Design, Synthesis, and Evaluation of ¹⁸F-Labeled Tracers Targeting Fibroblast Activation Protein for Brain Imaging.

ABSTRACT: Fibroblast activation protein (FAP) is closely related to central nervous system diseases such as stroke and brain tumors, but PET tracers that can be used for brain imaging have not been reported. Here, we designed, synthesized, and evaluated ¹⁸F-labeled UAMC1110 derivatives suitable for brain imaging targeting FAP. By substituting the F atom for the H atom on the aromatic ring of compound UAMC1110, 1a-c were designed and prepared. 1a-c were confirmed to have a high affinity for FAP through molecular docking and enzyme assay. [¹⁸F]1a-c were successfully prepared and confirmed to have high affinity. The stability in vivo indicates that no obvious metabolites of [¹⁸F]1a

SUBMITTER: Yu Z 

PROVIDER: S-EPMC10644484 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature