Development of Novel ¹¹C-Labeled Selective Orexin-2 Receptor Radioligands for Positron Emission Tomography Imaging.

ABSTRACT: Orexin 2 receptors (OX₂R) represent a vital subtype of orexin receptors intricately involved in the regulation of wakefulness, arousal, and sleep-wake cycles. Despite their importance, there are currently no positron emission tomography (PET) tracers available for imaging the OX₂R in vivo. Herein, we report [¹¹C]1 ([¹¹C]OX₂-2201) and [¹¹C]2 ([¹¹C]OX₂-2202) as novel PET ligands. Both compounds 1 (K _i = 3.6 nM) and 2 (K _i = 2.2 nM) have excellent binding affinity activities toward OX₂R and target selectivity (OX₂/OX₁ > 600 folds). In vitro autoradiography in the rat brain suggested good to excellent

SUBMITTER: Rong J 

PROVIDER: S-EPMC10577698 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature