多功能模块合成心肌显像剂^(18)F-FTHA及Micro-PET显像

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

用国产氟多功能模块合成心肌脂肪酸代谢显像剂18 F-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18 F-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50min。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,60min心肌摄取为19.04ID%/g;心与肝放射性摄取比在60~90min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。

18F-6-thia-14-fluoro-heptadecanoic acid （ISF-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. Biodistri- bution studies in the NH rats and Micro-PET/CT imaging studies in the SD rat were per- formed. The results showed that total synthesis time was about 50 minutes and the uncor- rected 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.