中山大学学报（医学科学版）2011，Vol.32Issue(1)：99-103,115,6.
18F-氟代乙酸盐自动化合成及其动物实验研究
Rapid Automated Radiosynthesis and Animal Experiments of[18F]Fluoroacetate
摘要
Abstract
[Objective]The aim of the study was to investigate and validate the feasibility of fully automated synthesis of [18F]fluoroacetate (18F-FAC) as an oncologic PET tracer.[Methods]Two fully automated synthetic procedures of 18F-FAC have been developed using benzyl-2-bromoacetate as a precursor.One was an on-column hydrolysis procedure using a IBA 18F-FDG synthesizer, consisting of nucleophilic [18F]fluorination, hydrolysis and purification on the Sep-Pak cartridges.The other one was a two-step one-pot procedure using a modified commercial PET-MF-2V-IT-I synthesizer, consisting of nucleophilic [18F]fluorination and hydrolysis in the same reaction vessel, and purification with the Sep-Pak cartridges.Also, 18F-FAC and 18F-FDG PET images were performed on the mice models bearing hepatocellular carcinoma.[Results]The radiochemical purity of 18F-FAC was 95％ by the two procedures.The on-column hydrolysis procedure was a simple, rapid, and fully automated synthesis of 18F-FAC in a high and reproducible radiochemical yield exceeding 50-60％ (decay uncorrected) within the total synthesis time of 28 min.Whereas,18F-FAC was produced by the one-pot procedure in an uncorrected radiochemical yield of 15-25％ within the total synthesis time of 26 min.18F-FAC PET imaging showed higher uptake of 18F-FAC than 18F-FDG in the tumors.[Conclusion]The new, simple, and rapid on-column hydrolysis procedure should be adaptable to the fully automated synthesis of 18F-FAC on a commercial fluorodeoxyglucose synthesizer.18F-FAC PET imaging is helpful to the diagnosis of hepatocellular carcinoma.关键词
18F-氟代乙酸盐/在柱水解法/一锅法/自动化合成/PET 显像/肝细胞癌分类
医药卫生引用本文复制引用
邓怀福,文富华,唐刚华,王红亮,易畅,吴克宁,史新冲,孟悛非..18F-氟代乙酸盐自动化合成及其动物实验研究[J].中山大学学报（医学科学版）,2011,32(1):99-103,115,6.基金项目
国际原子能机构(IAEA)资助课题(15245) （IAEA）
中山大学"百人计划"引进人才科研启动基金(80000-3126132) （80000-3126132）
国家高技术研究发展计划(863计划)专题课题(2008AA02Z430) （863计划）
