Banister Samuel D, Manoli Miral, Kassiou Michael
Brain and Mind Research Institute, The University of Sydney, NSW, 2050, Australia; School of Chemistry, The University of Sydney, NSW, 2006, Australia.
J Labelled Comp Radiopharm. 2013 Mar-Apr;56(3-4):215-24. doi: 10.1002/jlcr.3010.
Sigma (σ) receptors are unique mammalian proteins, distributed in the central nervous system and elsewhere, which are increasingly implicated in the pathophysiology of virtually all major central nervous system disorders. The heterogeneous but wide distribution of σ1 in the brain has prompted the development of selective radiotracers for imaging these sites using positron emission tomography (PET). To date, some 50 carbon-11-labelled and fluorine-18-labelled candidate PET radioligands targeting σ receptors have been reported. The historical development of selective σ1 receptor ligands as potential PET imaging agents, as well as the radiochemistry and application of the most recently developed examples, is described herein.
西格玛（σ）受体是独特的哺乳动物蛋白，分布于中枢神经系统及其他部位，几乎与所有主要中枢神经系统疾病的病理生理学都日益相关。σ1在大脑中分布不均但范围广泛，这促使人们开发出选择性放射性示踪剂，用于通过正电子发射断层扫描（PET）对这些部位进行成像。迄今为止，已报道了约50种针对σ受体的碳-11标记和氟-18标记的候选PET放射性配体。本文描述了选择性σ1受体配体作为潜在PET成像剂的历史发展，以及最新开发实例的放射化学和应用。
