Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Veterans Administration Ann Arbor Healthcare System, Ann Arbor, Michigan 48105, United States.
ACS Chem Neurosci. 2021 May 5;12(9):1472-1479. doi: 10.1021/acschemneuro.1c00245. Epub 2021 Apr 23.
Since the earliest days of nuclear medicine, there has been interest in using PET and SPECT imaging to interrogate and quantify the cholinergic system. In this Viewpoint we highlight key milestones in the development of cholinergic imaging agents, including identification of radiopharmaceuticals targeting the receptors, transporters, and enzymes of the cholinergic synapse, as well as fundamental developments in the radiopharmaceutical sciences (e.g., cyclotron targetry, radiochemistry) that have enabled translation of the most promising agents into clinical use. We also provide an overview of the current state-of-the-art in cholinergic PET imaging, with an emphasis on radiotracers that are in human studies at PET centers around the world.
自核医学的早期以来,人们一直有兴趣使用 PET 和 SPECT 成像来探测和定量胆碱能系统。在本观点中,我们重点介绍了胆碱能成像剂发展中的关键里程碑,包括鉴定针对胆碱能突触的受体、转运体和酶的放射性药物,以及放射性药物科学(例如回旋加速器靶标、放射化学)的基本发展,这些发展使最有前途的药物得以转化为临床应用。我们还概述了当前胆碱能正电子发射断层扫描成像的最新技术,重点介绍了世界各地 PET 中心的人类研究中使用的放射性示踪剂。