Roy Pritam, Guo Yan, Muzik Otto, Woodcock Eric A, Jiang Huailei
Cyclotron and Radiochemistry Core, Karmanos Cancer Institute Detroit, MI, USA.
PET Center, Karmanos Cancer Institute Detroit, MI, USA.
Am J Nucl Med Mol Imaging. 2024 Dec 15;14(6):351-356. doi: 10.62347/QFGP5253. eCollection 2024.
Colony-stimulating factor 1 receptor (CSF1R) is almost exclusively expressed on microglia in the human brain and thus, has promise as a biomarker for imaging microglia density as a proxy for neuroinflammation. [C]CPPC is a radiotracer with selective affinity to CSF1R, and has been evaluated for in-human microglia PET imaging. The flourine-18 labeled CPPC derivative, 5-cyano-N-(4-(4-(2-[F]fluoroethyl)piperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide ([F]FCPPC), was previously synthesized, however, with a low radiochemical yield using manual radiosynthesis. In this work, we report a fully automated radiosynthesis of [F]FCPPC on a Synthra RNplus research module. In a total synthesis time of 50 min, [F]FCPPC was obtained in decay corrected radiochemical yields of 26.8 ± 0.1% (n = 3) with >99% radiochemical purities. Quality control testing showed that [F]FCPPC met all release criteria. In sum, we report the first fully automated radiosynthesis of [F]FCPPC, a promising radiopharmaceutical for imaging microglia in humans.
集落刺激因子1受体（CSF1R）几乎仅在人类大脑的小胶质细胞上表达，因此，有望作为一种生物标志物，通过成像小胶质细胞密度来替代神经炎症。[C]CPPC是一种对CSF1R具有选择性亲和力的放射性示踪剂，已用于人体小胶质细胞PET成像评估。氟-18标记的CPPC衍生物5-氰基-N-（4-（4-（2-[F]氟乙基）哌嗪-1-基）-2-（哌啶-1-基）苯基）呋喃-2-甲酰胺（[F]FCPPC）此前已合成，但采用手动放射性合成时放射化学产率较低。在本研究中，我们报告了在Synthra RNplus研究模块上对[F]FCPPC进行的全自动化放射性合成。在50分钟的总合成时间内，获得了衰变校正放射化学产率为26.8±0.1%（n = 3）且放射化学纯度>99%的[F]FCPPC。质量控制测试表明，[F]FCPPC符合所有放行标准。总之，我们报告了[F]FCPPC的首次全自动化放射性合成，[F]FCPPC是一种用于人体小胶质细胞成像的有前景的放射性药物。
