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Development of the Colin transporter imaging agent for early diagnosis of Alzheimer's disease

Research Project

Project/Area Number 23591813
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Radiation science
Research InstitutionKanazawa University

Principal Investigator

SHIBA Kazuhiro  金沢大学, 学際科学実験センター, 教授 (40143929)

Co-Investigator(Kenkyū-buntansha) KITAMURA Yoji  金沢大学, 学際科学実験センター, 准教授 (10368483)
KOZAKA Takashi  金沢大学, 学際科学実験センター, 助教 (50579836)
Project Period (FY) 2011 – 2013
Project Status Completed (Fiscal Year 2013)
Budget Amount *help
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2011: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywordsアルツハイマー病 / コリン作動性神経 / 分子イメージング / アセチルコリントランスポーター / SPECT / コリン作動性神経系 / SPECT / PET
Research Abstract

We aimed at the development of the imaging probe for early diagnosis of Alzheimer's disease (AD). The cognitive impairment of AD is related to the cholinergic nerve system. we targeted the cholin transporter(ChT) and the acetylcholine transporter(VAChT) which exist in pre-synapse in cholinergic nerve. We synthesized the imaging probes with high affinity for ChT or VAChT. We could not develope a probe with high affinity for ChT in in vitro assays. However, I could synthesize a probe with high affinity for VAChT such as (-)-o-iododecalinvesamicol(OIDV). Radioiodinated OIDV ((-)-[I-125]OIDV) accumulated in rat brain through B.B.B. In vivo blocking and ex vivo autoradiography study showed that (-)-[I-125]OIDV selevtively accumulated in the VAChT in rat brain. These results showed that (-)-[I-125]OIDV bound selectively to VAChT in rat brain in vivo. Radioiodinated (-)-OIDV labeled with I-123 was suggested to be useful as a VAChT imaging agent for SPECT.

Report

(4 results)
  • 2013 Annual Research Report   Final Research Report ( PDF )
  • 2012 Research-status Report
  • 2011 Research-status Report
  • Research Products

    (24 results)

All 2014 2013 2012 2011

All Journal Article (4 results) (of which Peer Reviewed: 4 results) Presentation (20 results)

  • [Journal Article] Regional brain imaging of vesicular acetylcholine transporter (VAChT) using o-[^<12>5I]iodo-trans-decalin vesamicol as a new potential imaging probe2014

    • Author(s)
      Kozaka, T., Uno, I., Kitamura, Y., Miwa, D., Azim,MA., Ogawa, K. Shiba. K
    • Journal Title

      Synapse

      Volume: Vol. 68 Issue: 3 Pages: 107-113

    • DOI

      10.1002/syn.21720

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Regional brain imaging of vesicular acetylcholine transporter (VAChT) using o-[125I]iodo-trans-decalinvesamicol as a new potential imaging probe.2014

    • Author(s)
      Takashi Kozaka, Izumi Uno, Yoji Kitamura, Daisuke Miwa, Mohammad Anwar-ul Azim, Kazuma Ogawa, Kazuhiro Shiba.
    • Journal Title

      Synapse

      Volume: 68 Pages: 107-113

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT)2012

    • Author(s)
      Kozaka, T., Uno, I., Kitamura, Y., Miwa, D., Ogawa, K., Shiba, K
    • Journal Title

      Bioorganic & Medicinal Chemistry

      Volume: Vol.20 Issue: 16 Pages: 4936-4941

    • DOI

      10.1016/j.bmc.2012.06.040

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).2012

    • Author(s)
      Takashi Kozaka, Izumi Uno, Yoji Kitamura, Daisuke Miwa, Kazuma Ogawa, Kazuhiro Shiba.
    • Journal Title

      Bioorganic & Medicinal Chemistry

      Volume: 20 Pages: 4936-4941

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Presentation] Evaluation of radiolabeled o-bromo- decalinvesamicol (OBDV) as a PET ligand for the Vesicular Acetylcholine Transporter (VAChT)2014

    • Author(s)
      Azim, MA., Kozaka, T., Uno, I., Miwa, D., Kitamura, Y., Ogawa, K., Kawai, K., Makino, A., Kiyono, Y and Shiba, K
    • Organizer
      International Workshop on Molecular Functional Imaging for Brain and Gynecologic Oncology
    • Place of Presentation
      ユアーズホテルフクイ(福井市)
    • Related Report
      2013 Final Research Report
  • [Presentation] Evaluation of radiolabeled o-bromo-decalinvesamicol (OBDV) as a PET ligand for the Vesicular Acetylcholine Transporter (VAChT).2014

    • Author(s)
      Mohammad Anwar-ul Azim , Takashi Kozaka, Izumi Uno, Daisuke Miwa, Yoji Kitamura, Kazuma Ogawa, Keiichi Kawai, Akira Makino, Yasushi Kiyono, Kazuhiro Shiba.
    • Organizer
      International Workshop on Molecular Functional Imaging for Brain and Gynecologic Oncology.
    • Place of Presentation
      ユアーズホテルフクイ、福井市、福井県
    • Related Report
      2013 Annual Research Report
  • [Presentation] 脳内小胞アセチルコリントランスポーター(VAChT)のPETイメージングプローブ[^<11>C]OMDVの開発2013

    • Author(s)
      三輪大輔,小阪孝史,鵜野いずみ,北村陽二, Azim Mohammad A.,河村和紀,小川数馬,川井恵一,柴和弘
    • Organizer
      第11回次世代を担う若手のためのフィジカル・ファーマフォーラム
    • Place of Presentation
      清水テルサおよび三保園ホテル(静岡市)
    • Related Report
      2013 Final Research Report
  • [Presentation] VAChTイメージング用[^<125>I]OIDVのジアステレオマー分離とin vivo脳内動態変化2013

    • Author(s)
      鵜野いずみ、小阪孝史、三輪大輔、北村陽二、Azim Mohammad A、小川数馬、川井恵一、柴和弘
    • Organizer
      第11回次世代を担う若手のためのフィジカル・ファーマフォーラム
    • Place of Presentation
      清水テルサおよび三保園ホテル(静岡市)
    • Related Report
      2013 Final Research Report
  • [Presentation] The development of potential vesicular acetylcholine transporter (VAChT) PET imaging probes2013

    • Author(s)
      Kozaka T, Miwa D, Uno I, Kitamura Y, Azim MA, Ogawa K, Kinuya S, Kawai K, Shiba K
    • Organizer
      2013 SNMMI 60th annual meeting. Vancouber Convention Centre
    • Place of Presentation
      Vancouber, BC, Canada
    • Related Report
      2013 Final Research Report
  • [Presentation] In vivo evaluation of radioiodinated o-iodo-trans- decalinvesamicol(OIDV)as a vesicular acetylcholine transporter (VAChT) imaging agent2013

    • Author(s)
      Uno I, Kozaka T, Kitamura Y, Miwa D, Azim MA, Ogawa K, Kawai K, Taki J, Kinuya S, Shiba K
    • Organizer
      2013 SNMMI 60th annual meeting
    • Place of Presentation
      Vancouber Convention Centre, Vancouber, BC, Canada
    • Related Report
      2013 Final Research Report
  • [Presentation] アルツハイマー病の早期診断を目的とした新規PET用VAChTイメージング剤[^<11>C]OMDVの合成とin vivo評価2013

    • Author(s)
      小阪孝史、三輪大輔、鵜野いずみ、北村陽二、Mohammad Anwer-ul AZIM,川村和紀、小川数馬、川井恵一、柴和弘
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      パシフィコ横浜、横浜市
    • Related Report
      2013 Final Research Report
  • [Presentation] OIDVのジアステレオマー分離とその選択的VAChTイメージング剤としての評価2013

    • Author(s)
      鵜野いずみ、小阪孝史、三輪大輔、北村陽二、Mohammad Anwer-ul AZIM,小川数馬、川井恵一、柴和弘
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      パシフィコ横浜、横浜市
    • Related Report
      2013 Final Research Report
  • [Presentation] The development of potential vesicular acetylcholine transporter (VAChT) PET imaging probes.2013

    • Author(s)
      Kozaka T, Miwa D, Uno I, Kitamura Y, Azim MA, Ogawa K, Kinuya S, Kawai K, Shiba K.
    • Organizer
      2013 SNMMI 60th annual meeting.
    • Place of Presentation
      Vancouber Convention Centre, Vancouber, Canada
    • Related Report
      2013 Annual Research Report
  • [Presentation] In vivo evaluation of radioiodinated o-iodo-trans-decalinvesamicol(OIDV) as a vesicular acetylcholine transporter (VAChT) imaging agent.2013

    • Author(s)
      Uno I, Kozaka T, Kitamura Y, Miwa D, Azim MA, Ogawa K, Kawai K, Taki J, Kinuya S, Shiba K.
    • Organizer
      2013 SNMMI 60th annual meeting.
    • Place of Presentation
      Vancouber Convention Centre, Vancouber, Canada
    • Related Report
      2013 Annual Research Report
  • [Presentation] VAChTイメージング用[125I]OIDVのジアステレオマー分離と in vivo 脳内動態変化2013

    • Author(s)
      鵜野 いずみ、小阪 孝史、三輪 大輔、北村 陽二、Azim Mohammad A、小川 数馬、川井 恵一、柴 和弘.
    • Organizer
      第11回次世代を担う若手のためのフィジカル・ファーマフォーラム
    • Place of Presentation
      清水テルサ、静岡市、静岡県
    • Related Report
      2013 Annual Research Report
  • [Presentation] 脳内小胞アセチルコリントランスポーター(VAChT)のPETイメージングプローブ[11C]OMDVの開発,2013

    • Author(s)
      三輪大輔, 小阪孝史, 鵜野いずみ, 北村陽二, Azim Mohammad A., 河村和紀, 小川数馬, 川井恵一, 柴 和弘,
    • Organizer
      第11回次世代を担う若手のためのフィジカル・ファーマフォーラム
    • Place of Presentation
      清水テルサ、静岡市、静岡県
    • Related Report
      2013 Annual Research Report
  • [Presentation] アルツハイマー病の早期診断を目的とした新規PET用VAChTイメージング剤[11C]OMDVの合成とin vivo 評価2013

    • Author(s)
      小阪孝史、三輪大輔、鵜野いずみ、北村陽二、Mohammad Anwer-ul AZIM, 川村和紀、小川数馬、川井恵一、柴 和弘
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      パシフィコ横浜(横浜市)
    • Related Report
      2012 Research-status Report
  • [Presentation] OIDVのジアステレオマー分離とその選択的VAChTイメージング剤としての評価2013

    • Author(s)
      鵜野いずみ、小阪孝史、三輪大輔、北村陽二、Mohammad Anwer-ul AZIM, 小川数馬、川井恵一、柴 和弘
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      パシフィコ横浜(横浜市)
    • Related Report
      2012 Research-status Report
  • [Presentation] PET用VAChTイメージング剤の開発研究2012

    • Author(s)
      小阪孝史,三輪大輔,鵜野いずみ,北村陽二,Azim Mohammad Anwar-ul,小川数馬,川井恵一,絹谷清剛,柴和弘
    • Organizer
      第12回放射性医薬品・画像診断薬研究会
    • Place of Presentation
      京都テルサ,京都市
    • Year and Date
      2012-12-15
    • Related Report
      2013 Final Research Report
  • [Presentation] 前シナプスコリン作動性神経描画用新規VAChTイメージング剤の開発2012

    • Author(s)
      鵜野いずみ、小阪孝史、三輪大輔、北村陽二、道関美祐、小川数馬、川井恵一、河原栄、柴和弘
    • Organizer
      第7回日本分子イメージング学会総会・学術大会
    • Place of Presentation
      アクトシティ浜松(浜松市)
    • Related Report
      2013 Final Research Report
  • [Presentation] 前シナプスコリン作動性神経描画用新規VAChTイメージング剤の開発2012

    • Author(s)
      鵜野いずみ、小阪孝史、三輪大輔、北村陽二、道関美祐、小川数馬、川井恵一、河原 栄、柴 和弘、
    • Organizer
      第7回日本分子イメージング学会総会・学術大会
    • Place of Presentation
      アクトシティ浜松(浜松市)
    • Related Report
      2012 Research-status Report
  • [Presentation] PET用VAChTイメージング剤の開発研究2012

    • Author(s)
      小阪孝史,三輪大輔,鵜野いずみ,北村陽二,Azim Mohammad Anwar-ul,小川数馬,川井恵一, 絹谷清剛, 柴 和弘
    • Organizer
      第12回放射性医薬品・画像診断薬研究会
    • Place of Presentation
      京都テルサ(京都市)
    • Related Report
      2012 Research-status Report
  • [Presentation] VAChTイメージング用新規プローブの合成とその評価2011

    • Author(s)
      鵜野いずみ,小阪孝史,北村陽二,小川数馬,川井恵一,絹谷清剛,柴和弘
    • Organizer
      第11回放射性医薬品・画像診断薬研究会
    • Place of Presentation
      京都市
    • Year and Date
      2011-12-03
    • Related Report
      2013 Final Research Report
  • [Presentation] Vesamicol誘導体を用いた新規VAChTイメージング剤の開発2011

    • Author(s)
      小阪孝史,鵜野いずみ,北村陽二,小川数馬,川井恵一,絹谷清剛,柴和弘
    • Organizer
      第51回日本核医学会学術総会
    • Place of Presentation
      筑波市
    • Year and Date
      2011-10-29
    • Related Report
      2013 Final Research Report

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Published: 2011-08-05   Modified: 2019-07-29  

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