基于同位素交换的^(18)F标记方法研究进展  

Research progress on isotope-exchange-based ^(18)F-labeling methods

作　　者：吕圣吉 李中婧 李子婧 Lyu Shengji;Li Zhongjing;Li Zijing(Center for Molecular Imaging and Translational Medicine,School of Public Health,Xiamen University,Xiamen 361102,China)

机构地区：[1]厦门大学公共卫生学院分子影像暨转化医学研究中心,厦门361102

出　　处：《中华核医学与分子影像杂志》2023年第5期316-320,共5页Chinese Journal of Nuclear Medicine and Molecular Imaging

基　　金：国家自然科学基金(81971674)。

摘　　要：采用同位素交换策略进行18F标记具有以下特点:(1)可以实现部分水相标记;(2)反应条件相对温和;(3)标记产物无需分离操作。其适用于敏感生物分子的一步标记, 具有临床应用潜力。该文系统综述了发生在碳原子和非碳原子(硅、硼、磷、硫、镓和铁)上的18F/19F同位素交换方法, 探讨了不同反应类型、标记条件以及典型标记底物上的不同取代基团等因素对放射化学产率、摩尔比活度的影响, 浅析了各个标记方法的前沿应用。The application of isotope exchange can realize radiolabeling in partially aqueous media,proceed under mild reaction conditions,and exclude complex purification procedure.It is suitable for one-step labeling of sensitive biomolecules with clinical application potential.This review systematically introduces the ^(18)F/19F isotope exchange reactions based on carbon and those non-carbon-based reaction centers including silicon,boron,phosphorus,sulfur,gallium and iron.Discussions of the effects on isotope exchange radiochemical yields and molar activities by different reaction types,and labeling conditions and substitute groups on classic labeled substrate are held where possible,as well as recent applications in using these methodologies to develop PET probes.

关 键 词：同位素标记 氟放射性同位素 发展趋势 

分 类 号：R811[医药卫生—放射医学]