2023 Fiscal Year Final Research Report
Establishment of simultaneous quantitative determination method and pharmacokinetic model for anti-doping drug clenbuterol metabolites
| Project/Area Number |
21K11375
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 59020:Sports sciences-related
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| Research Institution | Nihon University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
宮本 葵 日本大学, 薬学部, 講師 (20513914)
青山 隆彦 日本大学, 薬学部, 准教授 (70384633)
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| Project Period (FY) |
2021-04-01 – 2024-03-31
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| Keywords | クレンブテロール / 薬物代謝 / 薬物動態 / アンチドーピング |
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| Outline of Final Research Achievements |
In this study, we attempted to chemically synthesize the nitro derivative of clenbuterol, which is one of the oxidative metabolites. According to retrosynthetic analysis and investigation using benzoic acid derivatives as starting materials, we were able to synthesized the desired nitro derivative on a gram scale in 5 steps with a total yield of 41%. Also, we carried out optical resolution of the synthesized nitro derivative, clarified its absolute configuration, and succeeded in establishing a preparation to optically active clenbuterol. We found conditions applicable to the simultaneous measurement of nitro metabolite and clenbuterol in rat liver microsomes, and clarified that it is possible to predict the metabolite pharmacokinetics using a model experiment using acetaminophen.
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| Free Research Field |
医薬品化学
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| Academic Significance and Societal Importance of the Research Achievements |
治療目的ではなく競技能力の向上を目的として摂取される薬物、いわゆるドーピング禁止薬の代謝物に関する知見は非常に乏しい。本研究では、気管支拡張薬として用いられる一方で、筋肉増強薬としてドーピング禁止薬に指定されているクレンブテロールとその代謝物に着目し研究を遂行した。本研究により得られた知見は、「うっかりドーピング」を含めたドーピング検査においてより正確な判定を可能とし、公正なスポーツを行うための活動に寄与できるものと考える。
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