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

Joachim Brumberg, Richard Aarnio, Anton Forsberg, Päivi Marjamäki, Vera Kerstens, Mohammad M Moein, Sangram Nag, Saara Wahlroos, Michael Kassiou, Albert D Windhorst, Christer Halldin, Merja Haaparanta-Solin, Patrik Fazio, Vesa Oikonen, Juha O Rinne & Andrea Varrone
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...
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