Radiosynthesis and evaluation of a fluorine-18 radiotracer [¹⁸F]FS1P1 for imaging sphingosine-1-phosphate receptor 1.

ABSTRACT: Assessment of sphingosine-1-phosphate receptor 1 (S1PR1) expression could be a unique tool to determine the neuroinflammatory status for central nervous system (CNS) disorders. Our preclinical results indicate that PET imaging with [¹¹C]CS1P1 radiotracer can quantitatively measure S1PR1 expression changes in different animal models of inflammatory diseases. Here we developed a multiple step F-18 labeling strategy to synthesize the radiotracer [¹⁸F]FS1P1, sharing the same structure with [¹¹C]CS1P1. We explored a wide range of reaction conditions for the nucleophilic radiofluorination starting with the key ortho-nitrobenzaldehyde precursor 10. The tertiary amine additive TMEDA proved crucial to achieve high radiochemical yield of ortho-[^18<

SUBMITTER: Qiu L 

PROVIDER: S-EPMC8970350 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature