Design, Synthesis, and Evaluation of a New Fluorescent Ligand for the M₂ Muscarinic Acetylcholine Receptor.

ABSTRACT: The M₂ muscarinic acetylcholine receptor (M₂R) is a G protein-coupled receptor involved in regulating cardiovascular functions and mediation of central muscarinic effects, such as movement, temperature control, and antinociceptive responses. Molecular probes targeting this receptor are therefore important in exploring its pathophysiological role at a molecular level. Herein, we report the design, synthesis, and evaluation of a new fluorescent probe for M₂R based on an anthranilamide ligand. In radioligand binding experiments, the presented Oregon Green 488-labeled conjugate (33) exhibited high M₂R affinity (K _i = 2.4 nM), a moderate preference for the M₂R over the M₄ receptor, and excellent to pronou

SUBMITTER: Szabo R 

PROVIDER: S-EPMC11995211 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature