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