The development of delivery systems to transport some specific radiotracers across the blood-brain barrier (BBB) needs to be investigated for brain imaging. [¹⁸F]FLT (3′-deoxy-3′-¹⁸F-fluoro-l-thymidine), an analogue substrate of the nucleoside thymidine, has been developed as a proliferation tracer for oncological PET studies. Unfortunately, low-grade brain tumors are poorly visualized due to the low uptake of [¹⁸F]FLT in brain tissue, preventing its use in PET imaging to detect brain tumors at an early stage. Based on our previous work, a redox chemical delivery system (CDS) related to Bodor’s strategy was developed to enable the penetration of FLT into the brain. To this end, FLT was covalently linked to a series of lipophilic carriers based on a 1,4-dihydroquinoline structure. To determine the best carrier, various sets of [¹¹C]CDS-FLT were prepared and injected into rats. Pleasingly, in vivo results let us suggest that this CDS is a promising approach to overcome the BBB to target low-grade brain tumors for PET imaging.

中文翻译：

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通过有前途的靶向系统将FLT输送至中枢神经系统：合成，[ ¹¹ C]放射合成和体内评估

需要研究开发用于跨血脑屏障（BBB）转运某些特定放射性示踪剂的递送系统的方法，以进行脑成像。[ ¹⁸ F] FLT（3'-脱氧-3'- ¹⁸ F-氟-1-胸苷），一种核苷胸苷的类似底物，已被开发为肿瘤PET研究的增殖示踪剂。不幸的是，由于低摄取[ ¹⁸F] FLT在脑组织中发挥作用，阻止其在PET成像中用于早期检测脑部肿瘤。在我们之前的工作的基础上，开发了与Bodor策略有关的氧化还原化学物质输送系统（CDS），以使FLT能够渗透到大脑中。为此，将FLT与基于1，4-二氢喹啉结构的一系列亲脂性载体共价连接。为了确定最佳的载体，制备了各组[ ¹¹ C] CDS-FLT并注射到大鼠中。令人高兴的是，体内结果让我们建议，这种CDS是克服BBB靶向低级脑肿瘤以进行PET成像的一种有前途的方法。