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

2023 Fiscal Year Final Research Report

• Project/Area Number: 18K08832
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 55050:Anesthesiology-related
• Research Institution: Jikei 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
• Keywords: 筋弛緩薬 / 開発 / 新規化合物 / 超短時間作用

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.

Free Research Field

麻酔科学

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。