Development of Carbon-11 Labeled Pyrimidine Derivatives as Novel Positron Emission Tomography (PET) Agents Enabling Brain Sigma-1 Receptor Imaging.

ABSTRACT: The sigma-1 receptor (σ1R) is a stress-activated chaperone protein that has emerged as a significant therapeutic target for neurodegenerative disorders. Developing effective positron emission tomography (PET) imaging probes targeting σ1R is crucial for visualizing its distribution and function in the brain, as well as facilitating related drug development. In this study, two novel ¹¹C-labeled PET probes based on the structure of a potent σ1R ligand Lan-0101 are designed and synthesized. PET imaging studies in mice reveal that [¹¹C]CNY-01 exhibits good brain uptake and binding specificity. Subsequent evaluation in non-human primates further demonstrates that [¹¹C]CNY-01 displays favorable brain penetration, slow clearance kinetics, and characteristics of irr

SUBMITTER: Bai P 

PROVIDER: S-EPMC12140300 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature