摘要
目的制备L-6-^18F-多巴（18F-FDOPA）并探讨其在小鼠体内生物分布及药代动力学，评价其探测胰岛素瘤的可行性。方法采用亲核反应三步法合成^18F-FDOPA，测定其标记率、放化纯及体外稳定性。注射后2、5、15、30、60和120 min分别处死正常小鼠（每时间点3只）获得主要脏器的放射性计数，行microPET动态观察18F-FDOPA在正常小鼠体内的生物分布。建立胰岛素瘤INS-1细胞株荷瘤裸鼠模型，行microPET动态扫描；勾画感兴趣区（ROI），获得正常小鼠主要脏器及荷瘤裸鼠肿瘤时间-放射性曲线（TAC）。结果18F-FDOPA标记合成产率为（11.0±0.4）%，放化纯为（99.3±0.2）%，室温放置120 min放化纯仍〉99%。^18F-FDOPA主要经肾脏排泄，血液内清除较快；注射后20～50 min胰腺摄取相对稳定，2个时间点摄取分别为（5.98±0.71）和（4.62±0.47）每克组织百分注射剂量率（%ID/g）。INS-1肿瘤早期相（2 min）有显著放射性摄取[（11.42±0.70） %ID/g]。结论^18F-FDOPA标记合成方法简单、放化纯高、稳定性好；早期显像有利于胰岛素瘤的检出。
ObjectiveTo synthesize ^18F-fluoro-L-3, 4-dihydroxyphenylalanine （^18F-FDOPA） and evaluate its biodistribution and kinetics in mice, in order to explore its feasibility for insulinoma detection.Methods18F-FDOPA was synthesized by a three-step nucleophilic reaction. Radiolabeling yield, radiochemical purity and stability in vitro were analyzed. Normal mice were scarified at 2, 5, 15, 30, 60 and 120 min postinjection to measure radioactive counts in main organs. Biodistribution and kinetics were evaluated by dynamic microPET in normal mice. The insulinoma tumor （INS-1） model was established and dynamic microPET was performed immediately after intravenous injection and stopped at 60 min. Region of interest （ROI） was drawn to access time-activity curve （TAC） in main organs and insulinoma.Results18F-FDOPA was prepared with radiochemical yield of （11.0±0.4）%, radiochemical purity of （99.3±0.2）%. The radiochemical purity was still 〉99% after being stored for 120 min at room temperature. Predominant uptake of ^18F-FDOPA was in the kidneys, and was cleared rapidly in blood. Pancreas showed stable uptake from 20 to 50 min, which was （5.98±0.71） percentage activity of injection dose per gram of tissue （%ID/g） at 20 min and （4.62±0.47） %ID/g at 50 min postinjection, respectively. ^18F-FDOPA showed high affinity to tumor tissue of insulinoma （（11.42±0.70） %ID/g） at 2 min.Conclusions18F-FDOPA could be easily synthesized in short total reaction time with high radiochemical purity and stability. Early phase imaging of ^18F-FDOPA may be helpful for insulinoma detection.
作者
赵震宇
张思伟
张朋俊
金志铭
张颖冬
王峰
Zhao Zhenyu;Zhang Siwei;Zhang Pengjun;Jin Zhiming;Zhang Yingdong;Wang Feng(Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, Nanjing 210006, China （ Zhao ZY, Zhang P J, Wang F;Department of Neurology, Nanjing First Hospital, Nanjing Medical University, Nanjing 210006, China （ Zhang YD;Department of Drug Research, Jiangsu Hnayi Technology Co. Ltd., Changshu 215522, China （Zhang SW, Jin ZM)
出处
《中华核医学与分子影像杂志》
CAS
北大核心
2018年第6期408-411,共4页
Chinese Journal of Nuclear Medicine and Molecular Imaging
基金
江苏省重点研发专项基金（BE2017612,BL2014014）
