A metabolically stable PET tracer for imaging synaptic vesicle protein 2A: synthesis and preclinical characterization of [¹⁸F]SDM-16.

ABSTRACT:

Purpose

To quantify the synaptic vesicle glycoprotein 2A (SV2A) changes in the whole central nervous system (CNS) under pathophysiological conditions, a high affinity SV2A PET radiotracer with improved in vivo stability is desirable to minimize the potential confounding effect of radiometabolites. The aim of this study was to develop such a PET tracer based on the molecular scaffold of UCB-A, and evaluate its pharmacokinetics, in vivo stability, specific binding, and nonspecific binding signals in nonhuman primate brains, in comparison with [¹¹C]UCB-A, [¹¹C]UCB-J, and [¹⁸F]SynVesT-1.

Methods

The racemic SDM-16 (4-(3,5-difluorophenyl)-1-((2-methyl-1H-imidazol-1-yl)methyl)pyrrolidin-2-one) and its two enantiomers were synthesized and assayed fo

SUBMITTER: Zheng C 

PROVIDER: S-EPMC8940841 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature