Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography

• Type of Material: Article
• Authors: Jing-Jing Zhang, Nanjing Forestry University; Hualong Fu, Harvard Medical School; Ruofan Lin, Nanjing Forestry University; Jingyin Zhou, Beijing Normal University; Ahmed Haider, Harvard Medical School; Weiwei Fang, Nanjing Forestry University; Nehal H. Elghazawy, German University in Cairo; Jian Rong, Emory University; Jiahui Chen, Emory University; yinlong Li, Emory University; Chongzhao Ran, Harvard Medical School; Thomas L. Collier, Emory University; Zhen Chen, Nanjing Forestry University; Steven Liang, Emory University
• Language: English
• Date: 2023-08-24
• Publisher: American Chemical Society Publications
• Publication Version: Final Published Version
• Copyright Statement: © 2023 The Authors. Published by American Chemical Society
• License: Creative Commons Attribution 4.0 International
• Final Published Version (URL): https://doi.org/10.1021%2Facs.jmedchem.3c00573
• Title of Journal or Parent Work: Journal of Medicinal Chemistry
• Volume: 66
• Issue: 16
• Start Page: 10889
• End Page: 10916
• Grant/Funding Information: A.H. was supported by the Swiss National Science Foundation (SNSF). S.H.L. gratefully acknowledges the support provided, in part, by the Emory Radiology Chair Fund and Emory School of Medicine Endowed Directorship.
• Keywords: cognitive decline; therapeutic; diagnostic; neurological disorders; Cholinergic receptors; neurodegenerative diseases; Positron emission tomography (PET); cardiovascular impairment; noninvasive molecular imaging technique
• Research Categories: Psychology, Cognitive; Biology, Neuroscience

Abstract

Cholinergic receptors represent a promising class of diagnostic and therapeutic targets due to their significant involvement in cognitive decline associated with neurological disorders and neurodegenerative diseases as well as cardiovascular impairment. Positron emission tomography (PET) is a noninvasive molecular imaging tool that has helped to shed light on the roles these receptors play in disease development and their diverse functions throughout the central nervous system (CNS). In recent years, there has been a notable advancement in the development of PET probes targeting cholinergic receptors. The purpose of this review is to provide a comprehensive overview of the recent progress in the development of these PET probes for cholinergic receptors with a specific focus on ligand structure, radiochemistry, and pharmacology as well as in vivo performance and applications in neuroimaging. The review covers the structural design, pharmacological properties, radiosynthesis approaches, and preclinical and clinical evaluations of current state-of-the-art PET probes for cholinergic receptors.