Recent developments on PET radiotracers for TSPO and their applications in neuroimaging

作     者：Lingling Zhang Kuan Hu Tuo Shao Lu Hou Shaojuan Zhang Weijian Ye Lee Josephson Jeffrey H.Meyer Ming-Rong Zhang Neil Vasdev Jinghao Wang Hao Xu Lu Wang Steven H.Liang Lingling Zhang;Kuan Hu;Tuo Shao;Lu Hou;Shaojuan Zhang;Weijian Ye;Lee Josephson;Jeffrey H. Meyer;Ming-Rong Zhang;Neil Vasdev;Jinghao Wang;Hao Xu;Lu Wang;Steven H. Liang

作者机构：Center of Cyclotron and PET RadiopharmaceuticalsDepartment of Nuclear Medicine and PET/CT-MRI CenterThe First Affiliated Hospital of Jinan UniversityGuangzhou 510630China Department of Neurologythe First Affiliated Hospital of Jinan UniversityGuangzhou 510630China Department of Radiopharmaceuticals DevelopmentNational Institute of Radiological SciencesNational Institutes for Quantum and Radiological Science and TechnologyChiba 263-8555Japan Division of Nuclear Medicine and Molecular ImagingMassachusetts General Hospital&Department of RadiologyHarvard Medical SchoolBostonMA 02114USA Azrieli Centre for Neuro-RadiochemistryBrain Health Imaging CentreCentre for Addiction and Mental Health&Department of PsychiatryUniversity of TorontoToronto ON M5T 1R8Canada Department of Pharmacythe First Affiliated Hospital of Jinan UniversityGuangzhou 510630China 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2021年第11卷第2期

页      面：373-393页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：support of K.C.Wong Education Foundation(China) the Project of Innovative Team for the Guangdong Universities(2018KCXTD001,China) financially supported by the National Natural Science Foundation of China(Nos.81701751 and 81871383) Guangdong Basic and Applied Basic Research Foundation(2020A1515011192,China) 

主　　题：TSPO Microglial activation Neuroinflammation Positron emission tomography(PET) CNS disorders 

摘      要：The 18 kDa translocator protein(TSPO),previously known as the peripheral benzodiazepine receptor,is predominately localized to the outer mitochondrial membrane in steroidogenic *** TSPO expression is relatively low under physiological conditions,but is upregulated in response to glial cell *** the primary index of neuroinflammation,TSPO is implicated in the pathogenesis and progression of numerous neuropsychiatric disorders and neurodegenerative diseases,including Alzheimer’s disease(AD),amyotrophic lateral sclerosis(ALS),Parkinson’s disease(PD),multiple sclerosis(MS),major depressive disorder(MDD)and obsessive compulsive disorder(OCD).In this context,numerous TSPO-targeted positron emission tomography(PET)tracers have been *** them,several radioligands have advanced to clinical research *** this review,we will overview the recent development of TSPO PET tracers,focusing on the radioligand design,radioisotope labeling,pharmacokinetics,and PET imaging ***,we will consider current limitations,as well as translational potential for future application of TSPO *** review aims to not only present the challenges in current TSPO PET imaging,but to also provide a new perspective on TSPO targeted PET tracer discovery *** these challenges will facilitate the translation of TSPO in clinical studies of neuroinflammation associated with central nervous system diseases.