First-in-Humans Brain PET Imaging of the GluN2B-Containing N-methyl-d-aspartate Receptor with (R)-¹¹C-Me-NB1.

ABSTRACT: The N-methyl-d-aspartate receptor (NMDAR) plays a crucial role in neurodegenerative diseases such as Alzheimer disease and in the treatment of major depression by fast-acting antidepressants such as ketamine. Given their broad implications, GluN2B-containing NMDARs have been of interest as diagnostic and therapeutic targets. Recently, (R)-¹¹C-Me-NB1 was investigated preclinically and shown to be a promising radioligand for imaging GluN2B subunits. Here, we report on the performance characteristics of this radioligand in a first-in-humans PET study. Methods: Six healthy male subjects were scanned twice on a fully integrated PET/MR scanner with (R)-¹¹C-Me-NB1 for 120 min. Brain uptake and tracer distribution over time were investigated by SUV

SUBMITTER: Rischka L 

PROVIDER: S-EPMC9157734 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature