Development of probes and methods for noninvasive and quantitative assessment of efflux systems in the brain

• Project/Area Number: 20790920
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Radiation science
• Research Institution: National Institute of Radiological Sciences
• Principal Investigator: OKAMURA Toshimitsu National Institute of Radiological Sciences, 分子イメージング研究センター, 研究員 (80443068)
• Project Period (FY): 2008 – 2009
• Project Status: Completed (Fiscal Year 2009)
• Budget Amount: ¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000); Fiscal Year 2009: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000); Fiscal Year 2008: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
• Keywords: 放射性医薬品 / PET薬剤 / グルタチオン抱合体 / 異物排出トランスポータ / プリン

Research Abstract

The aim of this study is to develop radioactive probes for noninvasive and quantitative measurement of brain efflux systems. The novel probe readily enters the brain and is converted to its glutathione conjugate, which is specifically transported by an efflux transporter MRP1. The probe can measure brain efflux systems noninvasively and quantitatively.

Research Products

• [Journal Article] Noninvasive and quantitative assessment of the function of multidrug resistance-associated protein 1 in the living brain (2009)
  • Author(s): Okamura, T.;Kikuchi, T.;Okada, M.; Toramatsu, C.; Fukushi, K.;Takei, M.; Irie, T.
  • Journal Title: J Cereb Blood Flow Metab 29 Pages: 504-511
  • Peer Reviewed
• [Journal Article] Reactivity of 6-Halopurine Analogs with Glutathione as a Radiotracer for Assessing Function of Multidrug Resistance-Associated Protein 1 (2009)
  • Author(s): Okamura, T.;Kikuchi, T.;Fukushi, K.; Irie, T.
  • Journal Title: J Med Chem 52 Pages: 7284-7288
  • Peer Reviewed
• [Journal Article] Reactivity of 6-Halopurine Analogs with Glutathione as a Radiotracer for Assessing Function of Multidrug Resistance-Associated Protein 1 (2009)
  • Author(s): Toshimitsu Okamura
  • Journal Title: Journal of medicinal chemistry 52 Pages: 7284-7288
  • Peer Reviewed
• [Journal Article] Noninvasive and quantitative assessment of the function of multidrug resistance-associated protein 1 in the living brain (2009)
  • Author(s): Toshimitsu Okamura
  • Journal Title: Journal of Cerebral Blood Flow & Metabolism 29 Pages: 504-511
  • Peer Reviewed
• [Presentation] 6-Bromo-7-[11C]- methylpurine is a Specific Probe for the ABC Transporter Mrp1, but not for Mrp2, Pgp, and Bcrp (2009)
  • Author(s): Okamura, T., et, al.
  • Organizer: Annual Congress of the European Association of Nuclear Medicine
  • Place of Presentation: Barcelona International Convention Center, Barcelona.
  • Year and Date: 2009-10-13
• [Presentation] Evaluation of the conversion rate of 6-halogenopurine derivatives as a probe for assessing mrpl function (2009)
  • Author(s): Okamura, T., et, al.
  • Organizer: 18th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: Shaw Conference Centre, Edmonton
  • Year and Date: 2009-07-14
• [Presentation] Evaluation of the conversion rate of 6-halogenopurine derivatives as a probe for assessing mrpl function (2009)
  • Author(s): Toshimitsu Okamura
  • Organizer: 18th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: カナダエドモントン
  • Year and Date: 2009-07-14
• [Presentation] A PET Probe for Quantitatively Assessing the Efflux Transport Function of Multidrug Resistance-Associated Protein 1 in the Brain (2008)
  • Author(s): Okamura, T., et, al.
  • Organizer: World Molecular Imaging Congress
  • Place of Presentation: The Acropolis Convention Center, Nice
  • Year and Date: 2008-09-13
• [Presentation] A PET Probe for Quantitatively Assessing the Efflux Transport Function of Multidrug Resistance-Associated Protein 1 in the Brain (2008)
  • Author(s): Toshimitsu Okamura
  • Organizer: World Molecular Imaging Congress (WMIC)
  • Place of Presentation: 仏蘭西ニース
  • Year and Date: 2008-09-13
• [Remarks]
  • URL: http://www.nirs.go.jp/db/seikadb/Welcome.php
• [Remarks]
  • URL: http://www.nirs.go.jp/db/seikadb/Welcome.php