Imaging of Transmembrane AMPA Receptor Regulatory Proteins by Positron Emission Tomography.

ABSTRACT: The transmembrane α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptor regulatory protein γ-8 (TARP γ-8) constitutes an auxiliary subunit of AMPA receptors, which mediates various brain functions including learning and memory. TARP γ-8 has emerged as a promising therapeutic target for central nervous system disorders. Despite considerable efforts, previously reported TARP γ-8 PET radioligands, such as [¹¹C]TARP-1903 and [¹¹C]TARP-1811 series, were plagued by limited brain uptake and/or high nonspecific binding in vivo. Herein, we developed two novel ¹¹C-labeled probes, [¹¹C]8 and [¹¹C]15 (also named as [¹¹C]TARP-2105), of which the latter exhibited a reasonable brain uptake as well as specific

SUBMITTER: Yu Q 

PROVIDER: S-EPMC10448436 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature