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In vivo evaluation of 11C-labeled 2-arylpropionic acid as a PET probe for COXs in neuroinflammation

Research Project

Project/Area Number 22790517
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Applied pharmacology
Research InstitutionThe Institute of Physical and Chemical Research

Principal Investigator

SHUKURI Miho  独立行政法人理化学研究所, 分子プローブ機能評価研究チーム, 研究員 (20525571)

Project Period (FY) 2010 – 2011
Project Status Completed (Fiscal Year 2011)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2011: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2010: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000)
Keywordsシクロオキシゲナーゼ / 非ステロイド性抗炎症薬 / PET / 脳炎症 / ミクログリア / 神経変性疾患 / LPS / アラキドン酸カスケード / 脳内炎症
Research Abstract

In order to develop the imaging agent for the in vivo monitoring of COXs activity and/or expression, a series of 2-arylpropionic acid derivatives of NSAIDs were labeled with 11C. Among them, we found that^<11> C-labeled ketoprofen-methyl ester(KTP-Me), its acid form rather specific to COX-1, showed superior sensitivity to inflammation of rat brain. In addition, our results suggest that^<11> C-KTP-Me recognize the changes of COX-1 expression in brain, and provide new evidence for the specific imaging of microglial activation. PET study in monkeys also showed the high accumulation of^<11> C-KTP-Me in neuroinflammatory area. The safety, biodistribution and kinetics of^<11> C-KTP-Me in both rats and monkeys indicate that it should be acceptable for the use of study in human.

Report

(3 results)
  • 2011 Annual Research Report   Final Research Report ( PDF )
  • 2010 Annual Research Report
  • Research Products

    (27 results)

All 2012 2011 2010 Other

All Journal Article (7 results) (of which Peer Reviewed: 3 results) Presentation (18 results) Remarks (2 results)

  • [Journal Article] 脳内COX-1を標的分子とした活性化マイクログリアのイメージング2012

    • Author(s)
      宿里充穗, 他
    • Journal Title

      日本分子イメージング学会機関誌

      Volume: 5 Pages: 13-16

    • Related Report
      2011 Annual Research Report
  • [Journal Article] In vivo expression of cyclooxygenase-1 in activated microglia/macrophages during neuroinflammation visualized by PET with^<11> C-Ketoprofen-methyl ester2011

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Tadayuki Takashima, Kiyoshi Matsumura, Osamu Inoue, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe, Hirotaka Onoe
    • Journal Title

      J Nucl Med

      Volume: 52 Pages: 1094-1101

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] ^<11> C標識非ステロイド性抗炎症薬(NSAIDs)による脳炎症のイメージング2011

    • Author(s)
      宿里充穗、高島好聖、尾上浩隆
    • Journal Title

      PETジャーナル

      Volume: 15巻 Pages: 28-30

    • Related Report
      2011 Final Research Report
  • [Journal Article] 脳内COX-1を標的分子とした活性化マイクログリアのイメージング2011

    • Author(s)
      宿里充穗,高島好聖,徳田景子,松村潔,土居久志,鈴木正昭,渡辺恭良,尾上浩隆
    • Journal Title

      日本分子イメージング学会機関誌

      Volume: 5巻 Pages: 13-16

    • Related Report
      2011 Final Research Report
  • [Journal Article] In vivo expression of cyclooxygenase-1 in activated microglia and macrophages duringneuroinflammation visualized by PET with11C-ketoprofen methyl ester2011

    • Author(s)
      Shukuri M, Takashima-Hirano M, Tokuda K,Takashima T, Matsumura K, Inoue O, Doi H,Suzuki M, Watanabe Y, Onoe H
    • Journal Title

      J Nucl Med

      Volume: 52 Issue: 7 Pages: 1094-101

    • DOI

      10.2967/jnumed.110.084046

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] ^<11>C標識非ステロイド性抗炎症薬(NSAIDs)による脳炎症のイメージング2011

