基于ExploraGN／LC双模块的16α-[^18F]氟-17β-雌二醇全自动化合成

Fully automated synthesis of 16a-[ ^18F ] fluoro-17β-estrogen using Explora GN/LC dual module

目的应用多功能放射性药物标记模块Explora GN联合液相分离模块ExploraLC制备高纯度的16a-[^18F]氟-17β-雌二醇（^18F-FES）。方法基于ExploraGN多功能合成模块和ExploraLC液相色谱分离模块，同时结合自制的固相萃取装置，采用“一锅法”完成^18F—FES的合成和分离。用分析型HPLC测^18F-FES的放化纯。进行^18F-FES与ER阳性细胞（MCF-7细胞）的饱和结合实验。结果该方法的总合成时间（包括HPLC分离和赋型）为60min，放射化学产率为45％（衰减校正之后），放化纯〉98％，没有明显的化学杂质。MCF-7细胞和^18F-FES结合表现为受体与配体的可饱和性实验特性，Kd和Bmax分别为（2．922±0．619）nmol／L和（4．193±0．360）nmol／L。结论应用ExploraGN／LC双模块成功地制备了高化学纯度和高放化纯的^18F—FES；^18F-FES具有与ER结合的特性，可为乳腺癌ERPET／CT显像提供安全、有效的特异性显像剂。

Objective To-synthesize 16a- [ ^18 F ] fluoro-17β-estrogen （ ^18 F-FES） with high chemical and radiochemical purity using multifunctional radiolabeling module of Explora GN and separation module of Explora LC （Explora GN/LC dual module）. Methods Explora GN/LC dual module and ＂one-pot＂ radiochemical process were applied for fully automated synthesis and separation of ^18F-FES. The radiochemical purity of ^18F-FES was analyzed by HPLC. The saturation binding test of ^18F-FES with ER （ER-positive MCF-7 cell line） was applied to examine the biological activity of 18 F-FES. Results is F-FES synthesis procedure took 60 min, with radiochemical yield about 45% and radiochemical purity higher than 98%. The Kd and Bmax of MCF-7 cells with is F-FES were （2. 922 ± 0.619） nmol/L and （4. 193 ± 0. 360） nmol/L respectively. Conclusions 18 F-FES can be automatically synthesized by Explora GN/LC dual module with high chemical purity and radioehemieal purity. It would be a potential PET tracer to be used in estrogen-relatod molecular imaging.