^(18)F标记氟甲基胆碱的半自动合成及其生物分布

Semi-automatic Synthesis and Biological Evaluation of ^(18)F-FCH as an Oncologic PET Tracer

利用18F-FDG化学合成模块(CPCU)改装的半自动化多用氟标药物仪合成了氟甲基胆碱(18F-FCH),并进行了放射化学纯度测定、稳定性分析、生物分布、荷瘤小鼠显像以及安全性检验。利用半自动装置合成只需要55 min,产率稳定,产品的放射化学纯度大于99%,体外稳定性良好1。8F-FCH的正常小鼠体内分布与文献报道的11C-Choline相似,毒性较小。荷瘤小鼠显像结果表明,18F-FCH可选择性地浓集于肿瘤细胞,是较好的肿瘤显像剂。

^18F-fluromethylcholine （^18F-FCH） as a PET tracer is synthesized. The semi-automatic synthesis assembly of ^18F-FCH is modified from CPCU（CTI）. The radiochemical purity is measured by analytical HPLC. The radiochemical yield and the radiochemical purity of ^18F-FCH are 15% and 〉99 %, respectively. The total radiosynthesis time is 55 rain after EOB. The labeled product exhibited low toxicity. The biodistribution in normal mice and the toxicity are studied. PET imaging with ^18F-FCH is performed on tumor xenograft murine model. The semi-automatic synthesis assembly is promising to be used for routine clinic radiopharmaceutial preparation and preliminary study has shown the usefulness of ^18F-FCH as an oncologic PET tracer.