A Facile Radiolabeling of [(18)F]FDPA via Spirocyclic Iodonium Ylides: Preliminary PET Imaging Studies in Preclinical Models of Neuroinflammation

通过螺环碘鎓叶立德对[(18)F]FDPA进行简便的放射性标记:神经炎症临床前模型中的初步PET成像研究

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Abstract

A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a (18)F-ligand, [(18)F]2 ([(18)F]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [(18)F]2 demonstrated saturable specific binding to TSPO, substantially elevated brain uptake, and slow washout of bound PET signal in the preclinical models of brain neuroinflammation (cerebral ischemia and Alzheimer's disease).

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