[^(18)F]FDOPA放射标记合成工艺研究进展  

Research progress in radiolabelling synthesis of[^(18)F]FDOPA

作　　者：彭灿 董国生 李希臣 李政 韩雨霏 张涛 PENG Can;DONG Guo-sheng;LI Xi-chen;LI Zheng;HAN Yu-fei;ZHANG Tao(Department of Radiopharmaceuticals,School of Pharmacy,Nanjing Medical University,Nanjing 211166,China;Nuclear Medicine Clinical Transformation Center,Nanjing Medical University,Nanjing 210029,China)

机构地区：[1]南京医科大学药学院核药学系,南京211166 [2]南京医科大学核医药临床转化中心,南京210029

出　　处：《中国新药杂志》2024年第12期1233-1242,共10页Chinese Journal of New Drugs

基　　金：国家自然科学基金资助项目(12275135);江苏省高校自然科学研究项目(21KJB350015,22KJB350008);南京医科大学引进人才科研启动基金资助项目(NMUR20210003);南京医科大学内涵建设重点项目;南京医科大学科技发展基金资助项目(NMUB20210014)。

摘　　要：正电子发射断层扫描(positron emission tomography,PET)放射性示踪剂6-[^(18)F]氟-3,4-二羟基-L-苯丙氨酸([^(18)F]6-fluoro-3,4-dihydroxy-L-phenylalanine,[^(18)F]FDOPA)广泛用于中枢神经系统疾病的多巴胺代谢成像,然而以高产率放射性合成高比活度的[^(18)F]FDOPA极其困难。近年来随着[^(18)F]FDOPA在脑肿瘤、神经内分泌肿瘤和婴儿期局灶性高胰岛素血症等恶性疾病中的广泛应用,迫切需要开发更优的[^(18)F]FDOPA合成方法以满足日益增长的临床需求。该综述总结了[^(18)F]FDOPA放射合成工艺的研究进展,并且详细介绍了由不同放射标记方法所获得[^(18)F]FDOPA的放射性化学产率、比活度、对映体纯度和合成时间,为优化[^(18)F]FDOPA的放射性合成提供参考,以期获得适用于临床研究的高放射性化学放化产率和纯度以及高比活度的[^(18)F]FDOPA。The PET radiotracer,[^(18)F]6-fluoro-3,4-dihydroxy-L-phenylalanine([^(18)F]FDOPA),is widely used to image dopamine metabolism in central nervous system diseases.However,the radiosynthesis of[^(18)F]FDOPA in high radiochemical yields and specific activities is quite challenging.In recent years,with the widespread application of[^(18)F]FDOPA in malignant diseases such as brain tumors,neuroendocrine tumors,and focal hyperinsulinemia in infancy,there is an urgent need to develop improved synthetic approaches for[^(18)F]FDOPA to fulfill growing clinical demands.This review summarizes the research progress of radiosynthetic process of[^(18)F]FDOPA and introduces radiochemical yields,specific activities,enantiomeric purities,and synthesis time of[^(18)F]FDOPA from different radiolabeling strategies in details.This review could be a reference for optimization of[^(18)F]FDOPA radiosynthesis to obtain[^(18)F]FDOPA with high radiochemical yield and purity as well as high specific activity which is suitable for clinical studies.

关 键 词：6-[^(18)F]氟-3 4-二羟基-L-苯丙氨酸 正电子发射断层扫描 放射化学合成 放化产率 中枢神经系统疾病 

分 类 号：R963[医药卫生—微生物与生化药学]