American journal of nuclear medicine and molecular imaging · 2024
Radiosynthesis and evaluation of a novel 18F-labeled tracer for PET imaging of glycogen synthase kinase 3.
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Xiao Zhiwei, Li Yinlong, Haider Ahmed, Pfister Stefanie K, Rong Jian, Chen Jiahui, Zhao Chunyu, Zhou Xin, Song Zhendong, Gao Yabiao, Patel Jimmy S, Collier Thomas L, Ran Chongzhao, Zhai Chuangyan, Yuan Hongjie, Liang Steven H
Аннотация
Glycogen synthase kinase 3 (GSK3) is a multifunctional serine/threonine kinase family that regulates diverse biological processes including glucose metabolism, insulin activity and energy homeostasis. Dysregulation of GSK3 is implicated in the development of several diseases such as type 2 diabetes mellitus, Alzheimer's disease (AD), and various cancer types. In this study, we report the synthesis and evaluation of a novel positron emission tomography (PET) ligand compound 28 (codenamed [18F]GSK3-2209). The PET ligand [18F]28 was obtained via copper-mediated radiofluorination in more than 32% radiochemical yields, with high radiochemical purity and high molar activity. In vitro autoradiography studies in rodents demonstrated that this tracer exhibited a high specific binding to GSK3. Furthermore, PET imaging studies of [18F]28 revealed its ability to penetrate the blood-brain barrier (BBB).