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Development of Generator Produced Positron Emitting Radionuclide Containing Diagnostic Radiopharmaceutical

Research Project

Project/Area Number 62890005
Research Category

Grant-in-Aid for Developmental Scientific Research

Allocation TypeSingle-year Grants
Research Field 広領域
Research InstitutionKYOTO UNIVERSITY

Principal Investigator

YOKOYAMA Akira  Kyoto Univ. Fac. Pharm. Sci. Professor, 薬学部, 教授 (90025685)

Co-Investigator(Kenkyū-buntansha) HAZUE Masaaki  Nihon Medi-phisics Co. Ltd. Research, Development, Director, 技術部, 技術部長
YONEKURA Yoshiharu  Kyoto Univ., School Med. Lecturers, 医学部, 講師 (60135572)
FUJIBAYASHI Yasuhisa  Kyoto Univ. School Med. Res. Associate, 医学部, 助手 (50165411)
荒野 泰  京都大学, 薬学部, 助手 (90151167)
Project Period (FY) 1987 – 1989
Project Status Completed (Fiscal Year 1989)
Budget Amount *help
¥6,300,000 (Direct Cost: ¥6,300,000)
Fiscal Year 1989: ¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 1988: ¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 1987: ¥5,100,000 (Direct Cost: ¥5,100,000)
KeywordsPositron Emitted Radionuclide / Radiopharmaceutical / 62-Cu Generator / 62-Cu Dithiosemicarbazone complex / 62-Cu-HSA / 62-Cu Labeled Fatty Acid / 68-Ga Citrate / 68-Ga Labeled Monoclonal Antibody / 62-Cuジェネレ-タ / 62-Cuジチオセミカルバゾ-ン錯体 / 脳血流診断薬剤 / 68-Ga標識抗体 / 68-Ga標識抗体用スペ-サ / 68Ga標識ジゴキシン / ラジオイムノアッセイ / ポジトロン核医学診断 / 62ー銅ジェネレータ / ポジトロン核医学診断薬 / 62ー銅標識ヒト血清アルブミン / 局所血液量診断薬剤 / 62ー銅標識高級脂肪酸 / 心筋エネルギー代謝機能診断薬剤
Research Abstract

To promote the expansion of Position Nuclear Medicine,our attention was focused in the establishment of generator production system for position emitting radiometallic nuclide (P-RI) and in the development of P-RI labeled pharmaceuticals for the diagnosis of tumor and brain, heart disorders . At first, 62-Cu, 68-M, 82-Rb and 52m-Mn generators attracted our interest, however, according to progress in the international arena, the development of 1) 62-Cu generator system, 2) 62-Cu and 3) 68-Ga labeled diagnostic agents occupies more imminent place. On those basis, the results are described below as follows:
1) Production of 62-Cu generator system : at first, the 63-Cu (p, 2n) 62-Zn nuclear reaction using natural copper as the target was carried out; then, a separation methodology for the 62-Cu daughter from its 62-Zn parent was surveyed. After studying various analytical conditions, the elution of the daughter as the 62-Ci-glycine complex enabled the achievement of a practical generator sy … More stem for the production of of 62-Cu with high purity and high yield.
2) 62-Cu labeled diagnostic agent: based on the ability of dithiosemicarbazone (DTS) to render highly stable, compact and unchanged complex with 62-Cu, this molecule was used for the design of bifunctional chelating agents, such as, the 62-Cu labeled albumin, 62-Cu labeled long chain fatty acids (function diagnosis of myocardium metabolism), 62-Cu-DTS-esther derivatives (cerebral blood flow diagnosis). Then, the accumulation mechanism of each developed agent in the tissue or organ of interest was evaluated according, to the basic,requirement needed for their future clinical applicability.
3) 68-Ga labeled diagnostic agent: the use of radiolabeled 68-Ga-citrate for the tumor diagnosis in Nuclear Medicine calls for some basic studies enabling its specific accumulation within the short half-life. Also, some in-vitro and in-vivo studies with 68-Ga labeled tumor antibodies for its plausible use in Nuclear medicine is under progress.
In conclusion, each result set together the pathway for future development. Less

Report

(3 results)
  • 1989 Annual Research Report   Final Research Report Summary
  • 1988 Annual Research Report
  • Research Products

    (27 results)

All Other

All Publications (27 results)

  • [Publications] 横山陽: "核医学診断と金属錯体" 化学工業. 38. 318-325 (1987)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Mitsura Koizumi: "Preparation of 67-Ga Labeled Antibodies Using Deferoxamine as a Bifunctional Chelate;An Improved Method" Journal of Immunological Methods. 104. 93-102 (1987)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasushi Fujibayashi: "Zn-62-EDDA(Ethylenediamine-N,N'-diacetic Acid)Chelate as a pancreas Targetting Drug;A Radiopharmaceutical Design for Functional Diangosis" PLZEN.LEK.SBORN.,Suppl.49. 269-273 (1987)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Teruyasu Suzuki: "Arterical and Venous Thrombus Imaging Using Ga-DFO-DAS-Fibrino-gen;Its Clinical Applicability" Radiation Research. 5. 154-158 (1987)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasusi Arano: "Design,Synthesis and 64-Cu Labeling of Fatty Acid Analogs Containing Dithiosemicarbazone Chelate" Applied Radiation Isotopes. 40. 745-749 (1989)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasuhisa Fujibayashi: "A New Zinc-62/Copper-62 Generator as a Copper-62 Souce for PET Radiopharmaceuticals" Jounal of Nuclear Medicine. 30. 1834-1842 (1989)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] 横山陽: "金属イオンの高選択的組織内濃縮-核医学診断薬剤の開発" 細胞. 22. 28-31 (1990)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasuhisa Fujibayashi: "62-Cu-Labeling of Human Serum Albumin-Dithiosemicarbazone Conjugate(HSA-DTS)for Regional Plasma Volume Measurement:Application of New 62-Zn/62-Cu Generator System" Chemical & Pharmaceutical Bulletin. 37. (1990)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Takako Furukawa: "Ga-Labeling of IgG with high Specific Radioactivity" Chemical & Pharmaceutical Bulletin.

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Akira Yokoyama: "Nuclear Medicine and Radiometallic Complexes." KAGAKUKOGYO, 38, 318-325 (1987).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Mitsuru Koizumi: "Preparation of 67-Ga Labeled Antibodies Using Deferoxamine as a Bifunctional Chelate; An Improved Method." J. Immunol. Method, 104, 93-102 (1987).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasuhisa Fujibayashi: "Zn-62-EDDA(Ethylenediamine-N, N'-diacetic Acid) Chelate as a Pancreas Targeting Drug; A Radiopharmaceutical Design for Functional Diagnosis." PLZEN. LEK. SBORN. SUPPL. 49, 269-273(1987).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Teruyasu Suzuki: "Arterial and Venous Thrombus Imaging Using Ga-DFO-DAS-Fibrinogen; Its Clinical Applicability." Radiation Research, 5, 154-158 (1987).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasushi Arano: "Design, Synthesis and 64-Cu Labeling of Fatty Acid Analogs Containing Dithiosemicarbazone Chelate." Appl. Radiat. Isotop. 40, 745-749 (1989).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasuhisa Fujibayashi: "A New Zinc-62/Copper-62 Generator as a Copper-62 Source for PET Radiopharmaceuticals." J. Nucl. Med. 30, 1834-1842 (1989).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Akira Yokoyama: "Selective Concentration of Metal Ions into Target Tissues-Development of Diagnostic Agents for Nuclear Medicine." SAIBOU, 22, 28-31 (1990).

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasuhisa Fujibayashi: "62-Cu-Labeling of Human Serum Albumin-Dithiosemicarbazone Conjugate (HSA-DTS) for Regional Plasma Volume Measurement: Application of New 62-Zn/62-Cu Generator System." Chem. Pharm. Bull. 37 (1990) -in press-.

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Takako Furukawa: "Ga-Labeling of IgG with High Specific Radioactivity." Chem. Pharm. Bull.

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1989 Final Research Report Summary
  • [Publications] Yasushi Arano: "Design,Synthesis and 64-Cu Labeling of Fatty Acid Analogs Containing Dithiosemicarbazone Chelate" Applied Radiation Isotopes. 40. 754-749 (1989)

    • Related Report
      1989 Annual Research Report
  • [Publications] Yasuhisa Fujibayashi: "A New Zinc-62/Copper-62 Generator as a Copper-62 Source for PET Radiopharmaceuticals" Journal of Nuclear Medicine. 30. 1834-1842 (1989)

    • Related Report
      1989 Annual Research Report
  • [Publications] 横山陽: "金属イオンの高選択的組織内濃縮-核医学診断薬剤の開発" 細胞. 22. 28-31 (1990)

    • Related Report
      1989 Annual Research Report
  • [Publications] Yasuhisa Fujibayashi: "62-Cu-Labeling of Human Serum Albumin-Dithiosemicarbazone Conjugate(HSA-DTS)for Regional Plasma Volume Measurement:Application of New 62-Zn/62-Cu Generator System" Chemical & Pharmaceutical Bulletin. 37. (1990)

    • Related Report
      1989 Annual Research Report
  • [Publications] Takako Furukawa: "Ga-Labeling of IgG with High Specific Radioactivity" Chemical & Pharmaceutical Bulletin.

    • Related Report
      1989 Annual Research Report
  • [Publications] 藤林康久: Journal of Nuclear Medicine(Supplement). 29. 930 (1988)

    • Related Report
      1988 Annual Research Report
  • [Publications] 藤林康久: Journal of Nuclear Medicine.

    • Related Report
      1988 Annual Research Report
  • [Publications] 藤林康久: Journal of Nuclear Medicine.

    • Related Report
      1988 Annual Research Report
  • [Publications] 荒野泰: Nuclear Medicine and Biology.

    • Related Report
      1988 Annual Research Report

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Published: 1987-04-01   Modified: 2016-04-21  

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