    • Author(s)
      宿里充穗、高島好聖、尾上浩隆
    • Journal Title

      PETジャーナル

      Volume: 15 Pages: 28-30

    • Related Report
      2011 Annual Research Report
  • [Journal Article] General Method for the^<11> C-labeling of 2-arylpropionic acids and their esters : construction of a PET tracer library for a study of biological events involved in COXs expression2010

    • Author(s)
      Misato Takashima-Hirano, Miho Shukuri, Tadayuki Takashima, Miki Goto, Yasuhiro Wada, Yasuyoshi Watanabe, Hirotaka Onoe, Hisashi Doi, Masaaki Suzuki
    • Journal Title

      Chem. Eur. J

      Volume: 16 Pages: 4250-4258

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Presentation] Cyclooxygenase imaging in neuroinflammation and neurodegenerative diseases2012

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Kiyoshi Matsumura, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe, Hirotaka Onoe
    • Organizer
      The 14th Conference of Peace through Mind Brain Science
    • Place of Presentation
      Hamamatsu
    • Related Report
      2011 Final Research Report
  • [Presentation] Cyclooxygenase imaging in neuroinflammation and neurodegenerative diseases2012

    • Author(s)
      Shukuri M
    • Organizer
      The 14th Conference of Peace through Mind Brain Science
    • Place of Presentation
      Hamamatsu(招待講演)
    • Related Report
      2011 Annual Research Report
  • [Presentation] Imaging of activated microglia by PET with^<11> C-labeled Ketoprofen-methylester2011

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Kiyoshi Matsumura, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe & Hirotaka Onoe
    • Organizer
      EANM' 11
    • Place of Presentation
      Birmingham, UK
    • Related Report
      2011 Final Research Report
  • [Presentation] Cyclooxygenase-1 expression in activated microglia/macrophages during neuroinflammation2011

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Kiyoshi Matsumura, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe & Hirotaka Onoe
    • Organizer
      The 10th World Congress on Inflammation
    • Place of Presentation
      Paris
    • Related Report
      2011 Final Research Report
  • [Presentation] A novel PET probe, 11C-ketoprofen-methyl ester, targeting cyclooxygenase-1 in the brain2011

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Kiyoshi Matsumura, Miki Goto, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe & Hirotaka Onoe
    • Organizer
      2011 SNM Annual Meeting
    • Place of Presentation
      San Antonio, Texas
    • Related Report
      2011 Final Research Report
  • [Presentation] PETイメージングによる脳内炎症過程におけるCOX-1の機能解析-新規PETプローブ^<11> C-Ketoprofen-methyl esterを用いた検討-2011

    • Author(s)
      宿里充穗、高島好聖、徳田景子、松村潔、土居久志、鈴木正昭、渡辺恭良、尾上浩隆
    • Organizer
      第32回日本炎症・再生医学会
    • Place of Presentation
      京都
    • Related Report
      2011 Final Research Report
  • [Presentation] LPS誘発脳内炎症における活性化マイクログリアのイメージング2011

    • Author(s)
      宿里充穗、高島好聖、徳田景子、松村潔、土居久志、鈴木正昭、渡辺恭良、尾上浩隆
    • Organizer
      第6回日本分子イメージング学会学術集会
    • Place of Presentation
      神戸
    • Related Report
      2011 Final Research Report
  • [Presentation] LPS誘発脳内炎症における活性化マイクログリアのイメージング2011

    • Author(s)
      宿里充穗
    • Organizer
      第6回日本分子イメージング学会学術集会
    • Place of Presentation
      神戸国際会議場(神戸)
    • Related Report
      2011 Annual Research Report
  • [Presentation] PETイメージングによる脳内炎症過程におけるCOX-1の機能解析-新規PETプローブ^<11>C-Ketoprofen-methyl esterを用いた検討-2011

    • Author(s)
      宿里充穗
    • Organizer
      第32回日本炎症・再生医学会
    • Place of Presentation
      京都国際会館(京都)
    • Related Report
      2011 Annual Research Report
  • [Presentation] A novel PET probe, ^<11>C-ketoprofen-methyl ester, targeting cyclooxygenase-1 in the brain2011

