Simplified one-pot ¹⁸F-labeling of biomolecules with in situ generated fluorothiophosphate synthons in high molar activity.

ABSTRACT: Rationale: Conventional ¹⁸F-labeling methods that demand substrate pre-modification or lengthy radiosynthesis procedures have impeded the visualization and translation of numerous biomolecules, as biomarkers or ligands, using modern positron emission tomography techniques in vivo. Moreover, ¹⁸F-labeled biomolecules in high molar activity (A_m) that are indispensable for sensitive imaging could be only achieved under strict labeling conditions. Methods: Herein, ¹⁸F-labeled fluorothiophosphate (FTP) synthons in high A_m have been generated rapidly in situ in reaction solutions with < 5% water via nucleophilic substitution by wet [¹⁸F]F^-, which required minimal processing from cyclotr

SUBMITTER: Yang H 

PROVIDER: S-EPMC9830440 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature