[18F]DPA-714: Direct Comparison with [11C]PK11195 in a Model of Cerebral Ischemia in Rats

PLoS ONE

Volumn 8, Issue 2, 2013, Pages

  Boutin, Hervé ^a,b   Prenant, Christian ^b   Maroy, Renaud ^c   Galea, James ^b,d   Greenhalgh, Andrew D ^b,h   Smigova, Alison ^b   Cawthorne, Christopher ^b   Julyan, Peter ^e   Wilkinson, Shane M ^f   Banister, Samuel D ^f   Brown, Gavin ^b   Herholz, Karl ^b   Kassiou, Michael ^f,g   Rothwell, Nancy J ^b  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b UNIVERSITY OF MANCHESTER   (United Kingdom)

^c SERVICE HOSPITALIER FRÉDÉRIC JOLIOT   (France)

^d SALFORD ROYAL NHS FOUNDATION TRUST   (United Kingdom)

^e CHRISTIE HOSPITAL   (United Kingdom)

^f UNIVERSITY OF SYDNEY   (Australia)

^g UNIVERSITY OF SYDNEY   (Australia)

^h RESEARCH INSTITUTE OF THE MCGILL UNIVERSITY HEALTH CENTRE   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

DPA 714 F 18; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE C 11; TRACER; UNCLASSIFIED DRUG; CARBON; CD11B ANTIGEN; DIAGNOSTIC AGENT; FLUORINE; GLIAL FIBRILLARY ACIDIC PROTEIN; ISOQUINOLINE DERIVATIVE; MICROTUBULE ASSOCIATED PROTEIN; MTAP2 PROTEIN, RAT; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; N,N DIETHYL 2 (2 (4 (2 FLUOROETHOXY)PHENYL) 5,7 DIMETHYLPYRAZOLO(1,5 A)PYRIMIDIN 3 YL)ACETAMIDE; N,N-DIETHYL-2-(2-(4-(2-FLUOROETHOXY)PHENYL)-5,7-DIMETHYLPYRAZOLO(1,5-A)PYRIMIDIN-3-YL)ACETAMIDE; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRAIN ISCHEMIA; CONTROLLED STUDY; DISEASE SEVERITY; DRUG UPTAKE; EX VIVO STUDY; IN VIVO STUDY; MALE; MIDDLE CEREBRAL ARTERY OCCLUSION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RAT; SIGNAL NOISE RATIO; ANIMAL; BRAIN; COMPARATIVE STUDY; DISEASE MODEL; IMMUNOHISTOCHEMISTRY; METABOLISM; METHODOLOGY; MICROGLIA; PATHOLOGY; REPRODUCIBILITY; SCINTISCANNING; SPRAGUE DAWLEY RAT;

ANIMALS; ANTIGENS, CD11B; BRAIN; BRAIN ISCHEMIA; CARBON RADIOISOTOPES; DISEASE MODELS, ANIMAL; FLUORINE RADIOISOTOPES; GLIAL FIBRILLARY ACIDIC PROTEIN; IMMUNOHISTOCHEMISTRY; ISOQUINOLINES; MALE; MICROGLIA; MICROTUBULE-ASSOCIATED PROTEINS; POSITRON-EMISSION TOMOGRAPHY; PYRAZOLES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; REPRODUCIBILITY OF RESULTS; SIGNAL-TO-NOISE RATIO;

EID: 84873901664     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0056441     Document Type: Article

References (50)

1. Lucas SM, Rothwell NJ, Gibson RM, (2006) The role of inflammation in CNS injury and disease. Br J Pharmacol 147 Suppl 1 S232-40: S232-S240.
2. Shaftel SS, Griffin WS, O'Banion MK, (2008) The role of interleukin-1 in neuroinflammation and Alzheimer disease: an evolving perspective. J Neuroinflammation 5: 1742-2094.
3. Mrak RE, Griffin WS, (2001) Interleukin-1, neuroinflammation, and Alzheimer's disease. Neurobiol Aging 22: 903-908.
4. Glass CK, Saijo K, Winner B, Marchetto MC, Gage FH, (2010) Mechanisms underlying inflammation in neurodegeneration. Cell 140: 918-934.
5. Welsh P, Lowe GD, Chalmers J, Campbell DJ, Rumley A, et al. (2008) Associations of proinflammatory cytokines with the risk of recurrent stroke. Stroke 39: 2226-2230.
6. Touzani O, Boutin H, Chuquet J, Rothwell N, (1999) Potential mechanisms of interleukin-1 involvement in cerebral ischaemia. J Neuroimmunol 100: 203-215.
7. Benavides J, Quarteronet D, Imbault F, Malgouris C, Uzan A, et al. (1983) Labelling of "peripheral-type" benzodiazepine binding sites in the rat brain by using [3H]PK 11195, an isoquinoline carboxamide derivative: kinetic studies and autoradiographic localization. J Neurochem 41: 1744-1750.
8. Benavides J, Guilloux F, Rufat P, Uzan A, Renault C, et al. (1984) In vivo labelling in several rat tissues of 'peripheral type' benzodiazepine binding sites. Eur J Pharmacol 99: 1-7.
9. Le Fur G, Vaucher N, Perrier ML, Flamier A, Benavides J, et al. (1983) Differentiation between two ligands for peripheral benzodiazepine binding sites, [3H]RO5-4864 and [3H]PK 11195, by thermodynamic studies. Life Sci 33: 449-457.
10. Papadopoulos V, Baraldi M, Guilarte TR, Knudsen TB, Lacapere JJ, et al. (2006) Translocator protein (18 kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function. Trends Pharmacol Sci 27: 402-409.
11. Camsonne R, Crouzel C, Comar D, Maziere M, Prenant C, et al. (1984) Synthesis of N-(11-C) Methyl, N-(Methyl-1 Propyl), (Chloro-2 Phenyl)-1 Isoquinoleine Carboxamide-3 (PK 11195): A new ligand for peripheral benzodiazepine receptors. J Labelled Comp Radiopharm 21: 985-991.
12. Junck L, Olson JM, Ciliax BJ, Koeppe RA, Watkins GL, et al. (1989) PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site. Ann Neurol 26: 752-758.
13. Pappata S, Cornu P, Samson Y, Prenant C, Benavides J, et al. (1991) PET study of carbon-11-PK 11195 binding to peripheral type benzodiazepine sites in glioblastoma: a case report. J Nucl Med 32: 1608-1610.
14. Groom GN, Junck L, Foster NL, Frey KA, Kuhl DE, (1995) PET of peripheral benzodiazepine binding sites in the microgliosis of Alzheimer's disease. J Nucl Med 36: 2207-2210.
15. Gildersleeve DL, Van Dort ME, Johnson JW, Sherman PS, Wieland DM, (1996) Synthesis and evaluation of [123I]-iodo-PK11195 for mapping peripheral-type benzodiazepine receptors (omega 3) in heart. Nucl Med Biol 23: 23-28.
16. Kropholler MA, Boellaard R, Schuitemaker A, Folkersma H, van Berckel BN, et al. (2006) Evaluation of reference tissue models for the analysis of [11C](R)-PK11195 studies. J Cereb Blood Flow Metab 26: 1431-1441.
17. Kropholler MA, Boellaard R, van Berckel BN, Schuitemaker A, Kloet RW, et al. (2007) Evaluation of reference regions for (R)-[(11)C]PK11195 studies in Alzheimer's disease and mild cognitive impairment. J Cereb Blood Flow Metab 27: 1965-1974.
18. Lammertsma AA, Hume SP, (1996) Simplified reference tissue model for PET receptor studies. Neuroimage 4: 153-158.
