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Relevant bibliographies by topics / Second-generation TSPO ligand

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Academic literature on the topic 'Second-generation TSPO ligand'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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Journal articles on the topic "Second-generation TSPO ligand"

1

Sokias, Renee, Eryn L. Werry, Sook W. Chua, et al. "Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination." Med. Chem. Commun. 8 (November 15, 2016): 202–10. https://doi.org/10.1039/C6MD00523C.

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The 18 kDa translocator protein (TSPO) is a target for development of diagnostic imaging agents for glioblastoma and neuroinflammation. Clinical translation of TSPO imaging agents has been hindered by the presence of a polymorphism, rs6971, which causes a non-conservative substitution of alanine for threonine at amino acid residue 147 (TSPO A147T). Disclosed brain-permeant second-generation TSPO ligands bind TSPO A147T with reduced affinity compared to the wild type protein (TSPO WT). Efforts to develop a TSPO ligand that binds TSPO WT and TSPO A147T with similarly high affinity have been hamp

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2

Dickens, Alex M., Susanne Vainio, Päivi Marjamäki, et al. "Detection of Microglial Activation in an Acute Model of Neuroinflammation Using PET and Radiotracers 11C-(R)-PK11195 and 18F-GE-180." J Nucl Med. 55, no. 3 (2014): 466–72. https://doi.org/10.2967/jnumed.113.125625.

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It remains unclear how different translocator protein (TSPO) ligands reflect the spatial extent of astrocyte or microglial activation in various neuroinflammatory conditions. Here, we use a reproducible lipopolysaccharide (LPS)-induced model of acute central nervous system inflammation to compare the binding performance of a new TSPO ligand (18)F-GE-180 with (11)C-(R)-PK11195. Using immunohistochemistry, we also explore the ability of the TSPO ligands to detect activated microglial cells and astrocytes. METHODS: Lewis rats (n = 30) were microinjected with LPS (1 or 10 μg) or saline (1 μL

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3

Lee, Sang Hee, Nunzio Denora, Valentino Laquintana, et al. "Radiosynthesis and characterization of [18F]BS224: a next-generation TSPO PET ligand insensitive to the rs6971 polymorphism." European Journal of Nuclear Medicine and Molecular Imaging 49, no. 1 (2021): 110–24. http://dx.doi.org/10.1007/s00259-021-05617-4.

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Abstract Purpose Translocator protein 18-kDa (TSPO) positron emission tomography (PET) is a valuable tool to detect neuroinflammed areas in a broad spectrum of neurodegenerative diseases. However, the clinical application of second-generation TSPO ligands as biomarkers is limited because of the presence of human rs6971 polymorphism that affects their binding. Here, we describe the ability of a new TSPO ligand, [18F]BS224, to identify abnormal TSPO expression in neuroinflammation independent of the rs6971 polymorphism. Methods An in vitro competitive inhibition assay of BS224 was conducted with

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4

Kobayashi, Masato, Teresa Jiang, Sanjay Telu, et al. "11C-DPA-713 has much greater specific binding to translocator protein 18 kDa (TSPO) in human brain than 11C-(R)-PK11195." Journal of Cerebral Blood Flow & Metabolism 38, no. 3 (2017): 393–403. http://dx.doi.org/10.1177/0271678x17699223.

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Positron emission tomography (PET) radioligands for translocator protein 18 kDa (TSPO) are widely used to measure neuroinflammation, but controversy exists whether second-generation radioligands are superior to the prototypical agent 11C-( R)-PK11195 in human imaging. This study sought to quantitatively measure the “signal to background” ratio (assessed as binding potential ( BPND)) of 11C-( R)-PK11195 compared to one of the most promising second-generation radioligands, 11C-DPA-713. Healthy subjects had dynamic PET scans and arterial blood measurements of radioligand after injection of either

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5

Donat, Cornelius K., Khaled Gaber, Jürgen Meixensberger, et al. "Changes in Binding of [123I]CLINDE, a High-Affinity Translocator Protein 18 kDa (TSPO) Selective Radioligand in a Rat Model of Traumatic Brain Injury." Neuromolecular Medecine 18, no. 2 (2016): 158–69. https://doi.org/10.1007/s12017-016-8385-y.

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After traumatic brain injury (TBI), secondary injuries develop, including neuroinflammatory processes that contribute to long-lasting impairments. These secondary injuries represent potential targets for treatment and diagnostics. The translocator protein 18 kDa (TSPO) is expressed in activated microglia cells and upregulated in response to brain injury and therefore a potential biomarker of the neuroinflammatory processes. Second-generation radioligands of TSPO, such as [<sup>123</sup>I]CLINDE, have a higher signal-to-noise ratio as the prototype ligand PK11195. [<sup>123</sup>I]CLINDE h

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Molotkov, Andrei, Angeliki Mela, Peter D. Canoll, and Akiva Mintz. "CBMT-03. EVALUATION OF PET TRACERS TO DIFFERENTIATE IDH1 MUTANT GBM." Neuro-Oncology 21, Supplement_6 (2019): vi33. http://dx.doi.org/10.1093/neuonc/noz175.125.

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Abstract OBJECTIVE PET/CT offers the unique potential to noninvasively evaluate biomarker expression and aberrant metabolism. 18F-FDG has driven PET/CT to the forefront of cancer imaging, as altered glucose metabolism is a hallmark of oncogenesis. However, 18F-FDG is suboptimal for GBM due to high physiologic uptake in normal brain. The development of alternative tracers has reignited the field of PET/CT in GBM and offers hope for diagnosis and molecular staging in GBM. We hypothesize that fundamental differences in metabolism and oncogene expression present in IDH1 mutatant gliomas can be sho

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Airas, Laura, Alex M. Dickens, Petri Elo, et al. "In vivo PET imaging demonstrates diminished microglial activation after fingolimod treatment in an animal model of multiple sclerosis." J Nucl Med. 56, no. 2 (2015): 305–10. https://doi.org/10.2967/jnumed.114.149955.

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There is a great need for the monitoring of microglial activation surrounding multiple sclerosis lesions because the activation of microglia is thought to drive widespread neuronal damage. Recently, second-generation PET radioligands that can reveal the extent of microglial activation by quantifying the increased expression of the 18-kDa translocator protein have been developed. Here, we investigate whether PET imaging can be used to demonstrate the reduction in microglial activation surrounding a chronic focal multiple sclerosis (MS)-like lesion after treatment with fingolimod, an established

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8

Guo, Qi, David R. Owen, Eugenii A. Rabiner, Federico E. Turkheimer, and Roger N. Gunn. "A Graphical Method to Compare the in vivo Binding Potential of PET Radioligands in the Absence of a Reference Region: Application to [11C]PBR28 and [18F]PBR111 for TSPO Imaging." Journal of Cerebral Blood Flow & Metabolism 34, no. 7 (2014): 1162–68. http://dx.doi.org/10.1038/jcbfm.2014.65.

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Positron emission tomography (PET) radioligands for a reversible central nervous system (CNS) demand a high specific to nonspecific signal characterized by the binding potential ( BPND). The quantification of BPND requires the determination of the nondisplaceable binding usually derived from a reference region devoid of the target of interest. However, for many CNS targets, there is no valid reference region available. In such cases, the total volume of distribution ( VT) is often used as the outcome measure, which includes both the specific and nonspecific binding signals. Here we present a g

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Chang, Chi-Wei, Chuang-Hsin Chiu, Ming-Hsien Lin, et al. "GMP-compliant fully automated radiosynthesis of [18F]FEPPA for PET/MRI imaging of regional brain TSPO expression." EJNMMI Research 11, no. 1 (2021). http://dx.doi.org/10.1186/s13550-021-00768-9.

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Abstract Background Expression of translocator protein (TSPO) on the outer mitochondrial membrane of activated microglia is strongly associated with neuroinflammation. The second-generation PET ligand [18F]FEPPA specifically binds TSPO to enable in vivo visualization and quantification of neuroinflammation. We optimized a fully automated radiosynthesis method and evaluated the utility of [18F]FEPPA, the second-generation PET ligand specifically binds TSPO, in a mouse model of systemic LPS challenge to detect TSPO-associated signals of central and peripheral inflammation. In vivo dynamic PET/MR

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Helo, Yusuf, Graham E. Searle, Federica Borghese, Sonya Abraham, and Azeem Saleem. "Specificity of translocator protein-targeted positron emission tomography in inflammatory joint disease." EJNMMI Research 10, no. 1 (2020). http://dx.doi.org/10.1186/s13550-020-00736-9.

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Abstract Objective Expression of the translocator protein (TSPO) on inflammatory cells has facilitated imaging of synovitis with TSPO-targeted positron emission tomography (PET). We aimed to quantitatively assess the specificity of the second-generation TSPO PET radioligand, [11C]PBR28, and to generate simplified PET protocols in patients with inflammatory joint disease (IJD) in this pilot study. Methods Three IJD patients (two rheumatoid arthritis and one osteoarthritis) with knee involvement underwent dynamic [11C]PBR28-PET scans before and after administration of 90 mg of oral emapunil (XBD

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Dissertations / Theses on the topic "Second-generation TSPO ligand"

1

Sridharan, Sujata. "Quantitative analysis of positron emission tomography (PET) with the second generation translocator protein (TSPO) ligand [18F]GE-180." Thesis, University of Manchester, 2016. https://www.research.manchester.ac.uk/portal/en/theses/quantitative-analysis-of-positron-emission-tomography-pet-with-the-second-generation-translocator-protein-tspo-ligand-18fge180(01bdc97f-90f7-4db3-8268-f65e013640ab).html.

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Background: The 18 kDa translocator protein (TSPO), expressed at a low level in the healthy human central nervous system (CNS), is upregulated in inflammatory brain diseases by activated microglia and other immune cells. Using positron emission tomography (PET) radioligands targeting TSPO, it is possible to localise this signal and map the course of microglial activation and its effects on disease progression. Here, a newly developed second generation TSPO PET ligand, [18F]GE-180, was evaluated in different models of preclinical and clinical neuroinflammatory disease. Methods: A preclinical mo

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