2019 Fiscal Year Final Research Report
Development of post FDG radiopharmaceuticals-development of radiophameceuticals as p38 activity imageing probe -
| Project/Area Number |
17K10378
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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 |
Radiation science
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| Research Institution | Osaka University of Pharmaceutical Sciences |
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Principal Investigator |
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| Project Period (FY) |
2017-04-01 – 2020-03-31
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| Keywords | SPECT / 炎症性疾患 / P38α / 放射性プローブ / リウマチ / COPD |
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| Outline of Final Research Achievements |
The p38αinduces the production of inflammatory cytokines in response to stimuli, and is known to be activated during the early stages of inflammation. Thus, p38α is a potential target molecule for qualitative diagnosis of inflammatory diseases such as rheumatoid arthritis and chronic obstructive pulmonary disease. In this study, we designed and synthesized a radioiodinated pyrimidinopyridone derivative, namely 123/125I-FIC, as a novel p38α imaging probe. We evaluated the effectiveness of the probe by in vitro activity estimation, an in vivo biodistribution study, and in vivo SPECT/CT imaging in a mouse model of inflammation. Results of this study demonstrate the high synthetic efficiency, high inhibitory potency, high stability, excellent biodistribution profile, and in vivo imaging potency of 123/125I-FIC as a novel p38α imaging probe. 123I-FIC is thus a promising probe for qualitative diagnosis of inflammatory diseases.
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| Free Research Field |
放射性医薬品化学
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| Academic Significance and Societal Importance of the Research Achievements |
p38αは、様々な生命現象において重要な役割を果たしており、多くの疾患に関与する。p38α活性診断用放射性薬剤は、多くの疾患の診断に適用可能と期待され、特定の疾患だけでなく、適用範囲の広い診断薬剤として利用可能である。本研究により開発した放射性薬剤を用いた画像診断により、① 各種疾患の超早期診断 ② 各疾患治療時における早期効果判定 ③ 癌の耐性獲得の判定 が可能となる。さらには、治療薬の効果判定や予測から、治療における不要な投薬を回避することによる医療経済効果も期待できる。また、早期の治療開始により寛解期間も大幅に短縮され、患者の負担はもとより医療費の削減も寄与するものと考えられる。
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