19. Chauveau F, Boutin H, Van CN, Dolle F, Tavitian B, (2008) Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers. Eur J Nucl Med Mol Imaging 35: 2304-2319.
20. Dolle F, Luus C, Reynolds A, Kassiou M, (2009) Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Curr Med Chem 16: 2899-2923.
21. Luus C, Hanani R, Reynolds A, Kassiou M, (2010) The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned? Journal of Labelled Compounds & Radiopharmaceuticals 53: 501-510.
22. Owen DR, Howell OW, Tang SP, Wells LA, Bennacef I, et al. (2010) Two binding sites for [(3)H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation. J Cereb Blood Flow Metab.
23. Owen DR, Gunn RN, Rabiner EA, Bennacef I, Fujita M, et al. (2011) Mixed-affinity binding in humans with 18-kDa translocator protein ligands. J Nucl Med 52: 24-32.
24. Chauveau F, Van Camp N, Dolle F, Kuhnast B, Hinnen F, et al. (2009) Comparative Evaluation of the Translocator Protein Radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a Rat Model of Acute Neuroinflammation. J Nucl Med 50: 468-476.
25. Martin A, Boisgard R, Theze B, Van CN, Kuhnast B, et al. (2010) Evaluation of the PBR/TSPO radioligand [(18)F]DPA-714 in a rat model of focal cerebral ischemia. J Cereb Blood Flow Metab 30: 230-241.
26. Rojas S, Martin A, Arranz MJ, Pareto D, Purroy J, et al. (2007) Imaging brain inflammation with [(11)C]PK11195 by PET and induction of the peripheral-type benzodiazepine receptor after transient focal ischemia in rats. J Cereb Blood Flow Metab 27: 1975-1986.
27. Doorduin J, Klein HC, Dierckx RA, James M, Kassiou M, et al. (2009) [(11)C]-DPA-713 and [(18)F]-DPA-714 as New PET Tracers for TSPO: A Comparison with [(11)C]-(R)-PK11195 in a Rat Model of Herpes Encephalitis. Mol Imaging Biol 11: 386-398.
28. Benavides J, Capdeville C, Dauphin F, Dubois A, Duverger D, et al. (1990) The quantification of brain lesions with an ω3 site ligand: a critical analysis of animal models of cerebral ischaemia and neurodegeneration. Brain Res 522: 275-289.
29. Gerhard A, Schwarz J, Myers R, Wise R, Banati RB, (2005) Evolution of microglial activation in patients after ischemic stroke: a [11C](R)-PK11195 PET study. Neuroimage 24: 591-595.
30. Imaizumi M, Kim HJ, Zoghbi SS, Briard E, Hong J, et al. (2006) PET imaging with [(11)C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat. Neurosci Lett 411: 200-205.
31. Pappata S, Levasseur M, Gunn RN, Myers R, Crouzel C, et al. (2000) Thalamic microglial activation in ischemic stroke detected in vivo by PET and [11C]PK11195. Neurology 55: 1052-1054.
32. Sette G, Baron JC, Young AR, Miyazawa H, Tillet I, et al. (1993) In vivo mapping of brain benzodiazepine receptor changes by positron emission tomography after focal ischemia in the anesthetized baboon. Stroke 24: 2046-2057.
33. Longa EZ, Weinstein PR, Carlson S, Cummins R, (1989) Reversible middle cerebral artery occlusion without craniectomy in rats. Stroke 20: 84-91.
34. James ML, Fulton RR, Vercoullie J, Henderson DJ, Garreau L, et al. (2008) DPA-714, a new translocator protein-specific ligand: synthesis, radiofluorination, and pharmacologic characterization. J Nucl Med 49: 814-822.
35. Cremer JE, Hume SP, Cullen BM, Myers R, Manjil LG, et al. (1992) The distribution of radioactivity in brains of rats given [N-methyl-11C]PK 11195 in vivo after induction of a cortical ischaemic lesion. Int J Rad Appl Instrum B 19: 159-166.
36. Hastings DL, Reader AJ, Julyan PJ, Zweit J, Jeavons AP, et al. (2007) Performance characteristics of a small animal PET camera for molecular imaging. Nuclear Instruments and Methods in Physics Research Section A: Accelerators, Spectrometers, Detectors and Associated Equipment 573: 80-83.
37. Cawthorne C, Prenant C, Smigova A, Julyan P, Maroy R, et al. (2011) Biodistribution, pharmacokinetics and metabolism of interleukin-1 receptor antagonist (IL-1RA) using [(18) F]-IL1RA and PET imaging in rats. Br J Pharmacol 162: 659-672.
38. Reader AJ, Ally S, Bakatselos F, Manavaki R, Walledge RJ, et al. (2002) One-pass list-mode EM algorithm for high-resolution 3-D PET image reconstruction into large arrays. IEEE Trans Nucl Sci 49: 693-699.
39. Maroy R, Boisgard R, Comtat C, Frouin V, Cathier P, et al. (2008) Segmentation of rodent whole-body dynamic PET images: an unsupervised method based on voxel dynamics. IEEE Trans Med Imaging 27: 342-354.
40. Maroy R, Boisgard R, Comtat C, Jego B, Fontyn Y, et al. (2010) Quantitative organ time activity curve extraction from rodent PET images without anatomical prior. Med Phys 37: 1507-1517.
41. Schwarz AJ, Danckaert A, Reese T, Gozzi A, Paxinos G, et al. (2006) A stereotaxic MRI template set for the rat brain with tissue class distribution maps and co-registered anatomical atlas: application to pharmacological MRI. Neuroimage 32: 538-550.
42. Oliff HS, Weber E, Eilon G, Mark P, (1995) The role of strain/vendor differences on the outcome of focal ischemia induced by intraluminal middle cerebral artery occlusion in the rat. Brain Res 675: 20-26.
43. Aspey BS, Taylor FL, Terruli M, Harrison MJ, (2000) Temporary middle cerebral artery occlusion in the rat: consistent protocol for a model of stroke and reperfusion. Neuropathol Appl Neurobiol 26: 232-242.
44. Boutin H, Chauveau F, Thominiaux C, Gregoire MC, James ML, et al. (2007) 11C-DPA-713: a novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. J Nucl Med 48: 573-581.
45. Kropholler MA, Boellaard R, Schuitemaker A, van Berckel BN, Luurtsema G, et al. (2005) Development of a tracer kinetic plasma input model for (R)-[11C]PK11195 brain studies. J Cereb Blood Flow Metab 25: 842-851.
46. Schuitemaker A, van Berckel BN, Kropholler MA, Veltman DJ, Scheltens P, et al. (2007) SPM analysis of parametric (R)-[11C]PK11195 binding images: plasma input versus reference tissue parametric methods. Neuroimage 35: 1473-1479.
47. Schuitemaker A, van Berckel BN, Kropholler MA, Kloet RW, Jonker C, et al. (2007) Evaluation of methods for generating parametric (R-[11C]PK11195 binding images. J Cereb Blood Flow Metab 27: 1603-1615.
48. Thominiaux C, Damont A, Kuhnast B, Demphel S, Le Helleix S, et al. (2010) Radiosynthesis of 7-chloro-N,N-dimethyl-5-[11C]methyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, [11C]SSR180575, a novel radioligand for imaging the TSPO (peripheral benzodiazepine receptor) with PET. J Labelled Comp Radiopharm 53: 767-773.
49. Chauveau F, Boutin H, Van CN, Thominiaux C, Hantraye P, et al. (2011) In vivo imaging of neuroinflammation in the rodent brain with [11C]SSR180575, a novel indoleacetamide radioligand of the translocator protein (18 kDa). Eur J Nucl Med Mol Imaging 38: 509-514.
50. Damont A, Boisgard R, Kuhnast B, Lemee F, Raggiri G, et al. (2011) Synthesis of 6-[(18)F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET. Bioorg Med Chem Lett 21: 4819-4822.