Quantification of the purinergic P2X₇ receptor with [¹¹C]SMW139 improves through correction for brain-penetrating radiometabolites.

ABSTRACT: The membrane-based purinergic 7 receptor (P2X₇R) is expressed on activated microglia and the target of the radioligand [¹¹C]SMW139 for in vivo assessment of neuroinflammation. This study investigated the contribution of radiolabelled metabolites which potentially affect its quantification. Ex vivo high-performance liquid chromatography with a radio detector (radioHPLC) was used to evaluate the parent and radiometabolite fractions of [¹¹C]SMW139 in the brain and plasma of eleven mice. Twelve healthy humans underwent 90-min [¹¹C]SMW139 brain PET with arterial blood sampling and radiometabolite analysis. The volume of distribution was estimated by using one- and two- tissue compartment (TCM) modeling with single (V_T)

SUBMITTER: Brumberg J 

PROVIDER: S-EPMC9903223 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature