Fluorescent ligands for dopamine D₂/D₃ receptors.

ABSTRACT: Fluorescent ligands are versatile tools for the study of G protein-coupled receptors. Depending on the fluorophore, they can be used for a range of different applications, including fluorescence microscopy and bioluminescence or fluorescence resonance energy transfer (BRET or FRET) assays. Starting from phenylpiperazines and indanylamines, privileged scaffolds for dopamine D₂-like receptors, we developed dansyl-labeled fluorescent ligands that are well accommodated in the binding pockets of D₂ and D₃ receptors. These receptors are the target proteins for the therapy for several neurologic and psychiatric disorders, including Parkinson's disease and schizophrenia. The dansyl-labeled ligands exhibit binding affinities up to 0.44 nM and 0.29 nM at D₂

SUBMITTER: Allikalt A 

PROVIDER: S-EPMC7736868 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature