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

2008 Fiscal Year Final Research Report

• Project/Area Number: 19590114
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: National 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
• Keywords: AC-5216 / PET / SPECT / 末梢性ベンゾジアゼピン受容体

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。

Research Products

• [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 rat (2009)
  • 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
• [Journal Article] 18F]FEAC and [18F]FEDAC: two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in brain (2009)
  • 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
  • Peer Reviewed
• [Journal Article] Astroglial peripheral benzodiazepine receptor as an indicator of neurotrophic support by astrocytes coupled with nontoxic microgliosis (2008)
  • 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
  • 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 rat (2007)
  • Author(s): Yanamoto K., Zhang M.-R., Kumata K., Hatori A., Okada M., Suzuki K
  • Journal Title: Neuroscience Letters 428 Pages: 59-63
  • Peer Reviewed
• [Journal Article] [11C]AC-5216: A novel positron emission tomography ligand for peripheral-type benzodiazepine receptors in primate brain (2007)
  • 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
  • Peer Reviewed
• [Presentation] ONE-POT RADIOSYNTHESIS OF [13N]UREA AND [13N]CARBAMATE USING NO-CARRIER-ADDED [13N]NH3 (2008)
  • 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
• [Presentation] [11C]AC-5216: RADIOSYNTHESIS AND EVALUATION AS A NOVEL PET LIGAND FOR THE PERIPHERAL-TYPE BENZODIAZEPINE RECEPTOR IN BRAIN (2007)
  • 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
• [Remarks]
  • URL: http://www.nirs.go.jp/research/division/mic/group/t_hyoshiki-gijutu.html