Mach Robert H, Luedtke Robert R
Department of Radiology, Perelman School Medicine, University of Pennsylvania, Philadelphia, PA, USA.
Department of Pharmacology and Neuroscience, University of North Texas Health Science Center-Fort Worth, Fort Worth, TX, USA.
J Labelled Comp Radiopharm. 2018 Mar;61(3):291-298. doi: 10.1002/jlcr.3558. Epub 2017 Sep 26.
The dopamine D2-like receptors (ie, D2/3 receptors) have been the most extensively studied CNS receptor with Positron Emission Tomography (PET). The 3 different radiotracers that have been used in these studies are [ C]raclopride, [ F]fallypride, and [ C]PHNO. Because these radiotracers have a high affinity for both dopamine D2 and D3 receptors, the density of dopamine receptors in the CNS is reported as the D2/3 binding potential, which reflects a measure of the density of both receptor subtypes. Although the development of D2- and D3-selective PET radiotracers has been an active area of research for many years, this by and large presents an unmet need in the area of translational PET imaging studies. This article discusses some of the challenges that have inhibited progress in this area of research and the current status of the development of subtype selective radiotracers for imaging D3 and D2 dopamine receptors with PET.
多巴胺 D2 样受体（即 D2/3 受体）是利用正电子发射断层扫描（PET）研究最为广泛的中枢神经系统受体。这些研究中使用的 3 种不同放射性示踪剂分别是[碳]雷氯必利、[氟]法氯必利和[碳]PHNO。由于这些放射性示踪剂对多巴胺 D2 和 D3 受体均具有高亲和力，中枢神经系统中多巴胺受体的密度以 D2/3 结合潜能来报告，它反映了两种受体亚型密度的一种度量。尽管多年来 D2 和 D3 选择性 PET 放射性示踪剂的开发一直是一个活跃的研究领域，但总体而言，这在转化型 PET 成像研究领域仍是一个未满足的需求。本文讨论了一些阻碍该研究领域进展的挑战以及用于 PET 成像 D3 和 D2 多巴胺受体的亚型选择性放射性示踪剂的开发现状。