    • Author(s)
      Shukuri M
    • Organizer
      2011 SNM Annual Meeting
    • Place of Presentation
      San Antonio, Texas, USA
    • Related Report
      2011 Annual Research Report
  • [Presentation] Cyclooxygenase-1 expression in activated microglia/macrophages during neuroinflammation2011

    • Author(s)
      Shukuri M
    • Organizer
      The 10th World Congress on Inflammation
    • Place of Presentation
      Paris, France
    • Related Report
      2011 Annual Research Report
  • [Presentation] Imaging of activated microglia by PET with ^<11>C-labeled Ketoprofen-methylester2011

    • Author(s)
      Shukuri M
    • Organizer
      EANM'11 : Annual Congress of the European Association of Nuclear Medicine
    • Place of Presentation
      Birmingham, UK
    • Related Report
      2011 Annual Research Report
  • [Presentation] [C^^<11>] Ketoprofen-methyl esterのCOX isoform選択性に関する検討2010

    • Author(s)
      宿里充穂,高島好聖,徳田景子,松村潔,後藤美樹,土居久志,鈴木正昭,渡辺恭良,尾上浩隆
    • Organizer
      第50回日本核医学会学術総会
    • Place of Presentation
      埼玉
    • Related Report
      2011 Final Research Report
  • [Presentation] C^^<11>-Ketoprofen-methyl ester as a Novel Cyclooxygenase-1 Specific PET Probe for Imaging of Nuroinflammation2010

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Kiyoshi Matsumura, Miki Goto, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe, Hirotaka Onoe
    • Organizer
      World Molecular Imaging Conference
    • Place of Presentation
      Kyoto
    • Related Report
      2011 Final Research Report
  • [Presentation] COX imaging by PET with 11C-labeled nonsteroidal anti-inflammatory drugs(NSAIDs)2010

    • Author(s)
      Miho Shukuri, Misato Takashima-Hirano, Miki Goto, Tadayuki Takashima, Keiko Tokuda, Yasuyoshi Watanabe, Hisashi Doi, Masaaki Suzuki, and Hirotaka Onoe
    • Organizer
      World Pharma2010
    • Place of Presentation
      Copenhagen, Denmark
    • Related Report
      2011 Final Research Report
  • [Presentation] ^<11>C-Ketoprofen-methyl Ester as a Novel Cyclooxygenase-1 Specific PETProbe for Imaging of Neuroinflammation.2010

    • Author(s)
      Miho Shukuri
    • Organizer
      World Molecular Imaging Conference
    • Place of Presentation
      Kyoto
    • Related Report
      2010 Annual Research Report
  • [Presentation] COX imaging by PET with ^<11>C-labeled nonsteroidal anti-inflammatory drugs (NSAIDs).2010

    • Author(s)
      Miho Shukuri
    • Organizer
      World Pharma2010
    • Place of Presentation
      Copenhagen, Denmark
    • Related Report
      2010 Annual Research Report
  • [Presentation] [^<11>C] Ketoprofen-methyl esterのCOX isoform選択性に関する検討2010

    • Author(s)
      宿里充穗
    • Organizer
      第50回日本核医学会学術総会
    • Place of Presentation
      大宮
    • Related Report
      2010 Annual Research Report
  • [Remarks] プレスリリース:解熱・鎮痛作用を示す薬に目印をつけ、体内での可視化に成功-PET分子イメージングで抗炎症薬の体内の動きを見る-、2010年3月9日

    • Related Report
      2011 Final Research Report
  • [Remarks] プレスリリース:脳内炎症の発症の仕組みを解く酵素COX-1のライブイメージングに成功-COX-1を選択的に認識するPETプローブを開発-、2011年6月17日

    • Related Report
      2011 Final Research Report

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Published: 2010-08-23   Modified: 2016-04-21  

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