Imaging of the striatal and extrastriatal dopamine transporter with 18F-LBT-999: Quantification, biodistribution, and radiation dosimetry in nonhuman primates (772 views)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2011 Sep 1; 52(8): 1313-1321.
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Paper type: Journal Article,
Impact factor: 6.381, 5-year impact factor: 6.527
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-80051682570&partnerID=40&md5=b91eaee5d8c61f1431113f1822517248
Keywords: Dopamine Transporter, Radiobiology Dosimetry, Radiotracer Tissue Kinetics, Reference Tissue Method, Methyl 8 (4 Fluoro But 2 En 1 Yl) 3 (4 Tolyl) 8 Azabicyclo[3 2 1]octane 2 Carboxylate F 18, Radiopharmaceutical Agent, Unclassified Drug, Animal Experiment, Article, Caudate Nucleus, Controlled Study, Corpus Striatum, Drug Accumulation, Drug Blood Level, Drug Excretion, Drug Protein Binding, Female, Mesencephalon, Nonhuman, Positron Emission Tomography, Primate, Priority Journal, Putamen, Quantitative Analysis, Radiation Dose Distribution, Radioactivity, Thalamus, Tissue Distribution, Brain, Cocaine, Dopamine Plasma Membrane Transport Proteins, Fluorine Radioisotopes, Macaca Mulatta, Positron-Emission Tomography, Radiometry, Time Factors, X-Ray Computed, Treatment Outcome, Methyl 8 (4 Fluoro But 2 En 1 Yl) 3 (4 Tolyl) 8 Azabicyclo [3 2 1] Octane 2 Carboxylate F 18,
Affiliations:
*** IBB - CNR ***
Department of Clinical Neuroscience, Centre for Psychiatry Research, R5:02, Karolinska Hospital, SE-17176, Stockholm, Sweden
INSERM U930, CHRU Tours, Tours, France
Laboratoires Cyclopharma, Saint Beauzire, France
Department of Radiology and Radiological Sciences, Vanderbilt University, Nashville, TN, United States
Department of Nuclear Medicine, Karolinska Hospital, Stockholm, Sweden
References:
Not available.
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2011 Sep 1; 52(8): 1313-1321.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 6.381, 5-year impact factor: 6.527
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-80051682570&partnerID=40&md5=b91eaee5d8c61f1431113f1822517248
Keywords: Dopamine Transporter, Radiobiology Dosimetry, Radiotracer Tissue Kinetics, Reference Tissue Method, Methyl 8 (4 Fluoro But 2 En 1 Yl) 3 (4 Tolyl) 8 Azabicyclo[3 2 1]octane 2 Carboxylate F 18, Radiopharmaceutical Agent, Unclassified Drug, Animal Experiment, Article, Caudate Nucleus, Controlled Study, Corpus Striatum, Drug Accumulation, Drug Blood Level, Drug Excretion, Drug Protein Binding, Female, Mesencephalon, Nonhuman, Positron Emission Tomography, Primate, Priority Journal, Putamen, Quantitative Analysis, Radiation Dose Distribution, Radioactivity, Thalamus, Tissue Distribution, Brain, Cocaine, Dopamine Plasma Membrane Transport Proteins, Fluorine Radioisotopes, Macaca Mulatta, Positron-Emission Tomography, Radiometry, Time Factors, X-Ray Computed, Treatment Outcome, Methyl 8 (4 Fluoro But 2 En 1 Yl) 3 (4 Tolyl) 8 Azabicyclo [3 2 1] Octane 2 Carboxylate F 18,
Affiliations:
*** IBB - CNR ***
Department of Clinical Neuroscience, Centre for Psychiatry Research, R5:02, Karolinska Hospital, SE-17176, Stockholm, Sweden
INSERM U930, CHRU Tours, Tours, France
Laboratoires Cyclopharma, Saint Beauzire, France
Department of Radiology and Radiological Sciences, Vanderbilt University, Nashville, TN, United States
Department of Nuclear Medicine, Karolinska Hospital, Stockholm, Sweden
References:
Not available.
Imaging of the striatal and extrastriatal dopamine transporter with 18F-LBT-999: Quantification, biodistribution, and radiation dosimetry in nonhuman primates
The aim of this study was to evaluate the quantification, biodistribution, and radiation dosimetry of the novel dopamine transporter (DAT) radioligand 18F-(2S,3S)-methyl 8-((E)-4-fluorobut-2-en-1-yl)-3-(p-tolyl)-8- azabicyclo[3.2.1]octane-2-carboxylate (18F-LBT-999) in nonhuman primates. Methods: The brain study was conducted in 4 female rhesus monkeys. PET measurements were conducted for 243 min using the high-resolution research tomograph (HRRT) with the measurement of the metabolite-corrected arterial input function and protein binding. Quantification was performed with kinetic analysis using 2-tissue- and 1-tissue-compartment models, with Logan graphical analysis and with different reference tissue models. The outcome measures were total distribution volume (VT), nondisplaceable distribution volume (VND), binding potential relative to the free concentration of radioligand in plasma (BPF), and binding potential relative to the concentration of nondisplaceable radioligand in tissue (BPND) = VT - VND/VND using the cerebellum as a reference region. For the biodistribution and radiation dosimetry, 2 female cynomolgus monkeys were studied.Whole-body PET scans were obtained using a PET/CT system for approximately 250 min. Estimates of the absorbed radiation dose in humans were calculated using OLINDA/EXM software. Results: 18F-LBT-999 showed good brain uptake (300% standardized uptake value) and regional distribution according to known DAT density. The 2-tissuecompartment model was the preferred model for the quantification. Late peak equilibrium (120-140 min) and slow washout were observed in the striatum, with high variability of VT, BPF, and BPND. When the different models were compared with the 2-tissuecompartment model, the underestimation of VT or BPND was larger in the caudate and putamen than in the midbrain and thalamus. The reference tissue models were suitable for the quantification. The whole-body distribution study showed that the main routes of excretion of 18F-LBT-999 were the urinary and gastrointestinal systems, with the bladder being the critical organ. Accumulation of 18F-LBT-999 was found in the bone and skull, with a relatively high dose estimated for the osteogenic cells. The range of calculated effective dose was 0.021-0.022 mSv/MBq. Conclusion: 18F-LBT-999 seemed to be a suitable PET radioligand for the DAT quantification, particularly for extrastriatal regions. The skull uptake did not seem to be a limitation for brain imaging. The calculated dosimetry estimates based on data in nonhuman primates seemed comparable with those of other clinically used 18F-labeled radioligands, for example, 18F-FDG (0.024-0.027 mSv/MBq). Copyright © 2011 by the Society of Nuclear Medicine, Inc.
The aim of this study was to evaluate the quantification, biodistribution, and radiation dosimetry of the novel dopamine transporter (DAT) radioligand 18F-(2S,3S)-methyl 8-((E)-4-fluorobut-2-en-1-yl)-3-(p-tolyl)-8- azabicyclo[3.2.1]octane-2-carboxylate (18F-LBT-999) in nonhuman primates. Methods: The brain study was conducted in 4 female rhesus monkeys. PET measurements were conducted for 243 min using the high-resolution research tomograph (HRRT) with the measurement of the metabolite-corrected arterial input function and protein binding. Quantification was performed with kinetic analysis using 2-tissue- and 1-tissue-compartment models, with Logan graphical analysis and with different reference tissue models. The outcome measures were total distribution volume (VT), nondisplaceable distribution volume (VND), binding potential relative to the free concentration of radioligand in plasma (BPF), and binding potential relative to the concentration of nondisplaceable radioligand in tissue (BPND) = VT - VND/VND using the cerebellum as a reference region. For the biodistribution and radiation dosimetry, 2 female cynomolgus monkeys were studied.Whole-body PET scans were obtained using a PET/CT system for approximately 250 min. Estimates of the absorbed radiation dose in humans were calculated using OLINDA/EXM software. Results: 18F-LBT-999 showed good brain uptake (300% standardized uptake value) and regional distribution according to known DAT density. The 2-tissuecompartment model was the preferred model for the quantification. Late peak equilibrium (120-140 min) and slow washout were observed in the striatum, with high variability of VT, BPF, and BPND. When the different models were compared with the 2-tissuecompartment model, the underestimation of VT or BPND was larger in the caudate and putamen than in the midbrain and thalamus. The reference tissue models were suitable for the quantification. The whole-body distribution study showed that the main routes of excretion of 18F-LBT-999 were the urinary and gastrointestinal systems, with the bladder being the critical organ. Accumulation of 18F-LBT-999 was found in the bone and skull, with a relatively high dose estimated for the osteogenic cells. The range of calculated effective dose was 0.021-0.022 mSv/MBq. Conclusion: 18F-LBT-999 seemed to be a suitable PET radioligand for the DAT quantification, particularly for extrastriatal regions. The skull uptake did not seem to be a limitation for brain imaging. The calculated dosimetry estimates based on data in nonhuman primates seemed comparable with those of other clinically used 18F-labeled radioligands, for example, 18F-FDG (0.024-0.027 mSv/MBq). Copyright © 2011 by the Society of Nuclear Medicine, Inc.
Imaging of the striatal and extrastriatal dopamine transporter with 18F-LBT-999: Quantification, biodistribution, and radiation dosimetry in nonhuman primates
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Imaging of the striatal and extrastriatal dopamine transporter with 18F-LBT-999: Quantification, biodistribution, and radiation dosimetry in nonhuman primates
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Impact Factor: 3.274
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Impact Factor: 5.774
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View Export to BibTeX Export to EndNote
Varrone A, Halldin C
Molecular imaging of the dopamine transporter (792 views)
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Impact Factor: 7.022
View Export to BibTeX Export to EndNote
Darcourt J, Booij J, Tatsch K, Varrone A, Borght TV, Kapucu OL, Nagren K, Nobili F, Walker Z, Van Laere K
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Impact Factor: 5.036
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Varrone A, Sjoholm N, Eriksson L, Gulyas B, Halldin C, Farde L
* Advancement in PET quantification using 3D-OP-OSEM point spread function reconstruction with the HRRT (1557 views) (PDF 336 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Oct; 36(10): 1639-1650.
Impact Factor: 4.531
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Varrone A, Steiger C, Schou M, Takano A, Finnema SJ, Guilloteau D, Gulyas B, Halldin C
* In vitro autoradiography and in vivo evaluation in cynomolgus monkey of [18F]FE-PE2I, a new dopamine transporter PET radioligand (1549 views)
Synapse (ISSN: 0887-4476), 2009 Oct; 63(10): 871-880.
Impact Factor: 2.557
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Varrone A, Sansone V, Pellecchia MT, Amboni M, Salvatore E, De Michele G, Filla A, Barone P, Pappata S, Salvatore M
* Comparison between a dual-head and a brain-dedicated SPECT system in the measurement of the loss of dopamine transporters with [123I]FP-CIT (630 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Jul; 35(7): 1343-1349.
Impact Factor: 4.532
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Pellecchia MT, Varrone A, Annesi G, Amboni M, Cicarelli G, Sansone V, Annesi F, Rocca FE, Vitale C, Pappata S, Quattrone A, Barone P
* Parkinsonism and essential tremor in a family with pseudo-dominant inheritance of PARK2: An FP-CIT SPECT study (724 views)
Mov Disord (ISSN: 0885-3185, 1531-8257, 0885-3185linking), 2007 Mar 15; 22(4): 559-563.
Impact Factor: 3.207
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Varrone A, Sansone V, Pellecchia MT, Amboni M, Vitale C, Salvatore E, De Michele G, Garavaglia B, Annesi G, Brice A, Pappata S, Barone P, Salvatore M
* Longitudinal changes of dopamine transporter density in early-onset parkin disease measured with [I-123]FP-CIT SPECT (468 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2006 Sep; 33: N/D-N/D.
Impact Factor: 4.041
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Salvatore E, Varrone A, Sansone V, Nolano M, Bruni AC, De Rosa A, Santoro L, Pappata S, Filla A, De Michele G
* Characterization of nigrostriatal dysfunction in spinocerebellar ataxia 17 (608 views)
Mov Disord (ISSN: 0885-3185, 1531-8257, 0885-3185linking), 2006 Jun; 21(6): 872-875.
Impact Factor: 3.323
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Sansone V, Varrone A, Pellecchia MT, Amboni M, Salvatore E, De Michele G, Filla A, Barone P, Pappata S, Salvatore M
* Comparison Of A Dual-Headed And A Brain-Dedicated SPECT Camera In The Ability To Measure The Loss Of Dopamine Transporters With [123I]FP-CIT (553 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2005 Sep; 32: N/D-N/D.
Impact Factor: 3.883
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Varrone A, Salvatore E, Sansone V, De Michele G, Filla A, Pappata S, Salvatore M
* [123I]FP-CIT SPECT Study Of The Striatal Dopamine Transporter Density In Patients With Idiopathic Late Onset Cerebellar Ataxia And MSA-C (445 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2005 Sep; 32: N/D-N/D.
Impact Factor: 3.883
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Varrone A, Pellecchia MT, Amboni M, Sansone V, Salvatore E, Ghezzi D, Garavaglia B, Brice A, Brunetti A, Bonavita V, De Michele G, Salvatore M, Pappata S, Barone P
* Imaging of dopaminergic dysfunction with [123I]FP-CIT SPECT in early-onset parkin disease (4552 views)
Neurology (ISSN: 0028-3878, 1526-632x, 1526-632xelectronic), 2004 Dec 14; 63(11): 2097-2103.
Impact Factor: 5.973
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Varrone A, Salvatore E, De Michele G, Barone P, Sansone V, Pellecchia MT, Castaldo I, Coppola G, Brunetti A, Salvatore M, Pappata S, Filla A
* Reduced Striatal [123I]FP-CIT Binding in SCA2 Patients without Parkinsonism (756 views)
Annals Of Neurology, 2004 Mar; 55(3): 426-430.
Impact Factor: 11.91
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24 Records (19 excluding Abstracts).
Total impact factor: 101.716 (82.133 excluding Abstracts).
Total 5 year impact factor: 104.062 (82.785 excluding Abstracts).
Total impact factor: 101.716 (82.133 excluding Abstracts).
Total 5 year impact factor: 104.062 (82.785 excluding Abstracts).
772 views. Last view on Saturday 26 April 2025, 14:34:30
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