多功能模块合成心肌显像剂18F-FTHA及Micro-PET显像

doi:10.7538/tws.2013.26.04.0222

摘要/Abstract

摘要：

用国产氟多功能模块合成心肌脂肪酸代谢显像剂¹⁸F-FTHA用于临床研究。以苄基-14-(R，S)-对甲苯磺酰基-6-硫代十七烷酸酯为前体，在氟多功能模块上经亲核反应、水解及HPLC纯化，最后经固相萃取，得到¹⁸F-FTHA。研究其在正常NH小鼠体内的生物学分布以及正常SD大鼠Micro-PET显像。结果显示，¹⁸F-FTHA不校正合成效率为10.6%，合成时间为50 min。¹⁸F-FTHA的放化纯度为99%，体外稳定性良好。生物学分布结果表明，60 min心肌摄取为19.04 ID%/g; 心与肝放射性摄取比在60~90 min达到3~6倍；Micro-PET心肌显像清晰。结果提示，国产氟多功能模块合成¹⁸F-FTHA耗时短，放化纯度高，其质量符合氟-18药物的临床。

关键词: ¹⁸F-FTHA, 脂肪酸, 国产多功能模块

Abstract:

¹⁸F-6-thia-14-fluoro-heptadecanoic acid (¹⁸F-FTHA), a free fatty acid, has been used in myocardial PET imaging. In order to establish an automated synthesis module for routine production, a study was performed on domestic synthesis module. Methods: ¹⁸F-FTHA was prepared from Benzyl-14-tosyloxy-6-thia-heptadecanoate as precursor. Biodistribution studies in the NH rats and Micro-PET/CT imaging studies in the SD rat were performed. The results showed that total synthesis time was about 50 minutes and the uncorrected synthesis yield was 10.6%, radiochemical purity was higher than 99%, the product had good stability at room temperature. Biodistribution data in rats showed the uptake of heart was 19.04 ID%/g at 60 minutes, heart-to-liver ratios at 60 and 90 min were 6.4 and 3.2, respectively. Micro-PET/CT imaging of the SD rat showed intense cardiac uptake. Conclusions: Using this procedure a fast, reliable, automated synthesis for the myocardial PET tracer, ¹⁸F-FTHA, can be obtained.

Key words: ¹⁸F-FTHA, fatty acids, domestic synthesis module

张晓军;刘健;孙志军;徐白萱;田嘉禾;张锦明. 多功能模块合成心肌显像剂¹⁸F-FTHA及Micro-PET显像[J]. 同位素, 2013, 26(4): 222-227.

ZHANG Xiao-jun;LIU Jian;SUN Zhi-jun;XU Bai-xuan;TIAN Jia-he;ZHANG Jin-ming. Labeling and Imaging Study of Fatty Acid Analogue ¹⁸F-FHTA on Domestic Synthesis Module[J]. Journal of Isotopes, 2013, 26(4): 222-227.

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多功能模块合成心肌显像剂¹⁸F-FTHA及Micro-PET显像

Labeling and Imaging Study of Fatty Acid Analogue ¹⁸F-FHTA on Domestic Synthesis Module

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