用于报告基因hERL表达成像的[¹⁸F]FES全自动合成
Fully automatic synthesis of [¹⁸F]FES for reporter gene hERL expression imaging.
作者信息
Liang Sheng, Lan Xiaoli, Zhang Yongxue, Xu Xuemin, Li Biao
机构信息
Department of Nuclear Medicine, Ruijin Hospital, School of Medicine, Institute of Med-X, Shanghai Jiaotong University, Shanghai, China.
出版信息
Nucl Med Commun. 2012 Jan;33(1):29-33. doi: 10.1097/MNM.0b013e32834d3b92.
We have developed a fully automatic method for the synthesis of 16α-[¹⁸F]fluoroestradiol ([F]FES) using a TRACERlab FXFN module. Following [¹⁸F]fluorination, the intermediate was hydrolyzed with a mixture of 2 N HCl in acetonitrile (CH3CN) and then neutralized with sodium bicarbonate (NaHCO3). After HPLC purification, the decay-corrected radiochemical yield of [¹⁸F]FES was 50 ± 2.35% (n=4), which was stable up to 96.1 ± 0.3% (n=4) at 8 h. This new fully automated synthesis method provided high and reproducible yields and the produced [F]FES could be used to monitor in-vivo human estrogen receptor α ligand binding domain gene expression using PET images.
我们开发了一种使用TRACERlab FXFN模块全自动合成16α-[¹⁸F]氟雌二醇（[F]FES）的方法。在进行[¹⁸F]氟化反应后，中间体用2N盐酸与乙腈（CH3CN）的混合溶液进行水解，然后用碳酸氢钠（NaHCO3）中和。经过高效液相色谱纯化后，[¹⁸F]FES的衰变校正放射化学产率为50±2.35%（n = 4），在8小时内其稳定性高达96.1±0.3%（n = 4）。这种全新的全自动合成方法提供了高且可重复的产率，所制备的[F]FES可用于通过正电子发射断层扫描（PET）图像监测体内人类雌激素受体α配体结合域基因的表达。
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