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化学进展 2011, Vol. 23 Issue (7): 1501-1506 前一篇   后一篇

• 放射化学专辑 •

F-18标记放射性药物的新方法与新技术

黄华璠, 梁坤, 刘玉鹏, 黄士堂, 褚泰伟*   

  1. 北京大学化学与分子工程学院 放射化学与辐射化学重点学科实验室 北京分子科学国家实验室 北京 100871
  • 收稿日期:2010-10-01 修回日期:2011-03-01 出版日期:2011-07-24 发布日期:2012-03-15
  • 通讯作者: e-mail: twchu@pku.edu.cn E-mail:twchu@pku.edu.cn
  • 基金资助:

    国家自然科学基金项目(No.20771011,21071010)资助

下载PDF ( 1329 ) 引用
导出 被引次数 ( 5 )

New Methods and Techniques for F-18-labeled Radiopharmaceuticals

Huang Huafan, Liang Kun, Liu Yupeng, Huang Shitang, Chu Taiwei*   

  1. Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
  • Received:2010-10-01 Revised:2011-03-01 Online:2011-07-24 Published:2012-03-15

PET显像技术具有高分辨率和高灵敏度。这一技术需要合适的正电子核素标记的药物。在一系列核素中,18F是最适用于PET显像的。但是,氟的化学性质限制了18F药物的合成策略,大部分药物的18F标记费时费力。本文介绍了近几年18F标记放射性药物的新方法与新技术,包括18F 脱标识法、18F-FDG直接标记多肽、Al18F络合标记、水溶液中18F-氟硼酸酯的标记、基于微流控芯片的PET药物标记合成技术等,旨在为有关研究者提供参考。

关键词： 放射性药物化学, 标记, 硼酸酯, 微流控芯片, 氟-18

The availability of radiopharmaceuticals is one prerequisite for positron emission tomography (PET) investigation. 18F appears to be the best candidates among a number of positron emission nuclides. Nevertheless, the chemistry of fluorine limits 18F labeling strategies, the preparation of many 18F-labeling radiopharmaceuticals is still laborious and time-consuming. In this review, new 18F-labeling methods and techniques are described in radiopharmaceutical chemistry, including detagging 18F-labeled methodology, direct radiolabeling of peptides with FDG, Al18F-chelated labeling, aqueous 18F-labeling of boronic esters, microfluidics-based radiochemical synthesis technologies for PET probes and so on. This review will provide an overview in new 18F-labeling methods and techniques for researchers.

Contents
1 Introduction
2 Detagging 18F-labeling methodology
3 18F-labeling of peptides
3.1 Direct radiolabeling of peptides with [18F]FDG
3.2 Al 18F-labeling of NOTA conjugated peptides
4 Aqueous 18F-labeling of boronic esters
5 Microfluidics-based radiochemical synthesis technologies for PET probes
5.1 FDG synthesis using microfluidic devices
5.2 Other 18F-labeled PET probes prepared by microfluidics
6 Conclusion and outlook

Key words: radiopharmaceutical chemistry, labeling, boronic ester, microfluidic, fluoro-18

中图分类号: 

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