Comparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates: <i>(R)</i>-[¹¹C]NR2B-Me, <i>(R)</i>-[¹⁸F]of-Me-NB1, and <i>(S)</i>-[¹⁸F]of-NB1.

ABSTRACT: The NMDA receptor GluN2B subunit is a target of interest in neuropsychiatric disorders but to date there is no selective radiotracer available to quantify its availability in vivo. Here we report direct comparisons in non-human primates of three GluN2B-targeting radioligands: (R)-[¹¹C]NR2B-Me, (R)-[¹⁸F]OF-Me-NB1, and (S)-[¹⁸F]OF-NB1. Plasma free fraction, metabolism, tissue distribution and kinetics, and quantitative kinetic modeling methods and parameters were evaluated in two adult rhesus macaques. Free fraction in plasma was <2% for (R)-[¹¹C]NR2B-Me and (R)-[¹⁸F]OF-Me-NB1 and higher for (S)-[¹⁸F]OF-NB1 (15%). All radiotracers showed good brain uptake and distribution throug

SUBMITTER: Smart K 

PROVIDER: S-EPMC9274863 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature