In vivo imaging and characterization of [(18)F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET (865 views) (PDF restricted 290 views)
Nucl Med Biol (ISSN: 0969-8051, 0883-2897, 0969-8051linking), 2015 Mar; 42(3): 309-316.
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Paper type: Journal Article, Research Support, Non-U. S. Gov'T
Impact factor: 2.429, 5-year impact factor: 2.299
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84922883622&partnerID=40&md5=11ee166d047d6864c454e3bd3601bcfd
Keywords: Biodistribution, Microglia, Neuroinflammation, Pet, Tspo, [18f]dpa-714, Benzodiazepine Receptor, N Diethyl 2 [2 [4 (2 Fluoroethoxy)phenyl] 5, 7 Dimethylpyrazolo[1, 5 A]pyrimidin 3 Yl]acetamide F 18, Radiopharmaceutical Agent, Translocator Protein 18, Unclassified Drug, Animal Experiment, Article, Brain, Competitive Inhibition, Controlled Study, Heart, High Performance Liquid Chromatography, In Vivo Study, Mouse, Nonhuman, Pet-Ct Scanner, Positron Emission Tomography, Radioactivity, Spleen, Tissue Distribution, [(18)f]dpa-714, 4 Aminobutyric Acid Receptor, Bzrp Protein, Fluorine, Isoquinoline Derivative, Ligand, N Sec Butyl 1 (2 Chlorophenyl) N Methyl 3 Isoquinolinecarboxamide, N-Diethyl-2-(2-(4-(2-Fluoroethoxy)phenyl)-5, 7-Dimethylpyrazolo(1, 5-A)pyrimidin-3-Yl)acetamide, Pyrazole Derivative, Pyrimidine Derivative, Binding Competition, Computer Assisted Tomography, Diagnostic Use, Drug Effects, Metabolism, Radiography, Scintiscanning, Fluorine Radioisotopes, Positron-Emission Tomography, X-Ray Computed, Brain Diagnostic Imaging Drug Effects Metabolism , Isoquinolines Pharmacology , Pyrazoles Metabolism Pharmacokinetics Pharmacology , Pyrimidines Metabolism Pharmacokinetics Pharmacology , Gaba Metabolism
Affiliations:
*** IBB - CNR ***
Institute of Biostructure and Bioimaging, CNRNaples, Italy
Department of Advanced Biomedical Sciences, Federico II UniversityNaples, Italy
CEINGE, Biotecnologie Avanzate, s.c.a.r.l.Naples, Italy
Inserm U970, PARCC, Université Paris Descartes, Hôpital Européen Georges PompidouParis, France
CEA, I2BM, Service Hospitalier Frédéric JoliotOrsay, France
References:
Not available.
Nucl Med Biol (ISSN: 0969-8051, 0883-2897, 0969-8051linking), 2015 Mar; 42(3): 309-316.
Export to BibTeX Export to EndNote
Paper type: Journal Article, Research Support, Non-U. S. Gov'T
Impact factor: 2.429, 5-year impact factor: 2.299
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84922883622&partnerID=40&md5=11ee166d047d6864c454e3bd3601bcfd
Keywords: Biodistribution, Microglia, Neuroinflammation, Pet, Tspo, [18f]dpa-714, Benzodiazepine Receptor, N Diethyl 2 [2 [4 (2 Fluoroethoxy)phenyl] 5, 7 Dimethylpyrazolo[1, 5 A]pyrimidin 3 Yl]acetamide F 18, Radiopharmaceutical Agent, Translocator Protein 18, Unclassified Drug, Animal Experiment, Article, Brain, Competitive Inhibition, Controlled Study, Heart, High Performance Liquid Chromatography, In Vivo Study, Mouse, Nonhuman, Pet-Ct Scanner, Positron Emission Tomography, Radioactivity, Spleen, Tissue Distribution, [(18)f]dpa-714, 4 Aminobutyric Acid Receptor, Bzrp Protein, Fluorine, Isoquinoline Derivative, Ligand, N Sec Butyl 1 (2 Chlorophenyl) N Methyl 3 Isoquinolinecarboxamide, N-Diethyl-2-(2-(4-(2-Fluoroethoxy)phenyl)-5, 7-Dimethylpyrazolo(1, 5-A)pyrimidin-3-Yl)acetamide, Pyrazole Derivative, Pyrimidine Derivative, Binding Competition, Computer Assisted Tomography, Diagnostic Use, Drug Effects, Metabolism, Radiography, Scintiscanning, Fluorine Radioisotopes, Positron-Emission Tomography, X-Ray Computed, Brain Diagnostic Imaging Drug Effects Metabolism , Isoquinolines Pharmacology , Pyrazoles Metabolism Pharmacokinetics Pharmacology , Pyrimidines Metabolism Pharmacokinetics Pharmacology , Gaba Metabolism
Affiliations:
*** IBB - CNR ***
Institute of Biostructure and Bioimaging, CNRNaples, Italy
Department of Advanced Biomedical Sciences, Federico II UniversityNaples, Italy
CEINGE, Biotecnologie Avanzate, s.c.a.r.l.Naples, Italy
Inserm U970, PARCC, Université Paris Descartes, Hôpital Européen Georges PompidouParis, France
CEA, I2BM, Service Hospitalier Frédéric JoliotOrsay, France
References:
Not available.
In vivo imaging and characterization of [(18)F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET
Introduction: The translocator protein 18kDa (TSPO), a biochemical marker of neuroinflammation, is highly expressed in the brain activated microglia and it is also expressed by peripheral inflammatory cells and normal peripheral tissues. Thus, development of radioligands for the TSPO may contribute to further understanding the in vivo TSPO function in central and peripheral inflammatory processes and other pathologies. Here, we report the biodistribution, the specific binding and the radiometabolites of [18F]DPA-714, a promising fluorinated PET radiotracer, in normal mice using a microPET/CT scanner. Methods: The in vivo biodistribution and kinetics of [18F]DPA-714 were measured in mice brain and peripheral tissues. Specific binding to TSPO sites was assessed using pharmacological competitive studies by means of saturation experiments performed by i.v. injection of 1mg/kg of unlabeled DPA-714 or 3mg/kg of unlabeled PK11195. A region of interest analysis was performed to generate time-activity curves in the brain, heart, lung, kidney, spleen and liver. Metabolites assay was performed in the plasma and peripheral organs by radio-HPLC. Results: [18F]DPA-714 reached high concentration in lung, heart, kidney and spleen, tissues well known to be rich in TSPO sites. [18F]DPA-714 kinetics were faster in the lung and slower in the kidney. Pre-injection of unlabeled DPA-714 or PK11195 inhibited about 80% of [18F]DPA-714 uptake in the lung and heart (p<0.0005). The percentage of inhibition in the kidney was lower and achieved at later times only with DPA-714 (p<0.05) but not with PK11195. Sixty minutes after radiotracer injection only unmetabolized radioligand was found in the brain, lung, heart and spleen. Conclusion: These results suggest that [18F]DPA-714 is a suitable PET ligand for imaging in mice brain and peripheral tissues since it binds with high specificity TSPO binding sites and it is almost unchanged at 60minutes after radiotracer injection in the brain and TSPO-rich regions. © 2014 Elsevier Inc.
Introduction: The translocator protein 18kDa (TSPO), a biochemical marker of neuroinflammation, is highly expressed in the brain activated microglia and it is also expressed by peripheral inflammatory cells and normal peripheral tissues. Thus, development of radioligands for the TSPO may contribute to further understanding the in vivo TSPO function in central and peripheral inflammatory processes and other pathologies. Here, we report the biodistribution, the specific binding and the radiometabolites of [18F]DPA-714, a promising fluorinated PET radiotracer, in normal mice using a microPET/CT scanner. Methods: The in vivo biodistribution and kinetics of [18F]DPA-714 were measured in mice brain and peripheral tissues. Specific binding to TSPO sites was assessed using pharmacological competitive studies by means of saturation experiments performed by i.v. injection of 1mg/kg of unlabeled DPA-714 or 3mg/kg of unlabeled PK11195. A region of interest analysis was performed to generate time-activity curves in the brain, heart, lung, kidney, spleen and liver. Metabolites assay was performed in the plasma and peripheral organs by radio-HPLC. Results: [18F]DPA-714 reached high concentration in lung, heart, kidney and spleen, tissues well known to be rich in TSPO sites. [18F]DPA-714 kinetics were faster in the lung and slower in the kidney. Pre-injection of unlabeled DPA-714 or PK11195 inhibited about 80% of [18F]DPA-714 uptake in the lung and heart (p<0.0005). The percentage of inhibition in the kidney was lower and achieved at later times only with DPA-714 (p<0.05) but not with PK11195. Sixty minutes after radiotracer injection only unmetabolized radioligand was found in the brain, lung, heart and spleen. Conclusion: These results suggest that [18F]DPA-714 is a suitable PET ligand for imaging in mice brain and peripheral tissues since it binds with high specificity TSPO binding sites and it is almost unchanged at 60minutes after radiotracer injection in the brain and TSPO-rich regions. © 2014 Elsevier Inc.
In vivo imaging and characterization of [(18)F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET
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In vivo imaging and characterization of [(18)F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET
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Coda AR, Anzilotti S, Boscia F, Greco A, Panico M, Gargiulo S, Gramanzini M, Zannetti A, Albanese S, Pignataro G, Annunziato L, Salvatore M, Brunetti A, De Berardinis P, Quarantelli M, Palma G, Pappata S
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Varrone A, Soricelli A, Postiglione A, Salvatore M, Lassen N
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Soricelli A, Postiglione A, GrivetFojaja M, Mainenti PP, Discepolo A, Varrone A, Salvatore M, Lassen N
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Impact Factor: 2.692
View Export to BibTeX Export to EndNote
* In vivo imaging of CNS microglial activation/macrophage infiltration with combined [(18)F]DPA-714-PET and SPIO-MRI in a mouse model of relapsing remitting experimental autoimmune encephalomyelitis (248 views) (PDF 85 views)
Eur J Nucl Med (ISSN: 1619-7070linking, 1619-7089electronic, 1619-7070print), 2021 Jan; 48(1): 40-52.
Impact Factor: 7.18
View Export to BibTeX Export to EndNote
Rendina A, Drongitis D, Donizetti A, Fucci L, Milan G, Tripodi F, Giustezza F, Postiglione A, Pappata S, Ferrari R, Bossù P, Angiolillo A, Di Costanzo A, Caiazzo M, Vitale E
* CD33 and SIGLECL1 Immunoglobulin Superfamily Involved in Dementia (155 views)
J Neuropathol Exp Neurol (ISSN: 0022-3069linking), 2020 Jul 10; 79(8): 891-901.
Impact Factor: 3.51
View Export to BibTeX Export to EndNote
Perani D, Iaccarino L, Lammertsma AA, Windhorst AD, Edison P, Boellaard R, Hansson O, Nordberg A, Jacobs AH, Bottlaender M, Brooks D, Carroll MA, Chalon S, Gee A, Gerhard A, Halldin C, Herholz K, Herth MM, Hinz R, Knudsen GM, Kuhnast B, López-picón F, Moresco RM, Pappata S, Rinne JO, Rodriguez-vieitez E, Santiago-ribeiro MJ, Turkheimer FE, Van Laere K, Varrone A, Vercouillie J, Winkeler A
* A new perspective for advanced positron emission tomography-based molecular imaging in neurodegenerative proteinopathies (274 views)
Alzheimers Dement (ISSN: 1552-5260linking), 2019 Jun 20; N/D: N/D-N/D.
Impact Factor: 14.43
View Export to BibTeX Export to EndNote
Perani D, Iaccarino L, Jacobs AH, Lammertsma AA, Nordberg A, Windhorst AD, Gerhard A, Winkeler A, Jacobs AH, Gee A, Kuhnast B, Halldin C, Perani D, Brooks D, Rodriguez-vieitez E, Turkheimer FE, López-picón F, Knudsen GM, Vercouillie J, Rinne JO, Herholz K, Van Laere K, Santiago-ribeiro MJ, Herth MM, Carroll MA, Bottlaender M, Hansson O, Edison P, Hinz R, Boellaard R, Moresco RM, Pappata S
* Application of advanced brain positron emission tomography-based molecular imaging for a biological framework in neurodegenerative proteinopathies (318 views)
Alzheimers Dement (ISSN: 2352-8729print), 2019 Apr 16; 11: 327-332.
Impact Factor: 14.423
View Export to BibTeX Export to EndNote
Ugga L, Romeo V, Tedeschi E, Brunetti A, Quarantelli M
* Superparamagnetic iron oxide nanocolloids in MRI studies of neuroinflammation (757 views)
J Neurosci Methods (ISSN: 0165-0270linking, 1872-678xelectronic), 2018 Jun 18; 310: 12-23.
Impact Factor: 2.668
View Export to BibTeX Export to EndNote
Garello F, Pagoto A, Arena F, Buffo A, Blasi F, Alberti D, Terreno E
* MRI visualization of neuroinflammation using VCAM-1 targeted paramagnetic micelles (268 views)
Nanomedicine (ISSN: 1549-9634, 1549-9642), 2017 Nov 8; N/D: N/D-N/D.
Impact Factor: 6.5
View Export to BibTeX Export to EndNote
Pontillo G, Cocozza S, Lanzillo R, Borrelli P, De Rosa A, Brescia Morra V, Tedeschi E, PalmaG
* Brain Susceptibility Changes in a Patient with Natalizumab-Related Progressive Multifocal Leukoencephalopathy: A Longitudinal Quantitative Susceptibility Mapping and Relaxometry Study (297 views)
Front Neurol (ISSN: 1664-2295, 1664-2295linking, 1664-2295print), 2017 Jun 19; 8: 294-294.
Impact Factor: 3.508
View Export to BibTeX Export to EndNote
Gargiulo S, Coda AR, Panico M, Gramanzini M, Moresco RM, Chalon S, Pappata S
* Molecular imaging of neuroinflammation in preclinical rodent models using positron emission tomography (387 views)
Q J Nucl Med Mol Im (ISSN: 1824-4785, 1824-4478, 1827-1936), 2017 Mar; 61(1): 60-75.
Impact Factor: 2.368
View Export to BibTeX Export to EndNote
Quarantelli M
* MRI/MRS in neuroinflammation: methodology and applications (399 views)
Clin Transl Imaging (ISSN: 2281-5872print, 2281-5872linking), 2015; 3(6): 475-489.
Impact Factor: 0
View Export to BibTeX Export to EndNote
Jacobs AH, Tavitian B, TheInmindG, Pappata S, Quarantelli M
* Noninvasive molecular imaging of neuroinflammation (398 views) (PDF 216 views)
J Cereb Blood Flow Metab (ISSN: 0271-678x, 1559-7016electronic), 2012 Jul; 32(7): 1393-1415.
Impact Factor: 5.398
View Export to BibTeX Export to EndNote
Takano A, Gulyas B, Varrone A, Karlsson P, Sjoholm N, Larsson S, Jonsson C, Odh R, Sparks R, Al Tawil N, Hoffmann A, Zimmermann T, Thiele A, Halldin C
* Biodistribution and radiation dosimetry of the 18 kDa translocator protein (TSPO) radioligand [ 18F]FEDAA1106: A human whole-body PET study (487 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2011 Nov; 38(11): 2058-2065.
Impact Factor: 4.991
View Export to BibTeX Export to EndNote
Varrone A, Stepanov V, Nakao R, Toth M, Gulyas B, Emond P, Deloye JB, Vercouillie J, Stabin MG, Jonsson C, Guilloteau D, Halldin C
* Imaging of the striatal and extrastriatal dopamine transporter with 18F-LBT-999: Quantification, biodistribution, and radiation dosimetry in nonhuman primates (625 views)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2011 Sep 1; 52(8): 1313-1321.
Impact Factor: 6.381
View Export to BibTeX Export to EndNote
Gulyas B, Vas A, Toth M, Takano A, Varrone A, Cselenyi Z, Schain M, Mattsson P, Halldin C
* Age and disease related changes in the translocator protein (TSPO) system in the human brain: Positron emission tomography measurements with [11C]vinpocetine (664 views)
Neuroimage (ISSN: 1053-8119, 1053-8119linking), 2011 Jun 1; 56(3): 1111-1121.
Impact Factor: 5.895
View Export to BibTeX Export to EndNote
Pappata S, Varrone A, Vicidomini C, Milan G, De Falco C, Sansone V, Iavarone A, Comerci M, Loré E, Panico M, Quarantelli M, Postiglione A, Salvatore M
* SPECT imaging of GABAA/benzodiazepine receptors and cerebral perfusion in mild cognitive impairment (593 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2010 Jun; 37(6): 1156-1163.
Impact Factor: 5.036
View Export to BibTeX Export to EndNote
Odano I, Halldin C, Karlsson P, Varrone A, Airaksinen AJ, Krasikova RN, Farde L
* [18F]Flumazenil binding to central benzodiazepine receptor studies by PET. - Quantitative analysis and comparisons with [11C]flumazenil (443 views)
Neuroimage (ISSN: 1053-8119, 1053-8119linking), 2009 Apr 15; 45(3): 891-902.
Impact Factor: 5.739
View Export to BibTeX Export to EndNote
Vergote J, Chalon S, Emond P, Vercouillie J, Pappata S, Guilloteau D
* New SPECT and PET dementia tracers (438 views)
Med Nucl (ISSN: 0928-1258), 2009 Mar; 33(3): 137-141.
Impact Factor: 0.155
View Export to BibTeX Export to EndNote
Takano A, Halldin C, Varrone A, Karlsson P, Sjoholm N, Stubbs JB, Schou M, Airaksinen AJ, Tauscher J, Gulyas B
* Biodistribution and radiation dosimetry of the norepinephrine transporter radioligand (S, S)-[18F]FMeNER-D2: A human whole-body PET study (533 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Mar; 35(3): 630-636.
Impact Factor: 4.532
View Export to BibTeX Export to EndNote
Fonti R, Cheung N-KV, Bridger GJ, Guo H-F, Abrams MJ, Larson SM
99mTc-monoclonal antibody radiolabeled via hydrazino nicotinamide derivative for imaging disialoganglioside G(D2)-positive tumors (550 views)
Nucl Med Biol (ISSN: 0969-8051, 0883-2897), 1999; 26(6): 681-686.
Impact Factor: 1.623
View Export to BibTeX Export to EndNote
Varrone A, Soricelli A, Postiglione A, Salvatore M, Lassen N
Benzodiazepine receptor distribution in Alzheimer's disease with (123)I-iomazenil by SPECT (361 views)
Textbook Of Spect In Neurology And Psychiatry, 1997; N/D: N/D-N/D.
Impact Factor: 0
View Export to BibTeX Export to EndNote
Soricelli A, Postiglione A, GrivetFojaja M, Mainenti PP, Discepolo A, Varrone A, Salvatore M, Lassen N
Reduced cortical distribution volume of iodine-123 iomazenil in Alzheimer's disease as a measure of loss of synapses (520 views)
Eur J Nucl Med (ISSN: 0340-6997, 1619-7070, 1619-7089), 1996 Oct; 23(10): 1323-1328.
Impact Factor: 2.692
View Export to BibTeX Export to EndNote
20 Records (19 excluding Abstracts).
Total impact factor: 97.029 (97.029 excluding Abstracts).
Total 5 year impact factor: 66.285 (66.285 excluding Abstracts).
Total impact factor: 97.029 (97.029 excluding Abstracts).
Total 5 year impact factor: 66.285 (66.285 excluding Abstracts).
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