Zhu Xing-Xing, He Yun-Lin, Xie Ji-Kui, Wang Kai-Xuan, Wang Shi-Cun, Xie Qiang
Department of Nuclear Medicine, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, Anhui, China.
School of Pharmacy, Bengbu Medical College, Bengbu, 233030, Anhui, China.
Appl Radiat Isot. 2022 Jun;184:110213. doi: 10.1016/j.apradiso.2022.110213. Epub 2022 Mar 23.
Rheumatoid arthritis (RA) is a common autoimmune disease characterized by chronic synovial inflammation, which ultimately leads to joint deformity and dysfunction. [F]-GE-180 is a specific PET tracer of the 18 kDa translocator protein (TSPO), which is overexpressed on activated macrophages, and proposed as a biomarker of inflammation. Our study addresses the need to streamline the automatic synthesis of [F]-GE-180 to make it more accessible for routine production and widespread clinical evaluation and application. The nucleophilic radiofluorination was performed on an AllinOne synthesis module by SPE purification method, and the formulated [F]-GE-180 was obtained in non-decay corrected radiochemical yields of 69 ± 1.8% in 32 min. PET/CT imaging in animal model showed that [F]-GE-180 highly concentrated in joints from RA rats. This methodology facilitates efficient synthesis of [F]-GE-180 in a commercially available synthesis module and shows potential diagnosis performance in RA models.
类风湿性关节炎（RA）是一种常见的自身免疫性疾病，其特征为慢性滑膜炎症，最终会导致关节畸形和功能障碍。[F]-GE-180是18 kDa转位蛋白（TSPO）的一种特异性PET示踪剂，该蛋白在活化巨噬细胞上过度表达，并被提议作为炎症的生物标志物。我们的研究满足了简化[F]-GE-180自动合成的需求，使其更便于进行常规生产以及广泛的临床评估和应用。亲核放射性氟化反应通过固相萃取（SPE）纯化方法在一体化合成模块上进行，在32分钟内以非衰变校正放射性化学产率69±1.8%获得了配制好的[F]-GE-180。动物模型中的PET/CT成像显示，[F]-GE-180高度浓聚于类风湿性关节炎大鼠的关节中。该方法有助于在市售合成模块中高效合成[F]-GE-180，并在类风湿性关节炎模型中显示出潜在的诊断性能。
