Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography

Cholinergic receptorsrepresent a promising class of diagnosticand therapeutic targets due to their significant involvement in cognitivedecline associated with neurological disorders and neurodegenerativediseases as well as cardiovascular impairment. Positron emission tomography(PET) is a noninvasive molecular imaging tool that has helped to shedlight on the roles these receptors play in disease development andtheir diverse functions throughout the central nervous system (CNS).In recent years, there has been a notable advancement in the developmentof PET probes targeting cholinergic receptors. The purpose of thisreview is to provide a comprehensive overview of the recent progressin the development of these PET probes for cholinergic receptors witha specific focus on ligand structure, radiochemistry, and pharmacologyas well as in vivo performance and applications in neuroimaging. Thereview covers the structural design, pharmacological properties, radiosynthesisapproaches, and preclinical and clinical evaluations of current state-of-the-artPET probes for cholinergic receptors.