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

Journal of Medicinal Chemistry
Lu WangSteven H Liang

Abstract

A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a 18F-ligand, [18F]2 ([18F]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [18F]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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Citations

Oct 7, 2017·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Chongzhao RanAnna Moore
Mar 16, 2019·Nuclear Medicine Communications·He ZhangDengfeng Cheng
Jan 12, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Tamara BerdyyevaAnna Katrin Szardenings
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Oct 6, 2017·Journal of Labelled Compounds & Radiopharmaceuticals·Victor W Pike
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Jul 11, 2021·European Journal of Nuclear Medicine and Molecular Imaging·Nadja Van CampHervé Boutin
Sep 21, 2021·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Francisco R López-PicónOlof Solin

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