A Fast-Binding, Functionally Reversible, COX-2 Radiotracer for CNS PET Imaging.

ABSTRACT: Cyclooxygenase-2 (COX-2) is an enzyme that plays a pivotal role in peripheral inflammation and pain via the prostaglandin pathway. In the central nervous system (CNS), COX-2 is implicated in neurodegenerative and psychiatric disorders as a potential therapeutic target and biomarker. However, clinical studies with COX-2 have yielded inconsistent results, partly due to limited mechanistic understanding of how COX-2 activity relates to CNS pathology. Therefore, developing COX-2 positron emission tomography (PET) radiotracers for human neuroimaging is of interest. This study introduces [¹¹C]BRD1158, which is a potent and uniquely fast-binding, selective COX-2 PET radiotracer. [¹¹C]BRD1158 was developed by prioritizing potency at COX-2, isoform selectivity over COX-1, fast

SUBMITTER: Placzek MS 

PROVIDER: S-EPMC11117721 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature