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2003 Fiscal Year Final Research Report Summary

Development of miniaturized synthesis modules for preparation of PET radiopharmaceuticals

Research Project

Project/Area Number 13470177
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Research Field Radiation science
Research InstitutionTohoku University

Principal Investigator

IWATA Ren  Tohoku University, Cyclotron and Radioisotope Center, Professor, サイクロトロン・ラジオアイソトープセンター, 教授 (60143038)

Co-Investigator(Kenkyū-buntansha) YANAI Kazuhiko  Tohoku University, Graduate School of Medicine, Professor, 大学院・医学系研究科, 教授 (50192787)
YAMAZAKI Hiromichi  Tohoku University, Graduate School of Engineering, Associate professor, 大学院・工学研究科, 助教授 (00166654)
Project Period (FY) 2001 – 2003
KeywordsPET / Automated synthesis / Miniaturized synthesis module / Microreactor / Radiopharmaceutical / Labeling
Research Abstract

Procedures for the preparation of useful PET radiopharmaceuticals were first simplified for automated efficient synthesis and then miniaturized synthesis modules were developed using manifold miniature valves.
1.Loop method and solid phase extraction were successfully combined for efficient on-line processing of [^<11>C]methylation and HPLC purification of receptor ligands.
2.[^<18>F]Fluoromethyl triflate, a novel ^<18>F-labeling agent, was prepared from [^<18>F]fluoride and successfully applied to the synthesis of [^<18>F]fluorocholine and [^<18>F]fluoromethyl tyrosine.
3.A new synthesis module of a palm size was developed for the first time using miniature manifold valves. Using this technique a miniaturized module suitable for routine preparation of [^<11>C]methionine and [^<11>C]choline was developed.
4.Synthesis modules were also miniaturized for the preparation of [^<18>F]fluoromethyl triflate from [^<18>F]fluoride and the on-column preparation of [^<18>F]fluorocholine.

  • Research Products

    (16 results)

All Other

All Publications (16 results)

  • [Publications] R.Iwata, C.Pascali, A.Bogni, Y.Miyake, K.Yanai, T.Ido: "A Simple Loop Method for the Automated Preparation of [^<11>C]Raclopride from [^<11>C]Methyl Triflate"Applied Radiation Isotopes. 55. 17-22 (2001)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] R.Iwata, C.Pascali, A.Bogni, S.Furumoto, K.Terasaki, K.Yanai: "[^<18>F]Fluoromethyl triflate, a novel and reactive [^<18>F]fluoromethylating agent. Preparation and application to the on-column preparation of [^<18>F]fluorocholine"Applied Radiation Isotopes. 57. 347-352 (2002)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] S.Furumoto, R.Iwata, T.Ido: "Design and synthesis of fluorine-18 labeled matrix metalloproteinase inhibitors for cancer imaging"J.Labeled.Compounds and Radiopharmaceuticals. 45. 975-986 (2002)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] R.Iwata, S.Furumoto, C.Pascali, A.Bogni, K.Ishiwata: "Radiosynthesis of O-[^<11>C]methyl-L-tyrosine and O-[^<18>F]fluoromethyl-L-tyrosine as potential PET tracers for imaging amino acid transport"J.Labeled.Compounds and Radiopharmaceuticals. 46. 555-566 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] S.Furumoto, K.Takashima, K.Kubota, T.Ido, R.Iwata, H.Fukuda: "Tumor detection using ^<18>F-labeled matrix metalloproteinase-2 inhibitor"Nuclear Medicine and Biology. 30. 119-125 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Y.Funaki, M.Kato, R.Iwata, E.Sakurai, E.Sakurai, M.Tashiro, T.Ido, K.Yanai: "Evaluation of the binding characteristics of [5-^<11>C-methoxy]donepezil in the rat brain for in vivo visualization of acetylcholinesterase."J.Pharmacol.Sci.. 91. 105-112 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] T.Takahashi, T.Mizuno, T.Ido, R.Iwata, K.Watanabe: "Improved synthesis of pure [^<18>F]fluoro-compounds for PET studies from bromo-compounds."Appl.Radiat.Isot.. 58. 557-566 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] A.Bogni, E.Bombardieri, R.Iwata, L.Cadini, C.Pascali: "Stability of L-[S-methyl-^<11>C]methionine solutions."J.Radioanal.Nucl.Chem.. 256. 199-203 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] R.Iwata, C.Pascali, A.Bogni, Y.Miyake, K.Yanai, T.Ido: "A Simple Loop Method for the Automated Preparation of [^<11>C]Raclopride from [^<11>C]Methyl Triflate."Applied Radiation Isotopes. 55. 17-22 (2001)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] R.Iwata, C.Pascali, A.Bogni, S.Furumoto, K.Terasaki, K.Yanai: "[^<18>F]Fluoromethyl triflate, a novel and reactive [^<18>F]fluoromethylating agent. Preparation and application to the on-column preparation of[^<18>F]fluorocholine."Applied Radiation Isotopes. 57. 347-352 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] S.Furumoto, R.Iwata, T.Ido: "Design and synthesis of fluorine-18 labeled matrix metalloproteinase inhibitors for cancer imaging."J.Labeled. Compounds and Radiopharmaceuticals. 45. 975-986 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] R.Iwata, S.Furumoto, C.Pascali, A.Bogni, K.Ishiwata: "Radiosynthesis of O-[^<11>C]methyl-L-tyrosine and O-[^<11>F]fluoromethyl-L-tyrosine as potential PET tracers for imaging amino acid transport."J.Labeled. Compounds and Radiopharmaceuticals. 46. 555-566 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] S.Furumoto, K.Takashima, K.Kubota, T.Ido, R.Iwata, H.Fukuda: "Tumor detection using ^<18>F-labeled matrix metalloproteinase-2 inhibitor."Nuclear Medicine and Biology. 30. 119-125 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Y.Funaki, M.Kato, R.Iwata, E.Sakurai, E.Sakurai, M.Tashiro, T.Ido, K.Yanai: "Evaluation of the binding characteristics of [5-^<11>C-methoxy]donepezil in the rat brain for in vivo visualization of acetylcholinesterase."J.Pharmacol.Sci.. 91. 105-112 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] T.Takahashi, T.Mizuno, T.Ido, R.Iwata, K.Watanabe: "Improved synthesis of pure[^<18>F]fluoro-compounds for PET studies from bromo-compounds."Appl.Radiat.Isot.. 58. 557-566 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] A.Bogni, E.Bombardieri, K.Iwata, L.Cadini, C.Pascali: "Stability of L-[S-methyl-^<11>C]methionine solutions."J.Radioanal.Nucl.Chem.. 256. 199-203 (2003)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 2005-04-19  

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