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


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).

SUBMITTER: Wang L 

PROVIDER: S-EPMC5576052 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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

Wang Lu L   Cheng Ran R   Fujinaga Masayuki M   Yang Jian J   Zhang Yiding Y   Hatori Akiko A   Kumata Katsushi K   Yang Jing J   Vasdev Neil N   Du Yunfei Y   Ran Chongzhao C   Zhang Ming-Rong MR   Liang Steven H SH  

Journal of medicinal chemistry 20170605 12


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

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