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Recent developments on PET radiotracers for TSPO and their applications in neuroimaging 被引量:13
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作者 Lingling Zhang Kuan Hu +11 位作者 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 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2021年第2期373-393,共21页
The 18 kDa translocator protein(TSPO),previously known as the peripheral benzodiazepine receptor,is predominately localized to the outer mitochondrial membrane in steroidogenic cells.Brain TSPO expression is relativel... The 18 kDa translocator protein(TSPO),previously known as the peripheral benzodiazepine receptor,is predominately localized to the outer mitochondrial membrane in steroidogenic cells.Brain TSPO expression is relatively low under physiological conditions,but is upregulated in response to glial cell activation.As 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 developed.Among them,several radioligands have advanced to clinical research studies.In this review,we will overview the recent development of TSPO PET tracers,focusing on the radioligand design,radioisotope labeling,pharmacokinetics,and PET imaging evaluation.Additionally,we will consider current limitations,as well as translational potential for future application of TSPO radiopharmaceuticals.This 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 efforts.Addressing these challenges will facilitate the translation of TSPO in clinical studies of neuroinflammation associated with central nervous system diseases. 展开更多
关键词 TSPO Microglial activation NEUROINFLAMMATION Positron emission tomography(PET) CNS disorders
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