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2013 Fiscal Year Final Research Report

Development of PET molecular probes for imaging alpha-synuclein in the brain

Research Project

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Project/Area Number 23659605
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Radiation science
Research InstitutionTokyo Metropolitan Geriatric Hospital and Institute of Gerontology

Principal Investigator

TOYOHARA Jun  地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 専門副部長 (50425659)

Co-Investigator(Renkei-kenkyūsha) ISHIWATA Kiichi  地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究部長 (50143037)
SAKATA Muneyuki  地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究員 (00403329)
ISHII Kenji  地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究部長 (10231135)
ODA Keiichi  地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究員 (70224235)
Project Period (FY) 2011 – 2013
Keywords放射性医薬品・造影剤
Research Abstract

Five phenothiazine and a polyphenol derivatives were radiolabeled as potential PET molecular imaging probes for alpha-synuclein imaging in the brain. The four of five phenothiazine derivatives were successfully radiolabeled by 11C-methyl iodide or 11C-methyl triflate in a good yield with high specific activity. Dedicated small animal PET imaging showed these phenothiazine derivatives crossed the blood-brain barrier (BBB) with rapid washout from the brain. Another one-phenothiazine and polyphenol derivatives did not cross the BBB.
In conclusion, our initial studies suggested that phenothiazine derivatives are good candidate for in vivo imaging of alpha-synuclein aggregation in the brain. Further structural optimizations of these compounds are needed.

  • Research Products

    (10 results)

All 2013 2012

All Journal Article (3 results) (of which Peer Reviewed: 2 results) Presentation (6 results) Book (1 results)

  • [Journal Article] Application of [^<11>C]SA4503 to selection of novel sigma1 selective agonists2012

    • Author(s)
      Toyohara, J., Kobayashi, T., Mita, S. and Ishiwata K
    • Journal Title

      Nucl. Med. Biol

      Volume: Vo.39 Pages: 1117-1121

    • DOI

      10.1016/j.nucmedbio.2012.06.004

    • Peer Reviewed
  • [Journal Article] Re-evaluation of in vivo selectivity of [^<11>C]SA4503 to sigma1 receptors in the brain : contributions of emopamil binding protein2012

    • Author(s)
      Toyohara, J., Sakata, M. and Ishiwata, K
    • Journal Title

      Nucl. Med. Biol

      Volume: Vol.39 Pages: 1049-1052

    • DOI

      10.1016/j.nucmedbio.2012.03.002

    • Peer Reviewed
  • [Journal Article] Roles of sigma1 receptors in the mechanisms of action of CNS drugs2012

    • Author(s)
      Toyohara, J., Sakata, M. and Ishiwata, K
    • Journal Title

      Trans. Neurosci

      Volume: Vol.3 Pages: 294-299

    • DOI

      10.2478/s13380-012-0030-0

  • [Presentation] PET プローブ開発の基礎2013

    • Author(s)
      豊原 潤
    • Organizer
      PETサマーセミナー2013
    • Place of Presentation
      金沢
    • Year and Date
      20130823-25
  • [Presentation] Synthesis and evaluation of a fluorine-18-labeled 7α-(3-fluoropropyl)estradiol2013

    • Author(s)
      Okamoto, M., Matsui, A., Kitagawa, Y., Toyohara, J., Ishiwata, K., Yoshimoto, M. and Shimizu, I
    • Place of Presentation
      Jeju
    • Year and Date
      20130512-17
  • [Presentation] 新規PET 薬剤開発からfirst-in-human study まで―多施設共同研究への取り組み―2012

    • Author(s)
      豊原 潤、坂田宗之、織田圭一、石井賢二、石渡喜一
    • Organizer
      第52回日本核医学会学術総会
    • Place of Presentation
      札幌
    • Year and Date
      20121011-13
  • [Presentation] 化学薬学セッション : PET 薬剤の理解のために―PET 医師のための化学薬学の時間―2012

    • Author(s)
      豊原 潤
    • Organizer
      PET サマーセミナー2012
    • Place of Presentation
      松本
    • Year and Date
      20120831-0902
  • [Presentation] Dose sigma1 ligand [^<11>C]SA4503 bind to the emopamil binding protein in the brain in vivo?2012

    • Author(s)
      Toyohara, J., Sakata, M. and Ishiwata, K
    • Organizer
      The 9th international symposium on fuctional neuroreceptor mapping of the living brain
    • Place of Presentation
      Baltimore
    • Year and Date
      20120809-11
  • [Presentation] Sigma receptors2012

    • Author(s)
      Toyohara J
    • Organizer
      International symposium on PET and SPECT in neurology and psychiatry
    • Place of Presentation
      Groningen
    • Year and Date
      20120423-25
  • [Book] Trends on the role of PET in drug development2012

    • Author(s)
      Toyohara, J. and Ishiwata, K
    • Total Pages
      193-218
    • Publisher
      World scientific publishing Co

URL: 

Published: 2015-06-25  

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