Development of selective trapping method for reactive metabolites by fluorous interaction
| Project/Area Number |
15K07911
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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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| Research Field |
Physical pharmacy
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| Research Institution | Fukuoka University |
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Principal Investigator |
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| Research Collaborator |
Hayama Tadashi
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| Project Period (FY) |
2015-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Keywords | グルタチオントラッピング / フルオラス相互作用 / 医薬品反応性代謝物 / 液体クロマトグラフィー／質量分析計 / 反応性代謝物 / フルオラス / 分析化学 / フルオラスケミストリー |
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| Outline of Final Research Achievements |
In this study, utilizing fluorous interaction which is affinity between perfluoroalkyl compounds, an improved method for identification of reactive metabolites by glutathione trapping has been developed. This method includes selective perfluoroalkylation of α-carboxyl group of glutathione-trapped reactive metabolites with fluorous amine reagent through oxazolone chemistry. The obtained derivative could be analyzed selectively and sensitively with LC-MS/MS comparing with conventional methods. The proposed method will be useful for the identification of reactive metabolites in various pharmaceutical product.
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| Academic Significance and Societal Importance of the Research Achievements |
医薬品の開発研究段階で生体内における反応性代謝物の存在を把握しておくことは、上市後の重大な副作用リスクを回避する上で極めて重要視されている。本研究では、これまでに開発・利用されてきた方法を改良し、医薬品の反応性代謝物をより高感度かつ高選択的に検出できる方法を開発した。今後、これまでの方法では検出できなかった既知あるいは未知の医薬品反応性代謝物の分析への応用が期待される。
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Report
(5 results)
Research Products
(31 results)
