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2022 Fiscal Year Final Research Report

Development of efficient microscale automated module for radiosynthesis of 18F-labeled probes

Research Project

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Project/Area Number 20H03614
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Review Section Basic Section 52040:Radiological sciences-related
Research InstitutionTohoku University

Principal Investigator

Iwata Ren  東北大学, サイクロトロン・ラジオアイソトープセンター, 名誉教授 (60143038)

Co-Investigator(Kenkyū-buntansha) 高橋 和弘  福島県立医科大学, 公私立大学の部局等, 教授 (20370257)
原田 龍一  東北大学, 医学系研究科, 助教 (60735455)
Project Period (FY) 2020-04-01 – 2023-03-31
Keywordsマイクロスケール合成 / フッ素-18 / PETプローブ / 自動合成 / 標識反応 / 濃縮法
Outline of Final Research Achievements

Concentration-based microscale radiosynthesis (CBMR) of 18F-labeled probes, where a reaction solution was concentrated into DMSO by evaporating MeCN, was developed. A small AG MP-1 (1.5-2 mg) column allowed to reduce the volume of 20 mM K.222/KHCO3-MeOH to 50 uL by normal flow and to 10 uL by counter-flow for efficient release of [18F]fluoride (>90%). This method was applied to the automated 10-20 uL scale preparations of [18F]FET in overall radiochemical yields of 46±6% using a movable microsyringe. The CBMR was also successfully introduced to preparations of [18F]FDOPA and some probe on a commercial automated module such as a GE FASTlab and an SHI MPS200.
The CBMR method was improved for its robust, reproducible 18F-labeling reaction by changing the concentration procedure and then applied to radiosynthesis of five 18F-labed probes such as [18F]SMBT-1. Finally, a new, compact automated module for CBMR, consisting of 5 6-way valves and 5 microsyringe modules, was developed.

Free Research Field

PET診断プローブの自動合成装置開発

Academic Significance and Societal Importance of the Research Achievements

PETプローブ合成にマイクロスケール濃縮合成法を適用することで、反応に要する高価な前駆体やHPLC精製溶媒の使用量を大幅に削減でき、高品質なプローブの迅速な調製が可能になり、その有用性は非常に大きい。加えて、少ない18F放射能量と試薬量で短時間内に繰り返して合成できるため、標識反応条件等の最適化に使用することで新規18F標識プローブの開発を促進できる。また少量で迅速な合成が可能な本法は、多品種少量のPETプローブのオンデマンド合成に最適であり、PET診断の拡大と深化に利するものと期待される。

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Published: 2024-01-30  

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