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Development of a practical myocardial blood flow imaging agent based on novel F18-labeled phosphonium synthesis method

Research Project

Project/Area Number 16H05386
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Research Field Radiation science
Research InstitutionTohoku University

Principal Investigator

Furumoto Shozo  東北大学, サイクロトロン・ラジオアイソトープセンター, 教授 (00375198)

Research Collaborator TOMINIGA TAKAHIRO  
HARADA RYUICHI  
Project Period (FY) 2016-04-01 – 2019-03-31
Project Status Completed (Fiscal Year 2018)
Budget Amount *help
¥17,160,000 (Direct Cost: ¥13,200,000、Indirect Cost: ¥3,960,000)
Fiscal Year 2018: ¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2017: ¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
Fiscal Year 2016: ¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
KeywordsPET / 心筋血流 / ミトコンドリア / PETイメージング / 心筋イメージング / ホスホニウム / 心臓 / イメージング / 18F
Outline of Final Research Achievements

Myocardial imaging is an important technology for accurate diagnosis of ischemic heart disease and assessment of ischemic condition and myocardial viability. In this study, we worked on the development of a novel 18Flabeled tracer (18F-TAP) that can be used in PET nuclear medicine blood flow imaging. First, we synthesized 20 types of TAP derivatives of unlabeled form as standard compounds, and then actually succeeded to radiosynthesize 18 compounds of 18F-labeled forms among them. Then, we compared their pharmacokinetics in mice were evaluated by ex vivo biodistribution study. As a result, 18F-TAP-X showed high accumulation in heart tissue with high selectivity. 18F-TAP-X accumulated in cardiomyocytes in a mitochondrial membrane voltage-dependent manner, and in animal PET, it afforded a clear PET images of heart. From these results, we succeeded in developing the target myocardial imaging agent.

Academic Significance and Societal Importance of the Research Achievements

心臓核医学検査は心疾患の有益な診断方法として不可欠なものだが、本研究成果は、将来的に性能の高いPETによる心臓核医学検査の発展と普及に大きく貢献する可能性を秘めている。現在、国内では実用的な18F標識PET薬剤がなかったために臨床での心臓核医学研究は行われていないが、本研究で開発した18F標識PET薬剤を利用すれば、実用的な臨床心臓核医学研究が展開できる。さらにその臨床研究を礎として、将来的には、現在よりも質の高いPET心臓核医学検査が広く一般診療で利用されるようになると期待される。

Report

(4 results)
  • 2018 Annual Research Report   Final Research Report ( PDF )
  • 2017 Annual Research Report
  • 2016 Annual Research Report
  • Research Products

    (12 results)

All 2019 2018 2017 2016

All Presentation (11 results) (of which Int'l Joint Research: 2 results,  Invited: 3 results) Patent(Industrial Property Rights) (1 results) (of which Overseas: 1 results)

  • [Presentation] Fluorine-18 Labeled PET Tracers for Imaging Mitochondria2019

    • Author(s)
      古本祥三
    • Organizer
      3th International Symposium on Molecular Imaging, La Habana, Cuba
    • Related Report
      2018 Annual Research Report
    • Invited
  • [Presentation] 18F-ホスホニウム型MPIトレーサーの開発と18F-Flurpiridazとの動態比較2018

    • Author(s)
      伊東由夏、冨永隆裕、石川洋一、岩田錬、石渡喜一、古本祥三
    • Organizer
      第58回日本核医学会学術総会
    • Related Report
      2018 Annual Research Report
  • [Presentation] F-18標識PETトレーサー開発の最前線2018

    • Author(s)
      古本祥三
    • Organizer
      In vivoイメージングフォーラム2018
    • Related Report
      2018 Annual Research Report
  • [Presentation] 心筋血流イメージング剤18F-TAP-31の開発と18F-Flurpiridazとの比較評価2018

    • Author(s)
      冨永隆裕、秋田諒、石川洋一、岩田錬、石渡喜一、古本祥三
    • Organizer
      第13回日本分子イメージング学会総会・学術集会
    • Related Report
      2018 Annual Research Report
  • [Presentation] New 18F-Labeled PET Tracers for Myocardial Perfusion Imaging2018

    • Author(s)
      古本祥三
    • Organizer
      National Cyclotron and PET Centre Academic Conference 2018, Chulabhorn Graduate Institute, Bangkok
    • Related Report
      2018 Annual Research Report
    • Invited
  • [Presentation] Development of novel 18F-labeled phosphonium derivatives for mitochondria imaging by positron emission tomography2017

    • Author(s)
      Takahiro Tominaga, Ryo Akita, Yoichi Ishikawa, Ren Iwata, Kiichi Ishiwata, Shozo Furumoto
    • Organizer
      22st International Symposium on Radiopharmaceutical Sciences
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Novel 18F-labeled triarylphosphonium derivatives for mitochondria imaging2017

    • Author(s)
      S. Furumoto, T. Tominaga, R. Akita, A. Kazama, Y. Ishikawa, R., Iwata, K. Ishiwata
    • Organizer
      30th Annual EANM Congress of the European Association of Nuclear Medicine 2017
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 基礎研究におけるPET薬剤の生物学的評価手法2017

    • Author(s)
      古本 祥三
    • Organizer
      第57回日本核医学会学術総会
    • Related Report
      2017 Annual Research Report
    • Invited
  • [Presentation] 18F標識ホスホニウム型プローブの構造最適化と集積メカニズムの検証2017

    • Author(s)
      冨永 隆裕,秋田 諒,石川 洋一,岩田 錬,石渡 喜一,古本 祥三
    • Organizer
      第57回日本核医学会学術総会
    • Related Report
      2017 Annual Research Report
  • [Presentation] フッ素18標識心筋イメージング剤の開発2016

    • Author(s)
      古本祥三
    • Organizer
      第56回日本核医学会学術総会
    • Place of Presentation
      愛知県名古屋市
    • Year and Date
      2016-11-03
    • Related Report
      2016 Annual Research Report
  • [Presentation] ミトコンドリアを標的とした新規18F標識ホスホニウム型プローブの開発2016

    • Author(s)
      冨永隆裕、風間あずさ、石川洋一、岩田錬、石渡喜一、古本祥三
    • Organizer
      第56回日本核医学会学術総会
    • Place of Presentation
      愛知県名古屋市
    • Year and Date
      2016-11-03
    • Related Report
      2016 Annual Research Report
  • [Patent(Industrial Property Rights)] PHOSPHONIUM COMPOUND AND PRODUCTION METHOD THEREFOR2017

    • Inventor(s)
      Shozo FURUMOTO
    • Industrial Property Rights Holder
      TOHOKU UNIVERSITY
    • Industrial Property Rights Type
      特許
    • Filing Date
      2017
    • Related Report
      2017 Annual Research Report
    • Overseas

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Published: 2016-04-21   Modified: 2021-01-27  

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