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Academic literature on the topic 'DPA-713'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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Journal articles on the topic "DPA-713"

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Ordonez, Alvaro A., Supriya Pokkali, Vincent P. DeMarco, et al. "Radioiodinated DPA-713 Imaging Correlates with Bactericidal Activity of Tuberculosis Treatments in Mice." Antimicrobial Agents and Chemotherapy 59, no. 1 (2014): 642–49. http://dx.doi.org/10.1128/aac.04180-14.

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ABSTRACTCurrent tools for monitoring response to tuberculosis treatments have several limitations. Noninvasive biomarkers could accelerate tuberculosis drug development and clinical studies, but to date little progress has been made in developing new imaging technologies for this application. In this study, we developed pulmonary single-photon emission computed tomography (SPECT) using radioiodinated DPA-713 to serially monitor the activity of tuberculosis treatments in live mice, which develop necrotic granulomas and cavitary lesions. C3HeB/FeJ mice were aerosol infected withMycobacterium tub

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2

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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Cerutti, Erika, Annelaure Damont, Frédéric Dollé, Simona Baroni, and Silvio Aime. "Synthesis and characterization of an MRI Gd-based probe designed to target the translocator protein." Magnetic Resonance in Chemistry 51, no. 2 (2013): 116–22. https://doi.org/10.1002/mrc.3919.

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DPA-713 is the lead compound of a recently reported pyrazolo[1,5-a]pyrimidineacetamide series, targeting the translocator protein (TSPO 18 kDa), and as such, this structure, as well as closely related derivatives, have been already successfully used as positron emission tomography radioligands. On the basis of the pharmacological core of this ligands series, a new magnetic resonance imaging probe, coded DPA-C(6)-(Gd)DOTAMA was designed and successfully synthesized in six steps and 13% overall yield from DPA-713. The Gd-DOTA monoamide cage (DOTA = 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraac

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Werry, Eryn L., Victoria A. King, Melissa L. Barron, Samuel D. Banister, Renee Sokias, and Michael Kassiou. "Derivatives of the pyrazolo[1,5-a]pyrimidine acetamide DPA-713 as translocator protein (TSPO) ligands and pro-apoptotic agents in human glioblastoma." European Journal of Pharmaceutical Sciences 96 (September 19, 2016): 186–92. https://doi.org/10.1016/j.ejps.2016.09.026.

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The 18kDa translocator protein (TSPO) is a target for novel glioblastoma therapies due to its upregulation in this cancer and relatively low levels of expression in the healthy cortex. The pyrazolo[1,5-a]pyrimidine acetamides, exemplified by DPA-713 and DPA-714, are a class of high affinity TSPO ligands with selectivity over the central benzodiazepine receptor. In this study we have explored the potential anti-glioblastoma activity of a library of DPA-713 and DPA-714 analogues, and investigated the effect of amending the alkyl ether chain on TSPO affinity and functional potential. All ligands

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5

Yaqub, Maqsood, Nicki J. F. Verweij, Simone Pieplenbosch, Ronald Boellaard, Adriaan A. Lammertsma, and Conny J. van der Laken. "Quantitative Assessment of Arthritis Activity in Rheumatoid Arthritis Patients Using [11C]DPA-713 Positron Emission Tomography." International Journal of Molecular Sciences 21, no. 9 (2020): 3137. http://dx.doi.org/10.3390/ijms21093137.

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Treatment for rheumatoid arthritis (RA) should be started as early as possible to prevent destruction of bone and cartilage in affected joints. A new diagnostic tool for both early diagnosis and therapy monitoring would be valuable to reduce permanent joint damage. Positron emission tomography (PET) imaging of macrophages is a previously demonstrated non-invasive means to visualize (sub)clinical arthritis in RA patients. We developed a kinetic model to quantify uptake of the macrophage tracer [11C]DPA-713 (N,N-diethyl-2-[2-(4-methoxyphenyl)-5,7-dimethylpyrazolo [1,5-a]pyrimidin-3-yl]acetamide)

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6

Rubin, Leah H., Yong Du, Shannon Eileen Sweeney, et al. "Imaging Brain Injury in Former National Football League Players." JAMA Network Open 6, no. 10 (2023): e2340580. http://dx.doi.org/10.1001/jamanetworkopen.2023.40580.

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ImportancePilot studies that involved early imaging of the 18 kDa translocator protein (TSPO) using positron emission tomography (PET) indicated high levels of TSPO in the brains of active or former National Football League (NFL) players. If validated further in larger studies, those findings may have implications for athletes involved in collision sport.ObjectiveTo test for higher TSPO that marks brain injury and repair in a relatively large, unique cohort of former NFL players compared with former elite, noncollision sport athletes.Design, Setting, and ParticipantsThis cross-sectional study

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7

Banister, Samuel D., Corinne Beinat, Shane M. Wilkinson, et al. "Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)." Eur J Med Chem. 93 (February 7, 2015): 392–400. https://doi.org/10.1016/j.ejmech.2015.02.004.

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Sixteen new phenyl alkyl ether derivatives (12, 14-28) of the 5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-ylacetamide (DPA) class were synthesized and evaluated in a competition binding assay against [3H]PK11195 using 18 kDa translocator protein (TSPO) derived from rat kidney mitochondrial fractions. All analogues showed superior binding affinities for TSPO compared to DPA-713 (5) and DPA-714 (6). Picomolar affinities were observed for this class of TSPO ligands in this assay for the first time, with phenethyl ether 28 showing the greatest affinity (Ki = 0.13 nM). Additiona

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Wilson, Thomas C., Greg McSweeney, Sean Preshlock, et al. "Radiosynthesis of SPECT tracers via a copper mediated 123I iodination of (hetero)aryl boron reagents." Chemical Communications 52, no. 90 (2016): 13277–80. http://dx.doi.org/10.1039/c6cc07417k.

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The Cu-mediated [<sup>123</sup>I]iodination of aryl boronic pinacol esters and acids exhibits broad scope and is successfully applied to the labelling of four radiotracers, [<sup>123</sup>I]DPA-713, [<sup>123</sup>I]IMPY, [<sup>123</sup>I]MIBG and [<sup>123</sup>I]IPEB.

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Foss, Catherine A., Jamie S. Harper, Haofan Wang, Martin G. Pomper, and Sanjay K. Jain. "Noninvasive Molecular Imaging of Tuberculosis-Associated Inflammation With Radioiodinated DPA-713." Journal of Infectious Diseases 208, no. 12 (2013): 2067–74. http://dx.doi.org/10.1093/infdis/jit331.

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10

Damont, Annelaure, Sébastien Garcia-Argote, David-Alexandre Buisson, Bernard Rousseau, and Frédéric Dollé. "Efficient tritiation of the translocator protein (18kDa) selective ligand DPA-714." J Labelled Comp Radiopharm. 58, no. 1 (2015): 1–6. https://doi.org/10.1002/jlcr.3252.

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DPA-714 (N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide) is a recently discovered fluorinated ligand of the translocator protein 18 kDa (TSPO). Labelled with the short-lived positron emitter fluorine-18, this structure is today the radioligand of reference for in vivo imaging of microglia activation and neuroinflammatory processes with positron emission tomography. In the present work, an isotopically tritium-labelled version was developed ([3H]DPA-714), in order to access high resolution in vitro and ex vivo microscopic auto

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Conference papers on the topic "DPA-713"

1

Akerele, Mercy I., Sara A. Zein, Sneha Pandya, et al. "Feasibility of Population-Based Input Function for Kinetic Analysis of [11C]-DPA-713." In 2020 IEEE Nuclear Science Symposium and Medical Imaging Conference (NSS/MIC). IEEE, 2020. http://dx.doi.org/10.1109/nss/mic42677.2020.9508079.

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