Synthesis and Biological Evaluation of Enantiomerically Pure (R)- and (S)-[¹⁸F]OF-NB1 for Imaging the GluN2B Subunit-Containing NMDA receptors.

ABSTRACT: GluN2B subunit-containing N-methyl-d-aspartate (NMDA) receptors have been implicated in various neurological disorders. Nonetheless, a validated fluorine-18 labeled positron emission tomography (PET) ligand for GluN2B imaging in the living human brain is currently lacking. As part of our PET ligand development program, we have recently reported on the preclinical evaluation of [¹⁸F]OF-NB1 - a GluN2B PET ligand with promising attributes for potential clinical translation. However, the further development of [¹⁸F]OF-NB1 is currently precluded by major limitations in the radiolabeling procedure. These limitations include the use of highly corrosive reactants and racemization during the radiosynthesis. As such, the aim of this study was to develop a synthetic appro

SUBMITTER: Korff M 

PROVIDER: S-EPMC9901044 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature