須賀芳文、桒原雄希、近藤一郎
    • Organizer
      米国麻酔科学会
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research
  • [Patent(Industrial Property Rights)] 筋弛緩薬2022

    • Inventor(s)
      須永 宏
    • Industrial Property Rights Holder
      学校法人慈恵大学
    • Industrial Property Rights Type
      特許
    • Filing Date
      2022
    • Related Report
      2021 Research-status Report

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Published: 2018-04-23   Modified: 2025-01-30  

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