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

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 c...
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Autor*in:	Lingling Zhang [verfasserIn] Kuan Hu [verfasserIn] Tuo Shao [verfasserIn] Lu Hou [verfasserIn] Shaojuan Zhang [verfasserIn] Weijian Ye [verfasserIn] Lee Josephson [verfasserIn] Jeffrey H. Meyer [verfasserIn] Ming-Rong Zhang [verfasserIn] Neil Vasdev [verfasserIn] Jinghao Wang [verfasserIn] Hao Xu [verfasserIn] Lu Wang [verfasserIn] Steven H. Liang [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2021

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

Übergeordnetes Werk:	In: Acta Pharmaceutica Sinica B - Elsevier, 2013, 11(2021), 2, Seite 373-393
Übergeordnetes Werk:	volume:11 ; year:2021 ; number:2 ; pages:373-393

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.1016/j.apsb.2020.08.006

Katalog-ID:	DOAJ052045951

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spelling	10.1016/j.apsb.2020.08.006 doi (DE-627)DOAJ052045951 (DE-599)DOAJf41bf533ef0c495f89c741de8840c7ea DE-627 ger DE-627 rakwb eng RM1-950 Lingling Zhang verfasserin aut Recent developments on PET radiotracers for TSPO and their applications in neuroimaging 2021 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier 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. TSPO Microglial activation Neuroinflammation Positron emission tomography (PET) CNS disorders Therapeutics. Pharmacology Kuan Hu verfasserin aut Tuo Shao verfasserin aut Lu Hou verfasserin aut Shaojuan Zhang verfasserin aut Weijian Ye verfasserin aut Lee Josephson verfasserin aut Jeffrey H. Meyer verfasserin aut Ming-Rong Zhang verfasserin aut Neil Vasdev verfasserin aut Jinghao Wang verfasserin aut Hao Xu verfasserin aut Lu Wang verfasserin aut Steven H. Liang verfasserin aut In Acta Pharmaceutica Sinica B Elsevier, 2013 11(2021), 2, Seite 373-393 (DE-627)670211095 (DE-600)2631779-5 22113843 nnns volume:11 year:2021 number:2 pages:373-393 https://doi.org/10.1016/j.apsb.2020.08.006 kostenfrei https://doaj.org/article/f41bf533ef0c495f89c741de8840c7ea kostenfrei http://www.sciencedirect.com/science/article/pii/S2211383520306894 kostenfrei https://doaj.org/toc/2211-3835 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 11 2021 2 373-393
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callnumber-first	R - Medicine
author	Lingling Zhang
spellingShingle	Lingling Zhang misc RM1-950 misc TSPO misc Microglial activation misc Neuroinflammation misc Positron emission tomography (PET) misc CNS disorders misc Therapeutics. Pharmacology Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
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topic_title	RM1-950 Recent developments on PET radiotracers for TSPO and their applications in neuroimaging TSPO Microglial activation Neuroinflammation Positron emission tomography (PET) CNS disorders
topic	misc RM1-950 misc TSPO misc Microglial activation misc Neuroinflammation misc Positron emission tomography (PET) misc CNS disorders misc Therapeutics. Pharmacology
topic_unstemmed	misc RM1-950 misc TSPO misc Microglial activation misc Neuroinflammation misc Positron emission tomography (PET) misc CNS disorders misc Therapeutics. Pharmacology
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title	Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
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title_full	Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
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title_sort	recent developments on pet radiotracers for tspo and their applications in neuroimaging
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title_auth	Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
abstract	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.
abstractGer	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.
abstract_unstemmed	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.
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title_short	Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
url	https://doi.org/10.1016/j.apsb.2020.08.006 https://doaj.org/article/f41bf533ef0c495f89c741de8840c7ea http://www.sciencedirect.com/science/article/pii/S2211383520306894 https://doaj.org/toc/2211-3835
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author2	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
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up_date	2024-07-03T23:29:41.553Z
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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. 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Pharmacology</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Kuan Hu</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Tuo Shao</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Lu Hou</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Shaojuan Zhang</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Weijian Ye</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Lee Josephson</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Jeffrey H. 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Recent developments on PET radiotracers for TSPO and their applications in neuroimaging

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