Synthesis and Preliminary Evaluations of a Triazole-Cored Antagonist as a PET Imaging Probe ([¹⁸F]N2B-0518) for GluN2B Subunit in the Brain.

ABSTRACT: GluN2B is the most studied subunit of N-methyl-d-aspartate receptors (NMDARs) and implicated in the pathologies of various central nervous system disorders and neurodegenerative diseases. As pan NMDAR antagonists often produce debilitating side effects, new approaches in drug discovery have shifted to subtype-selective NMDAR modulators, especially GluN2B-selective antagonists. While positron emission tomography (PET) studies of GluN2B-selective NMDARs in the living brain would enable target engagement in drug development and improve our understanding in the NMDAR signaling pathways between normal and disease conditions, a suitable PET ligand is yet to be identified. Herein we developed an ¹⁸F-labeled potent antagonist, 2-((1-(4-[¹⁸F]fluoro-3-methylphenyl)-1 H-1,2,3-tr

SUBMITTER: Fu H 

PROVIDER: S-EPMC6727982 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature