Preclinical characterization of [¹⁸F]D₂-LW223: an improved metabolically stable PET tracer for imaging the translocator protein 18 kDa (TSPO) in neuroinflammatory rodent models and non-human primates.

ABSTRACT: Positron emission tomography (PET) targeting translocator protein 18 kDa (TSPO) can be used for the noninvasive detection of neuroinflammation. Improved in vivo stability of a TSPO tracer is beneficial for minimizing the potential confounding effects of radiometabolites. Deuteration represents an important strategy for improving the pharmacokinetics and stability of existing drug molecules in the plasma. This study developed a novel tracer via the deuteration of [¹⁸F]LW223 and evaluated its in vivo stability and specific binding in neuroinflammatory rodent models and nonhuman primate (NHP) brains. Compared with LW223, D₂-LW223 exhibited improved binding affinity to TSPO. Compared with [¹⁸F]LW223, [¹⁸F]D₂-LW223 has superior physicochemi

SUBMITTER: Liao K 

PROVIDER: S-EPMC11747005 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature