Selective α₃β₄ Nicotinic Acetylcholine Receptor Ligand as a Potential Tracer for Drug Addiction.

ABSTRACT: α₃β₄ Nicotinic acetylcholine receptor (nAChR) has been recognized as an emerging biomarker for the early detection of drug addiction. Herein, α₃β₄ nAChR ligands were designed and synthesized to improve the binding affinity and selectivity of two lead compounds, (S)-QND8 and (S)-T2, for the development of an α₃β₄ nAChR tracer. The structural modification was achieved by retaining the key features and expanding the molecular structure with a benzyloxy group to increase the lipophilicity for blood-brain barrier penetration and to extend the ligand-receptor interaction. The preserved key features are a fluorine atom for radiotracer development and a p-hydroxyl motif for ligand-rec

SUBMITTER: Kanasuwan A 

PROVIDER: S-EPMC9959096 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature