Evaluation of the PBR/TSPO Radioligand [ 18 F]DPA-714 in a Rat Model of Focal Cerebral Ischemia

Martín, Abraham; Boisgard, Raphaël; Thézé, Benoit; Van Camp, Nadja; Kuhnast, Bertrand; Damont, Annelaure; Kassiou, Michael; Dollé, Frédéric; Tavitian, Bertrand

doi:10.1038/jcbfm.2009.205

Cited by 212Neuroinflammation and Neurodegeneration MechanismsPharmacological Receptor Mechanisms and EffectsMedical Imaging Techniques and Applications

Evaluation of the PBR/TSPO Radioligand [ 18 F]DPA-714 in a Rat Model of Focal Cerebral Ischemia

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Martín, Abraham, Boisgard, Raphaël, Thézé, Benoit, Van Camp, Nadja, Kuhnast, Bertrand, Damont, Annelaure, Kassiou, Michael, Dollé, Frédéric +1 more·2010·Journal of Cerebral Blood Flow & Metabolism

DOI 10.1038/jcbfm.2009.205PMC PMC2949091

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Abstract

Focal cerebral ischemia leads to an inflammatory reaction involving an overexpression of the peripheral benzodiazepine receptor (PBR)/18-kDa translocator protein (TSPO) in the cerebral monocytic lineage (microglia and monocyte) and in astrocytes. Imaging of PBR/TSPO by positron emission tomography (PET) using radiolabeled ligands can document inflammatory processes induced by cerebral ischemia. We performed in vivo PET imaging with [(18)F]DPA-714 to determine the time course of PBR/TSPO expression over several days after induction of cerebral ischemia in rats. In vivo PET imaging showed significant increase in DPA (N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide) uptake on the injured side compared with that in the contralateral area on days 7, 11, 15, and 21 after ischemia; the maximal binding value was reached 11 days after ischemia. In vitro autoradiography confirmed these in vivo results. In vivo and in vitro [(18)F]DPA-714 binding was displaced from the lesion by PK11195 and DPA-714. Immunohistochemistry showed increased PBR/TSPO expression, peaking at day 11 in cells expressing microglia/macrophage antigens in the ischemic area. At later times, a centripetal migration of astrocytes toward the lesion was observed, promoting the formation of an astrocytic scar. These results show that [(18)F]DPA-714 provides accurate quantitative information of the time course of PBR/TSPO expression in experimental stroke.

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TSPO expression was found in microglia in active and chronic active lesions.
“Similar to previous studies, TSPO expression was found in microglia in active and chronic active lesions (Cosenza-Nashat et al., 2009; Martin et al., 2010; Lavisse et al., 2012a; Loth et al., 2016; Kaunzner et al., 2019).”
From A quantitative neuropathological assessment of translocator protein expression in multiple sclerosis (2019) · cites this paper as Martin et al., 2010
The Results (page not provided) show TSPO-positive microglia/macrophages in rat ischemic lesions, including at 30 days after ischemia. The paper does not classify those lesions as “active” or “chronic active,” so it supports the cellular finding but not the claimed lesion categories. (LLM, conf=0.87)
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Gulyás, B. Z., Tóth, M., Schain, M., Airaksinen, A. J., Vas, Á., Kostulas, K., Lindström, P., Hillert, J. A., & Halldin, C. (2012) · Journal of the Neurological Sciences · doi:10.1016/j.jns.2012.06.026 · Cited by 100 · see citing works
The translocator protein ligand [18F]DPA-714 images glioma and activated microglia in vivo
Winkeler, A., Boisgard, R., Awde, A. R., Dubois, A., Thezé, B., Zheng, J., Ciobanu, L., Dollé, F., Viel, T., Jacobs, A. H., et al. (2012) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-011-2041-4 · Cited by 95 · see citing works
“on a cryostat and were treated as reported previously [32].”
MethodResultInfluentialSelf-citation
Age and disease related changes in the translocator protein (TSPO) system in the human brain: Positron emission tomography measurements with [11C]vinpocetine
Gulyás, B., Vas, Á., Tóth, M., Takano, A., Varrone, A., Cselényi, Z., Schain, M., Mattsson, P., & Halldin, C. (2011) · NeuroImage · doi:10.1016/j.neuroimage.2011.02.020 · Cited by 94 · see citing works
“…[11C]DAA1106, [18F]FEDAA1106, [11C]DPA713, and [18F]DPA714 (Boutin et al., 2007; Doorduin et al., 2010; Endres et al., 2009; Fujimura et al., 2006; Higuchi, 2009; James et al., 2008; Kassiou et al., 2005; Martin et al., 2010; Okello et al., 2009a,b; Fujimura et al., 2010; Takano et al., 2010).”
[18F]DPA-714: Direct Comparison with [11C]PK11195 in a Model of Cerebral Ischemia in Rats
Boutin, H., Prenant, C., Maroy, R., Galea, J. P., Greenhalgh, A. D., Smigova, A., Cawthorne, C., Julyan, P. J., Wilkinson, S. M., Banister, S. D., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0056441 · Cited by 93 · see citing works
“[25]).”
MethodResultInfluentialSelf-citation
Neurobiology and Therapeutic Potential of Cyclooxygenase-2 (COX-2) Inhibitors for Inflammation in Neuropsychiatric Disorders
Sethi, R., Gómez‐Coronado, N., Walker, A. J., Robertson, O. D., Agustini, B., Berk, M., & Dodd, S. (2019) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2019.00605 · Cited by 88 · see citing works
Imaging neuroinflammation in Alzheimer's disease and other dementias: Recent advances and future directions
Varley, J. A., Brooks, D. J., & Edison, P. (2014) · Alzheimer s & Dementia · doi:10.1016/j.jalz.2014.08.105 · Cited by 81 · see citing works
Brain inflammation in a chronic epilepsy model: Evolving pattern of the translocator protein during epileptogenesis
Amhaoul, H., Hamaide, J., Bertoglio, D., Reichel, S. N., Verhaeghe, J. A. J., Geerts, E., Dam, D. V., Deyn, P. P. D., Kumar‐Singh, S., Katsifis, A. G., et al. (2015) · Neurobiology of Disease · doi:10.1016/j.nbd.2015.09.004 · Cited by 76 · see citing works
Blocking Lymphocyte Trafficking with FTY720 Prevents Inflammation-Sensitized Hypoxic–Ischemic Brain Injury in Newborns
Yang, D., Sun, Y., Bhaumik, S. K., Li, Y., Baumann, J. M., Lin, X., Zhang, Y., Lin, S.-H., Dunn, R. S., Liu, C., et al. (2014) · Journal of Neuroscience · doi:10.1523/jneurosci.2582-14.2014 · Cited by 76 · see citing works
“In addition, the FTY720 treatment markedly reduced the expression of MCP1 protein and TSPO, which are both indicators of neuroinflammation and microglial activation (Martín et al., 2010; Yang et al., 2013a) at 18 –24 h after LPS/HI injury (Fig.”
Background
Cholesterol metabolic reprogramming mediates microglia-induced chronic neuroinflammation and hinders neurorestoration following stroke
Zhao, Q., Li, J., Feng, J., Wang, X., Liu, Y., Wang, F., Liu, L., Jin, B., Lin, M. S., Wang, Y., et al. (2025) · Nature Metabolism · doi:10.1038/s42255-025-01379-7 · Cited by 84 · see citing works
“…(PLM), a gold standard method for detecting birefringent crystalline structures 22–25 , we observed a significant increase in cholesterol crystals within the lesion area during the chronic stroke phase (days 14, 30 and 90) compared to sham controls and earlier time points (days 3 and 7) (Fig.”
PET imaging of neuroinflammation in a rat traumatic brain injury model with radiolabeled TSPO ligand DPA-714
Wang, Y., Yue, X., Kiesewetter, D. O., Niu, G., Teng, G., & Chen, X. S. (2014) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-014-2727-5 · Cited by 77 · see citing works
“Therefore, [(18)F]DPA-714 has been used for PET imaging of neuroinflammation in different models [9, 17, 21].”
BackgroundMethod
TSPO imaging in animal models of brain diseases
Camp, N. V., Lavisse, S., Roost, P., Gubinelli, F., Hillmer, A. T., & Boutin, H. (2021) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-021-05379-z · Cited by 71 · see citing works
“increase in uptake from day 3 post-MCAO was reported, peaking at day 7 and remaining elevated up to day 14 when compared to baseline [76], in line with previous reports [65].”
BackgroundResult
Multimodal Imaging Reveals Temporal and Spatial Microglia and Matrix Metalloproteinase Activity after Experimental Stroke
Zinnhardt, B., Viel, T., Wachsmuth, L., Vrachimis, A., Wagner, S., Breyholz, H., Faust, A., Hermann, S., Kopka, K., Faber, C., et al. (2015) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.2015.149 · Cited by 70 · see citing works
Self-citation
Combined [18F]DPA-714 micro-positron emission tomography and autoradiography imaging of microglia activation after closed head injury in mice
Israel, I., Ohsiek, A., Al‐Momani, E., Albert-Weißenberger, C., Stetter, C., Mencl, S., Buck, A. K., Kleinschnitz, C., Samnick, S., & Sirén, A. (2016) · Journal of Neuroinflammation · doi:10.1186/s12974-016-0604-9 · Cited by 70 · see citing works
Imaging of Perfusion, Angiogenesis, and Tissue Elasticity after Stroke
Martín, A., Macé, É., Boisgard, R., Montaldo, G., Thezé, B., Tanter, M., & Tavitian, B. (2012) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.2012.49 · Cited by 68 · see citing works
Self-citation
Reduced PBR/TSPO Expression After Minocycline Treatment in a Rat Model of Focal Cerebral Ischemia: A PET Study Using [18F]DPA-714
Martín, A., Boisgard, R., Kassiou, M., Dollé, F., & Tavitian, B. (2010) · Molecular Imaging and Biology · doi:10.1007/s11307-010-0324-y · Cited by 68 · see citing works
“Recent immunohistochemistry studies also showed a steady increase of PBR/TSPO expression in microglia/macrophages, with a maximum at 11 days after transient MCA occlusion, followed by a trend to return to normal values of activated microglia at 30 days [12].”
BackgroundMethodResultInfluentialSelf-citation
In vivo imaging and characterization of [18F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET
Vicidomini, C., Panico, M., Greco, A., Gargiulo, S., Coda, A. R. D., Zannetti, A., Gramanzini, M., Roviello, G. N., Quarantelli, M., Alfano, B., et al. (2014) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2014.11.009 · Cited by 66 · see citing works
“While this radiotracer has been characterized ex vivo and in vivowithmicro-PET in experimental models of neuroinflammation [22–25], only limited data are available on [F]DPA-714 binding in peripheral tissues.”
BackgroundMethodSelf-citation
Serial Quantitative TSPO-Targeted PET Reveals Peak Microglial Activation up to 2 Weeks After an Epileptogenic Brain Insult
Brackhan, M., Bascuñana, P., Postema, J. M., Roß, T. L., Bengel, F. M., Bankstahl, M., & Bankstahl, J. P. (2016) · Journal of Nuclear Medicine · doi:10.2967/jnumed.116.172494 · Cited by 64 · see citing works
“Activated microglia and astroglia were both found to express TSPO in a rat model of stroke; however, the PET-derived time profile of in vivo TSPO expression corresponded to microglial and not astroglial activation (34).”
Background
Quantitative Preclinical Imaging of TSPO Expression in Glioma Using N,N-Diethyl-2-(2-(4-(2-18F-Fluoroethoxy)Phenyl)-5,7-Dimethylpyrazolo[1,5-a]Pyrimidin-3-yl)Acetamide
Tang, D., Hight, M. R., McKinley, E. T., Fu, A., Buck, J. R., Smith, R. A., Tantawy, M. N., Peterson, T. E., Colvin, D. C., Ansari, M. S., et al. (2012) · Journal of Nuclear Medicine · doi:10.2967/jnumed.111.095653 · Cited by 63 · see citing works
18F-FEAC and18F-FEDAC: PET of the Monkey Brain and Imaging of Translocator Protein (18 kDa) in the Infarcted Rat Brain
Yui, J., Maeda, J., Kumata, K., Kawamura, K., Yanamoto, K., Hatori, A., Yamasaki, T., Nengaki, N., Higuchi, M., & Zhang, M. (2010) · Journal of Nuclear Medicine · doi:10.2967/jnumed.109.072223 · Cited by 62 · see citing works
“Of these ligands, 11C-labeled N,N-diethyl2-[2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]acetamide (DPA-713) and 18F-labeled N, N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide (DPA-714) are promising PET ligands with potent binding affinity and suitable ki…”
BackgroundMethodInfluential
Applications of positron emission tomography in animal models of neurological and neuropsychiatric disorders
Virdee, K., Cumming, P. D., Caprioli, D., Jupp, B., Rominger, A., Aigbirhio, F. I., Fryer, T. D., Riss, P. J., & Dalley, J. W. (2012) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2012.01.009 · Cited by 60 · see citing works
Intranasal delivery of cell-penetrating anti-NF-κB peptides (Tat-NBD) alleviates infection-sensitized hypoxic–ischemic brain injury
Yang, D., Sun, Y., Lin, X., Baumann, J. M., Dunn, R. S., Lindquist, D. M., & Kuan, C.-Y. (2013) · Experimental Neurology · doi:10.1016/j.expneurol.2013.01.015 · Cited by 59 · see citing works
“…dual LPS4h/HI insult greatly increased the mRNA levels of IL-1β, IL-6, and Tspo (Translocator protein of 18 kDa, a marker for microglia activation; Martin et al., 2010; Choi et al., 2011) in the brain at 24 h recovery, which were markedly attenuated by intranasal delivery of tat-NBD peptides (p…”
Background
Translocator Protein Distribution Volume Predicts Reduction of Symptoms During Open-Label Trial of Celecoxib in Major Depressive Disorder
Attwells, S., Setiawan, E., Rusjan, P., Xu, C., Hutton, C., Rafiei, D., Varughese, B., Kahn, A., Kish, S. J., Vasdev, N., et al. (2020) · Biological Psychiatry · doi:10.1016/j.biopsych.2020.03.007 · Cited by 60 · see citing works
A specific dietary intervention to restore brain structure and function after ischemic stroke
Wiesmann, M., Zinnhardt, B., Reinhardt, D., Eligehausen, S., Wachsmuth, L., Hermann, S., Dederen, P. J. W. C., Hellwich, M., Kuhlmann, M. T., Broersen, L. M., et al. (2017) · Theranostics · doi:10.7150/thno.17559 · Cited by 58 · see citing works
“Previous studies have shown that the majority of PET signal is due to increased expression of TSPO by microglia [46, 81].”
Background
Acute neuroinflammation in a clinically relevant focal cortical ischemic stroke model in rat: longitudinal positron emission tomography and immunofluorescent tracking
Tóth, M., Little, P., Arnberg, F., Häggkvist, J., Mulder, J., Halldin, C., Gulyás, B. Z., & Holmin, S. (2015) · Brain Structure and Function · doi:10.1007/s00429-014-0970-y · Cited by 55 · see citing works
Could 18 F-DPA-714 PET imaging be interesting to use in the early post-stroke period?
Ribeiro, M. J., Vercouillie, J., Debiais, S., Cottier, J., Bonnaud, I., Camus, V., Banister, S. D., Kassiou, M., Arlicot, N., & Guilloteau, D. (2014) · EJNMMI Research · doi:10.1186/s13550-014-0028-4 · Cited by 55 · see citing works
“They concluded that this finding was probably due to different mechanisms related to the expansion of infarction, such as spreading depression [36].”
BackgroundSelf-citation
PET measurement of cyclooxygenase-2 using a novel radioligand: upregulation in primate neuroinflammation and first-in-human study
Shrestha, S., Kim, M.-J., Eldridge, M. A. G., Lehmann, M. L., Frankland, M. P., Liow, J., Yu, Z., Cortes-Salva, M. Y., Telu, S., Henter, I. D., et al. (2020) · Journal of Neuroinflammation · doi:10.1186/s12974-020-01804-6 · Cited by 55 · see citing works
“COX-2 can be upregulated and return to baseline within hours [31], whereas upregulation of TSPO takes days and can last for weeks [5, 24].”
Background
[18F]DPA-714 PET imaging of translocator protein TSPO (18 kDa) in the normal and excitotoxically-lesioned nonhuman primate brain
Lavisse, S., Inoue, K., Jan, C., Peyronneau, M., Petit, F., Goutal, S., Dauguet, J., Guillermier, M., Dollé, F., Rbah‐Vidal, L., et al. (2014) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-014-2962-9 · Cited by 54 · see citing works
Self-citation
Differential Expression of the 18 kDa Translocator Protein (TSPO) by Neoplastic and Inflammatory Cells in Mouse Tumors of Breast Cancer
Zheng, J., Boisgard, R., Siquier-Pernet, K., Decaudin, D., Dollé, F., & Tavitian, B. (2011) · Molecular Pharmaceutics · doi:10.1021/mp100433c · Cited by 54 · see citing works
Self-citation
Synthesis and Structure–Activity Relationships of 5,6,7-Substituted Pyrazolopyrimidines: Discovery of a Novel TSPO PET Ligand for Cancer Imaging
Tang, D., McKinley, E. T., Hight, M. R., Uddin, M. I., Harp, J. M., Fu, A., Nickels, M. L., Buck, J. R., & Manning, H. C. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm4001874 · Cited by 53 · see citing works
11C-DPA-713 Versus 18F-GE-180: A Preclinical Comparison of Translocator Protein 18 kDa PET Tracers to Visualize Acute and Chronic Neuroinflammation in a Mouse Model of Ischemic Stroke
Chaney, A. M., Cropper, H. C., Johnson, E. M., Lechtenberg, K. J., Peterson, T. C., Stevens, M. Y., Buckwalter, M. S., & James, M. L. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.118.209155 · Cited by 52 · see citing works
“This is in line with our findings demonstrating TSPO expression in the infarct core and border colocalizes almost exclusively with CD68, and agrees with results from a previous study using MCAO rats (28).”
Result
PET Imaging with [18F]FSPG Evidences the Role of System xc- on Brain Inflammation Following Cerebral Ischemia in Rats
Domercq, M., Szczupak, B., Gejo, J., Gómez‐Vallejo, V., Padró, D., Gona, K. B., Dollé, F., Higuchi, M., Matute, C., Llop, J., et al. (2016) · Theranostics · doi:10.7150/thno.15616 · Cited by 52 · see citing works
“Nevertheless, these results stand in contrast with the in vivo PET imaging distribution of TSPO, a well-known marker for neuroinflammation, following cerebral ischemia [26, 38] (Figure 3).”
Self-citation
Immunofluorescent spectral analysis reveals the intrathecal cannabinoid agonist, AM1241, produces spinal anti‐inflammatory cytokine responses in neuropathic rats exhibiting relief from allodynia
Wilkerson, J. L., Gentry, K. R., Dengler, E. C., Wallace, J. A., Kerwin, A. A., Kuhn, M. N., Zvonok, A. M., Thakur, G. A., Makriyannis, A., & Milligan, E. D. (2012) · Brain and Behavior · doi:10.1002/brb3.44 · Cited by 51 · see citing works
“…examination of astrocytes and microglia, it is notable that astrocyte end-feet frequently make intimate contact with microglia (Choi et al. 2009; Martin et al. 2010), providing a potential mechanism by which microglia, albeit activated but in an anti-inflammatory manner, can influence astrocyte…”
Background
PET Imaging of Stroke-Induced Neuroinflammation in Mice Using [18F]PBR06
Lartey, F. M., Ahn, G., Shen, B., Cord, K.-T., Smith, T. N., Chua, J. Y., Rosenblum, S., Liu, H., James, M. L., Chernikova, S. B., et al. (2013) · Molecular Imaging and Biology · doi:10.1007/s11307-013-0664-5 · Cited by 51 · see citing works
“In contrast to this study, the PET images from prior studies were registered with an MRI template of the rat brain [25, 26] or with the MRI of a normal rat brain, rather than MRI for the individual animals [14, 15].”
BackgroundResult
Amyloid load and translocator protein 18 kDa in APPswePS1-dE9 mice: a longitudinal study
Sérrière, S., Tauber, C., Vercouillie, J., Mothes, C., Pruckner, C., Guilloteau, D., Kassiou, M., Doméné, A., Garreau, L., Page, G., et al. (2015) · Neurobiology of Aging · doi:10.1016/j.neurobiolaging.2014.11.023 · Cited by 49 · see citing works
Self-citation
Imaging of brain TSPO expression in a mouse model of amyotrophic lateral sclerosis with 18F-DPA-714 and micro-PET/CT
Gargiulo, S., Anzilotti, S., Coda, A. R. D., Gramanzini, M., Greco, A., Panico, M., Vinciguerra, A., Zannetti, A., Vicidomini, C., Dollé, F., et al. (2016) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-016-3311-y · Cited by 48 · see citing works
Self-citation
Visualization of early infarction in rat brain after ischemia using a translocator protein (18 kDa) PET ligand [11C]DAC with ultra-high specific activity
Yui, J., Hatori, A., Kawamura, K., Yanamoto, K., Yamasaki, T., Ogawa, M., Yoshida, Y., Kumata, K., Fujinaga, M., Nengaki, N., et al. (2010) · NeuroImage · doi:10.1016/j.neuroimage.2010.08.010 · Cited by 48 · see citing works
“The increasing tendency on the specific binding of [11C]PK11195 (25 GBq/μmol) or [18F]DPA-714 (37–111 MBq/μmol) to TSPO has also been detected during the first week after ischemia (Rojas et al., 2007; Martin et al., 2009).”
BackgroundMethodInfluential
Thalamic neuroinflammation as a reproducible and discriminating signature for chronic low back pain
Torrado-Carvajal, Á., Toschi, N., Albrecht, D., Chang, K., Akeju, O., Kim, M., Edwards, R. R., Zhang, Y., Hooker, J. M., Duggento, A., et al. (2020) · Pain · doi:10.1097/j.pain.0000000000002108 · Cited by 46 · see citing works
In VivoPET Imaging of the α4β2 Nicotinic Acetylcholine Receptor As a Marker for Brain Inflammation after Cerebral Ischemia
Martín, A., Szczupak, B., Gómez‐Vallejo, V., Domercq, M., Cano, A., Padró, D., Muñoz, C., Higuchi, M., Matute, C., & Llop, J. (2015) · Journal of Neuroscience · doi:10.1523/jneurosci.3670-14.2015 · Cited by 45 · see citing works
Self-citation
Specific Imaging of Inflammation with the 18kDa Translocator Protein Ligand DPA-714 in Animal Models of Epilepsy and Stroke
Harhausen, D., Sudmann, V., Khojasteh, U., Müller, J. M., Zille, M., Graham, K., Thiele, A., Dyrks, T., Dirnagl, U., & Wunder, A. (2013) · PLoS ONE · doi:10.1371/journal.pone.0069529 · Cited by 44 · see citing works
“In contrast to the given publications [22,23], the aim of this study was to evaluate the specificity of [(18)F]DPA-714/ [(3)H]-DPA714 by (i) correlating high-resolution autoradiography with immunohistochemistry and (ii) addressing the impact of bloodbrain barrier changes.”
MethodResultInfluential
In vivo imaging biomarkers of neuroinflammation in the development and assessment of stroke therapies - towards clinical translation
Zinnhardt, B., Wiesmann, M., Honold, L., Barca, C., Schäfers, M. A., Kiliaan, A. J., & Jacobs, A. H. (2018) · Theranostics · doi:10.7150/thno.24128 · Cited by 44 · see citing works
“TSPO PET [18F]DPA-714 Sprague–Dawley rats tMCAo (2h) 11 days [53]”
BackgroundMethod
Preparation and evaluation of novel pyrazolo[1,5-a]pyrimidine acetamides, closely related to DPA-714, as potent ligands for imaging the TSPO 18 kDa with PET
Médran‐Navarrete, V., Damont, A., Peyronneau, M., Kühnast, B., Bernards, N., Pottier, G., Marguet, F., Puech, F., Boisgard, R., & Dollé, F. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.01.080 · Cited by 41 · see citing works
Self-citation
The potential of carbon‐11 and fluorine‐18 chemistry: illustration through the development of positron emission tomography radioligands targeting the translocator protein 18 kDa
Damont, A., Roeda, D., & Dollé, F. (2013) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.2992 · Cited by 41 · see citing works
Self-citation
Evaluation of neuroprotective effect of glucagon‐like peptide 1 analogs using neuroimaging
Femminella, G. D., & Edison, P. (2014) · Alzheimer s & Dementia · doi:10.1016/j.jalz.2013.12.012 · Cited by 41 · see citing works
“[40] Martin A, Boisgard R, Theze B, van Camp N, Kuhnast B, Damont A, et al.”
Inflammation in stroke: the role of cholinergic, purinergic and glutamatergic signaling
Martín, A., Domercq, M., & Matute, C. (2018) · Therapeutic Advances in Neurological Disorders · doi:10.1177/1756286418774267 · Cited by 40 · see citing works
Self-citation
Impact of hydroxytyrosol on stroke: tracking therapy response on neuroinflammation and cerebrovascular parameters using PET-MR imaging and on functional outcomes
Barca, C., Wiesmann, M., Calahorra, J., Wachsmuth, L., Döring, C., Foray, C., Heiradi, A., Hermann, S., Peinado, M. Á., Siles, E., et al. (2021) · Theranostics · doi:10.7150/thno.48110 · Cited by 40 · see citing works
“Therefore, TSPO expression by microglia/infiltrating macrophages and astrocytes seems to be spatiotemporally dependent [62,64-66].”
Background
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO)
Reynolds, A. J., Hanani, R., Hibbs, D. E., Damont, A., Pozzo, E. D., Selleri, S., Dollé, F., Martini, C., & Kassiou, M. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.07.135 · Cited by 40 · see citing works
Self-citation
Synergy of Combined tPA-Edaravone Therapy in Experimental Thrombotic Stroke
Sun, Y., Morozov, Y. M., Yang, D., Li, Y., Dunn, R. S., RAKIC, P. T., Chan, P. H., Abe, K., Lindquist, D. M., & Kuan, C.-Y. (2014) · PLoS ONE · doi:10.1371/journal.pone.0098807 · Cited by 39 · see citing works
“The tPA-edaravone therapy also reduced the rise of inflammatory cytokine transcripts, including IL-1b, IL-6, and peripheral benzodiazepine receptor (TSPO, a marker of activated microglia [32]) in the ipsilateral hemisphere (Fig.”
Background
A microPET study of the regional distribution of [11C]-PK11195 binding following temporary focal cerebral ischemia in the rat. Correlation with post mortem mapping of microglia activation
Hughes, J. L., Jones, P. S., Beech, J. S., Wang, D., Menon, D. K., Aigbirhio, F. I., Fryer, T. D., & Baron, J. (2011) · NeuroImage · doi:10.1016/j.neuroimage.2011.10.060 · Cited by 39 · see citing works
“Mainly because of the unreliable radiosynthesis of 11C-PK11195 (Chauveau et al., 2008), other TSPO ligands have been developed, and several have already been used in rodent stroke models (Arlicot et al., 2010; Imaizumi et al., 2007; Martin et al., 2010; Yui et al., 2011; Yui et al., 2010).”
The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?
Luus, C., Hanani, R., Reynolds, A. J., & Kassiou, M. (2010) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.1752 · Cited by 38 · see citing works
Self-citation
Radiotracers for imaging of Parkinson's disease
Gharibkandi, N. A., & Hosseinimehr, S. J. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.01.029 · Cited by 38 · see citing works
PET imaging of cannabinoid type 2 receptors with [ 11 C]A-836339 did not evidence changes following neuroinflammation in rats
Pottier, G., Gómez‐Vallejo, V., Padró, D., Boisgard, R., Dollé, F., Llop, J., Winkeler, A., & Martín, A. (2017) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x16685105 · Cited by 38 · see citing works
Self-citation
In vivo Evaluation of Inflammatory Bowel Disease with the Aid of μPET and the Translocator Protein 18 kDa Radioligand [18F]DPA-714
Bernards, N., Pottier, G., Thezé, B., Dollé, F., & Boisgard, R. (2014) · Molecular Imaging and Biology · doi:10.1007/s11307-014-0765-9 · Cited by 36 · see citing works
Self-citation
Molecular Imaging of Immune Cell Dynamics During De- and Remyelination in the Cuprizone Model of Multiple Sclerosis by [<sup>18</sup>F]DPA-714 PET and MRI
Zinnhardt, B., Belloy, M., Fricke, I. B., Orije, J., Guglielmetti, C., Hermann, S., Wagner, S., Schäfers, M., Van der Linden, A., & Jacobs, A. H. (2019) · Theranostics · doi:10.7150/thno.32461 · Cited by 30 · see citing works
[18F]-DPA-714 PET as a specific in vivo marker of early microglial activation in a rat model of progressive dopaminergic degeneration
Rodríguez-Chinchilla, T., Quiroga‐Varela, A., Molinet-Dronda, F., Belloso-Iguerategui, A., Merino-Galán, L., Jiménez‐Urbieta, H., Gago, B., & Rodríguez‐Oroz, M. (2020) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-020-04772-4 · Cited by 35 · see citing works
“The synthesis of the radiotracer N,N-diethyl-2-(2-(4([(18)F]fluoro)phenyl)-5,7-dimethylpyrazolo[1,5-a] pyrimidin-3yl) acetamide ([(18)F]-DPA-714) was performed using a TRACERlab FX FN synthesis module (GE, Healthcare, Waukesha, WI, USA), based on a one-step procedure, as previously described [26, 27].”
Method
Thalamic neurometabolite alterations in patients with knee osteoarthritis before and after total knee replacement
Weerasekera, A., Morrissey, E. J., Kim, M., Saha, A., Lin, Y., Alshelh, Z., Torrado-Carvajal, Á., Albrecht, D., Akeju, O., Kwon, Y., et al. (2021) · Pain · doi:10.1097/j.pain.0000000000002198 · Cited by 33 · see citing works
Radiosynthesis and characterization of [18F]BS224: a next-generation TSPO PET ligand insensitive to the rs6971 polymorphism
Lee, S., Denora, N., Laquintana, V., Mangiatordi, G. F., Lopedota, A. A., Lopalco, A., Cutrignelli, A., Franco, M., Delre, P., Song, I. H., et al. (2021) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-021-05617-4 · Cited by 31 · see citing works
“As described in previous studies, high TSPO expression was observed in the LPS-induced neuroinflammatory rat model [55] 4 days after injection and was maximum 11 days following ischemic stroke [56, 57].”
Mannitol-facilitated perfusion staining with 2,3,5-triphenyltetrazolium chloride (TTC) for detection of experimental cerebral infarction and biochemical analysis
Sun, Y., Yang, D., & Kuan, C.-Y. (2011) · Journal of Neuroscience Methods · doi:10.1016/j.jneumeth.2011.09.029 · Cited by 31 · see citing works
Neuroinflammation and β Amyloid Deposition in Alzheimer's Disease: In vivo Quantification with Molecular Imaging
Hommet, C., Mondon, K., Camus, V., Ribeiro, M. J., Beaufils, É., Arlicot, N., Corcia, P., Paccalin, M., Minier, F., Gosselin, T., et al. (2013) · Dementia and Geriatric Cognitive Disorders · doi:10.1159/000354363 · Cited by 30 · see citing works
Detection and quantification of remote microglial activation in rodent models of focal ischaemia using the TSPO radioligand CLINDE
Arlicot, N., Petit, E., Katsifis, A. G., Toutain, J., Divoux, D., Bodard, S., Roussel, S., Guilloteau, D., Bernaudin, M., & Chalon, S. (2010) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-010-1598-7 · Cited by 28 · see citing works
Replicating predictive serum correlates of greater translocator protein distribution volume in brain
Attwells, S., Setiawan, E., Wilson, A. A., Rusjan, P., Miler, L., Xu, C., Hutton, C., Husain, M. I., Kish, S. J., Vasdev, N., et al. (2019) · Neuropsychopharmacology · doi:10.1038/s41386-019-0561-y · Cited by 27 · see citing works
“For example, when elevated TSPO VT is present, it is associated with microglial activation but TSPO overexpression is not fully selective for microglial activation since TSPO is detectable in other cells such as astroglia and endothelial cells [11, 12].”
Background
[18F]DPA-714 PET Imaging of AMD3100 Treatment in a Mouse Model of Stroke
Wang, Y., Yue, X., Kiesewetter, D. O., Wang, Z., Lu, J., Niu, G., Teng, G., & Chen, X. S. (2014) · Molecular Pharmaceutics · doi:10.1021/mp500234d · Cited by 27 · see citing works
In vivo imaging of Α7 nicotinic receptors as a novel method to monitor neuroinflammation after cerebral ischemia
Colás, L., Domercq, M., Ramos‐Cabrer, P., Palma, A., Gómez‐Vallejo, V., Padró, D., Plaza‐García, S., Pulagam, K. R., Higuchi, M., Matute, C., et al. (2018) · Glia · doi:10.1002/glia.23326 · Cited by 26 · see citing works
“These results stand in agreement with the PET imaging distribution of TSPO, a well-known marker for neuroinflammation following cerebral ischemia (Domercq et al., 2016; Martin et al., 2010; Martin et al., 2015).”
BackgroundResultSelf-citation
In vivo multimodal imaging of adenosine A1 receptors in neuroinflammation after experimental stroke
Joya, A., Ardaya, M., Montilla, A., Garbizu, M., Plaza‐García, S., Gómez‐Vallejo, V., Padró, D., Gutiérrez, J. J., Ríos, X., Ramos‐Cabrer, P., et al. (2020) · Theranostics · doi:10.7150/thno.51046 · Cited by 26 · see citing works
“TSPO overexpression has been used as a surrogate marker for inflammatory activation after ischemia [20, 24], while a recent work form our group has demonstrated that [18F]FLT PET is able to detect proliferative inflammatory cells in the ischemic area after stroke [25].”
MethodSelf-citation
A Longitudinal PET/MRI Study of Colony-Stimulating Factor 1 Receptor–Mediated Microglia Depletion in Experimental Stroke
Barca, C., Kiliaan, A. J., Foray, C., Wachsmuth, L., Hermann, S., Faber, C., Schäfers, M. A., Wiesmann, M., Jacobs, A. H., & Zinnhardt, B. (2021) · Journal of Nuclear Medicine · doi:10.2967/jnumed.121.262279 · Cited by 24 · see citing works
“Established temporal dynamics of 18F-DPA-714 in stroke indicates the number of CD11b+TSPO+/Iba-1+TSPO+ cells peak around days 11-14, correlating with the peak of radiotracer uptake (21,22).”
Background
In vivo imaging translocator protein (TSPO) in autism spectrum disorder
Simpson, D., Gharehgazlou, A., Silva, T. M. S., Labrie‐Cleary, C., Wilson, A. A., Meyer, J. H., Mizrahi, R., & Rusjan, P. (2022) · Neuropsychopharmacology · doi:10.1038/s41386-022-01306-4 · Cited by 25 · see citing works
Inflammation, Obsessive-Compulsive Disorder, and Related Disorders
Meyer, J. H. (2021) · Current topics in behavioral neurosciences · doi:10.1007/7854_2020_210 · Cited by 24 · see citing works
The Relationship Between Serial [18 F]PBR06 PET Imaging of Microglial Activation and Motor Function Following Stroke in Mice
Lartey, F. M., Ahn, G., Ali, R., Rosenblum, S., Miao, Z., Arksey, N., Shen, B., Vilalta, M., Rafat, M., Liu, H., et al. (2014) · Molecular Imaging and Biology · doi:10.1007/s11307-014-0745-0 · Cited by 24 · see citing works
“Microglial activation was reported to peak at 11 days but reduced gradually over the next 20 days [33].”
Evaluation of the novel TSPO radiotracer [18F] VUIIS1008 in a preclinical model of cerebral ischemia in rats
Pulagam, K. R., Colás, L., Padró, D., Plaza‐García, S., Gómez‐Vallejo, V., Higuchi, M., Llop, J., & Martín, A. (2017) · EJNMMI Research · doi:10.1186/s13550-017-0343-7 · Cited by 24 · see citing works
“better signal-to-noise ratio in the ischemic lesion and the low level of non-specific binding in the contralateral brain hemisphere [3, 22, 24].”
BackgroundResultInfluentialSelf-citation
Positron emission tomography with 11C-flumazenil in the rat shows preservation of binding sites during the acute phase after 2h-transient focal ischemia
Rojas, S., Martín, A., Pareto, D., Herance, J. R., Abad, S., Ruiz, A., Flotats, N., Gispert, J. D., Llop, J., Gómez‐Vallejo, V., et al. (2011) · Neuroscience · doi:10.1016/j.neuroscience.2011.03.013 · Cited by 23 · see citing works
Self-citation
Lack of neuroinflammation in the HIV-1 transgenic rat: an [18F]-DPA714 PET imaging study
Lee, D. E., Yue, X., Ibrahim, W. G., Lentz, M. R., Peterson, K. L., Jagoda, E. M., Kassiou, M., Maric, D., Reid, W. C., & Hammoud, D. A. (2015) · Journal of Neuroinflammation · doi:10.1186/s12974-015-0390-9 · Cited by 23 · see citing works
“In this study, we set out to validate one of the newly designed TSPO ligands, [F]DPA-714, an F-labeled pyrazolopyrimidine, [19, 20, 26], as surrogate imaging biomarker of microglial activation (neuroinflammation), in vivo, in the brains of HIV-1 transgenic rats (Tg) compared to agematched controls.”
BackgroundMethodInfluentialSelf-citation
Neuroprotective effect of salvianolate lyophilized injection against cerebral ischemia in type 1 diabetic rats
Wang, F., He, Q., Wang, J., Yuan, Q., Guo, H. W., Chai, L., Wang, S., Hu, L., & Zhang, Y. (2017) · BMC Complementary and Alternative Medicine · doi:10.1186/s12906-017-1738-8 · Cited by 23 · see citing works
PET Imaging for Dynamically Monitoring Neuroinflammation in APP/PS1 Mouse Model Using [18F]DPA714
Hu, W., Pan, D., Wang, Y., Bao, W., Zuo, C., Guan, Y., Hua, F., Yang, M., & Zhao, J. (2020) · Frontiers in Neuroscience · doi:10.3389/fnins.2020.00810 · Cited by 22 · see citing works
“[18F]DPA714 PET has been used for various neuroinflammation models (Doorduin et al., 2009; Martín et al., 2009; Boutin et al., 2013; Lavisse et al., 2014; Wang et al., 2014).”
Method
TSPO imaging in stroke: from animal models to human subjects
Boutin, H., & Pinborg, L. H. (2015) · Clinical and Translational Imaging · doi:10.1007/s40336-015-0146-7 · Cited by 22 · see citing works
In vivo Imaging of Cannabinoid Type 2 Receptors: Functional and Structural Alterations in Mouse Model of Cerebral Ischemia by PET and MRI
Ni, R., Herde, A. M., Haider, A., Keller, C., Louloudis, G., Vaas, M., Schibli, R., Ametamey, S., Klohs, J., & Mu, L. (2021) · bioRxiv · doi:10.1007/s11307-021-01655-4 · Cited by 21 · see citing works

Evaluation of the TSPO (18KDa)/PBR radioligand ( 18 F) DPA-714 in a rat model of focal cerebral ischemia
Martín, A., Boisgard, R., Dollé, F., Camp, N. V., Thezé, B., Kassiou, M., & Tavitian, B. (2009)
Self-citation
Reduced PBR/TSPO Expression After Minocycline Treatment in a Rat Model of Focal Cerebral Ischemia: A PET Study Using [18F]DPA-714
Martín, A., Boisgard, R., Kassiou, M., Dollé, F., & Tavitian, B. (2010) · Molecular Imaging and Biology · doi:10.1007/s11307-010-0324-y · Cited by 68 · see citing works
Self-citation
Could 18 F-DPA-714 PET imaging be interesting to use in the early post-stroke period?
Ribeiro, M. J., Vercouillie, J., Debiais, S., Cottier, J., Bonnaud, I., Camus, V., Banister, S. D., Kassiou, M., Arlicot, N., & Guilloteau, D. (2014) · EJNMMI Research · doi:10.1186/s13550-014-0028-4 · Cited by 55 · see citing works
Self-citation
Cerebral focal neuroinflammation after acute stroke: Preliminary study with 18F-DPA-714
Ribeiro, M. J., Vercouillie, J., Cottier, J., Debiais, S., Bonnaud, I., Arlicot, N., Kassiou, M., & Guilloteau, D. (2013) · Journal of Nuclear Medicine
Self-citation
Detection of neuroinflammation before selective neuronal loss appearance after mild focal ischemia using [18F]DPA-714 imaging
Miyajima, N., Ito, M., Rokugawa, T., Iimori, H., Momosaki, S., Omachi, S., Shimosegawa, E., Hatazawa, J., & Abe, K. (2018) · EJNMMI Research · doi:10.1186/s13550-018-0400-x · Cited by 21 · see citing works

Authors: Martín, A., Boisgard, R., Thézé, B., Van Camp, N., Kuhnast, B., Damont, A., Kassiou, M., Dollé, F., & Tavitian, B.
Affiliations: Inserm (FR)
INSERM U803, Orsay, France
CEA, DSV, FBM, SHFJ, Laboratoire Imagerie Moléculaire Expérimentale, Orsay, France
Commissariat à l'Énergie Atomique et aux Énergies Alternatives (FR)
The University of Sydney (AU)
Corresponding author: Tavitian, Bertrand
ORCID: Martín, Abraham
Damont, Annelaure
Kassiou, Michael
Tavitian, Bertrand
Venue: Journal of Cerebral Blood Flow & Metabolism
Publisher: SAGE Publications
Published: 2009-09-30
Volume: 30
Issue: 1
Pages: 230-241
ISSN: 0271-678X (ISSN-L)
1559-7016
DOI: 10.1038/jcbfm.2009.205
PMC: PMC2949091
OpenAlex: W1982808247
Cited by: 206
References: 33
Citations by year: 2025: 6 · 2024: 6 · 2023: 6 · 2022: 7 · 2021: 39 · 2020: 23 · 2019: 11 · 2018: 11 · 2017: 8 · 2016: 12 · 2015: 15 · 2014: 14 · 2013: 11 · 2012: 12
FWCI: 7.48
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: journals.sagepub.com/page/policies/text-and-data-mining-license (tdm)
Locations: Journal of Cerebral Blood Flow & Metabolism (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Neuroscience › Neurology › Neuroinflammation and Neurodegeneration Mechanisms
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Pharmacological Receptor Mechanisms and Effects
Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
Keywords: [18F]DPA-714, focal cerebral ischemia, stroke, neuroinflammation, microglia/macrophages, astrocytes, PET radiotracer, rat model
MeSH terms: Animals, Astrocytes, Autoradiography, Carrier Proteins, Cell Count, Brain Ischemia, Data Interpretation, Statistical, Fluorine Radioisotopes, Image Processing, Computer-Assisted, Immunohistochemistry, Inflammation, Male, Pyrazoles, Pyrimidines, Receptors, GABA-A, Models, Statistical, Rats, Sprague-Dawley, Microglia, Radiopharmaceuticals, Stroke, Positron-Emission Tomography, Rats

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Evaluation of the PBR/TSPO Radioligand [ 18 F]DPA-714 in a Rat Model of Focal Cerebral Ischemia

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