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Development of PET, SPECT and Fluorescence Probes for Imaging of Peripheral Benzodiazepine Receptors

Research Project

Project/Area Number 19590114
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionNational Institute of Radiological Sciences

Principal Investigator

ZHANG Ming-rong  National Institute of Radiological Sciences, 分子イメージング研究センター, チームリーダー (80443076)

Project Period (FY) 2007 – 2008
Project Status Completed (Fiscal Year 2008)
Budget Amount *help
¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2008: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2007: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
KeywordsAC-5216 / PET / SPECT / 末梢性ベンゾジアゼピン受容体 / アルツハイマー病 / 末梢性ベンゾジアゾピン受容体 / PBR / [11C]DAA1106 / [11C]AC-5216 / [18F]FEDAA1106
Research Abstract

末梢性ベンゾジアゼピン受容体(peripheral-type benzodiazepine receptor, PBR)は末梢のみならず、脳内にもその存在は認められている。近年、PET(positron emission tomography)を応用し、アルツハイマー病などに伴う脳内マイクログリアの活性化によってPBRの変化に焦点を当てた研究は多く行われている。
申請者はPBRに特異性を示し、in vivo のリガンドとして極めて有効性が高い新規なPBRのPETイメージング剤[11C]AC-5216を創出することができ、臨床研究に使用されている。さらに[11C]AC-5216をLead Compound とし、数種のPETリガンドを開発することができた。

Report

(3 results)
  • 2008 Annual Research Report   Final Research Report ( PDF )
  • 2007 Annual Research Report
  • Research Products

    (18 results)

All 2009 2008 2007 Other

All Journal Article (11 results) (of which Peer Reviewed: 10 results) Presentation (4 results) Remarks (3 results)

  • [Journal Article] Evaluation of N-benzyl-N-[11C]methyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro -9H-purin-9-yl)acetamide ([11C]DAC) as a novel translocator protein (18 kDa) radioligand in kainic acid-lesioned rat2009

    • Author(s)
      Yanamoto K, Yamasaki T, Kumata K., Yui J., Odawara C., Kawamura K., Hatori A., Inoue O., Yamaguchi M., Suzuki K., Zhang M.-R.
    • Journal Title

      Synapse Doi 10.1002/syn.20678

    • Related Report
      2008 Final Research Report
  • [Journal Article] 18F]FEAC and [18F]FEDAC: two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in brain2009

    • Author(s)
      Yanamoto K., Kumata K., Yamasaki T., Odawara C., Kawamura K., Yui J., Hatori A., Suzuki K., Zhang M.-R
    • Journal Title

      Bioorganic and Medicinal Chemistry Letters 19

      Pages: 1707-1710

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] [^<18>F] FEAC and [^<18>F] FEDAC : two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in brain2009

    • Author(s)
      Ming-Rong Zhang, et al.
    • Journal Title

      Bioorganic and Medicinal Chemistry Letters 19

      Pages: 1707-1710

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Evaluation of N-benzyl-N-[^<11>C]methyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide ([^<11>C] DAC as a novel translocator protein (18kDa) radioligand in kainic acid-lesioned rat2009

    • Author(s)
      Ming-Rong Zhang, et al.
    • Journal Title

      Synapse (In press)

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Astroglial peripheral benzodiazepine receptor as an indicator of neurotrophic support by astrocytes coupled with nontoxic microgliosis2008

    • Author(s)
      Ji B., Maeda J., Sawada M., Ono M., Okauchi T., Inaji M., Zhang M.-R., Suzuki K., Ando K., Higuchi M., Suhara T
    • Journal Title

      Journal of Neuroscience 28

      Pages: 12255-12267

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Astroglial peripheral benzodiazepine receptor as an indicator of neurotrophic support by as trocytes coupled with nontoxic microgliosis2008

    • Author(s)
      Ming-Rong Zhang, et al.
    • Journal Title

      Journal of Neuroscience 28

      Pages: 12255-12267

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] In vitro and ex vivo autoradiography studies on peripheral-type benzodiazepine receptor binding using [11C]AC-5216 in normal and kainic acid-lesioned rat2007

    • Author(s)
      Yanamoto K., Zhang M.-R., Kumata K., Hatori A., Okada M., Suzuki K
    • Journal Title

      Neuroscience Letters 428

      Pages: 59-63

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] [11C]AC-5216: A novel positron emission tomography ligand for peripheral-type benzodiazepine receptors in primate brain2007

    • Author(s)
      .Zhang M.-R., Kumata K., Maeda J., Yanamoto K., Hatori A., Okada M., Higuchi M., Obayashi S., Suhara T., Suzuki K
    • Journal Title

      Journal of Nuclear Medicine 48

      Pages: 1853-1861

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[131I]iodo-5-methoxybenzyl)acetamide: a potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain.2007

    • Author(s)
      Ming-Rong Zhang, et. al.
    • Journal Title

      Journal of Medicinal Chemistry 50

      Pages: 2735-2742

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A practical route for synthesizing a PET ligand containing [18F]fluorobenzene using reaction of diphenyliodonium salt with[18F]F.2007

    • Author(s)
      Ming-Rong Zhang, et. al.
    • Journal Title

      Tetrahedron Letters 48

      Pages: 8632-8635

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] [11C]AC-5216: A novel positron emission tomography ligand for peripheral-type benzodiazepine receptors in primate brain.2007

    • Author(s)
      Ming-Rong Zhang, et. al.
    • Journal Title

      Journal of Nuclear Medicine 48

      Pages: 1853-1861

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Presentation] ONE-POT RADIOSYNTHESIS OF [13N]UREA AND [13N]CARBAMATE USING NO-CARRIER-ADDED [13N]NH32008

    • Author(s)
      Zhang M.-R., Kumata K., Ogawa M., Kato K., Suzuki K
    • Organizer
      7^<th> International Conference of Nuclear and Radiochemistry
    • Place of Presentation
      ブタペスト、ハンガリー
    • Year and Date
      2008-08-24
    • Related Report
      2008 Final Research Report
  • [Presentation] ONE-POT RADIOSYNTHESIS OF [^<13>N] UREA AND [^<13>N] CARBAMATE USING NO-CARRIER-ADDED [^<13>N] NH_32008

    • Author(s)
      Ming-Rong Zhang, et al.
    • Organizer
      7^h International Conference of Nuclear and Radiochemistry
    • Place of Presentation
      ブタペスト、ハンガリー
    • Year and Date
      2008-08-24
    • Related Report
      2008 Annual Research Report
  • [Presentation] [11C]AC-5216: RADIOSYNTHESIS AND EVALUATION AS A NOVEL PET LIGAND FOR THE PERIPHERAL-TYPE BENZODIAZEPINE RECEPTOR IN BRAIN2007

    • Author(s)
      Zhang M.-R., K. Kumata, J. Maeda, K. Yanamoto, M. Amitani, J. Noguchi, T. Okauchi, T. Suhara, K. Suzuki
    • Organizer
      7^<th> International Symposium on Radiopharmaceutical
    • Place of Presentation
      アーヘン、ドイツ
    • Year and Date
      2007-04-30
    • Related Report
      2008 Final Research Report
  • [Presentation] [11C]AC-5216:RADIOSYNTHESIS AND EVALUATION AS A NOVEL POSITRON EMISSION TOMOGRAP HY LIGAND FOR PERIPHERAL-TYPE BENZODIAZEPINE RECEPTORS IN PRIMATE BRAIN.2007

    • Author(s)
      Ming-Rong Zhang, et. al.
    • Organizer
      17th International symposium on radiopharmaceutical sciences
    • Place of Presentation
      アーヘン、ドイツ
    • Year and Date
      2007-04-30
    • Related Report
      2007 Annual Research Report
  • [Remarks]

    • URL

      http://www.nirs.go.jp/research/division/mic/group/t_hyoshiki-gijutu.html

    • Related Report
      2008 Final Research Report
  • [Remarks]

    • URL

      http://www.nirs.go.jp/research/division/mic/group/t_hyoshiki-gijutu.html

    • Related Report
      2008 Annual Research Report
  • [Remarks]

    • URL

      http://www.nirs.go.jp/research/division/mic/group/t_hyoshiki-gijutu.html

    • Related Report
      2007 Annual Research Report

URL: 

Published: 2007-04-01   Modified: 2016-04-21  

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