Radiation dosimetry and biodistribution of the TSPO ligand 11C-DPA-713 in humans

Journal of Nuclear Medicine

Volumn 53, Issue 2, 2012, Pages 330-335

  Endres, Christopher J ^a   Coughlin, Jennifer M ^a   Gage, Kenneth L ^a   Watkins, Crystal C ^a   Kassiou, Michael ^b,c   Pomper, Martin G ^a  

^a DEPARTMENT OF PATHOLOGY   (United States)

^b UNIVERSITY OF SYDNEY   (Australia)

^c UNIVERSITY OF SYDNEY   (Australia)

Author keywords

Dosimetry; Microglia; PET CT; Radiotracer tissue kinetics; Translocator protein

Indexed keywords

DPA 713 C 11; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG;

ADULT; ARTICLE; COMPUTER ASSISTED EMISSION TOMOGRAPHY; DATA ANALYSIS SOFTWARE; DOSIMETRY; DRUG ABSORPTION; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG UPTAKE; FEMALE; HUMAN; HUMAN EXPERIMENT; ISOTOPE LABELING; KIDNEY; LUNG; MALE; MEAN RESIDENCE TIME; NORMAL HUMAN; PANCREAS; PRIORITY JOURNAL; RADIATION DOSE DISTRIBUTION; RADIOACTIVITY; SINGLE DRUG DOSE; SPLEEN; TISSUE DISTRIBUTION; WHOLE BODY RADIATION;

ACETAMIDES; ADULT; CARBON RADIOISOTOPES; FEMALE; HUMANS; INJECTIONS; LIGANDS; MALE; PYRAZOLES; PYRIMIDINES; RADIOMETRY; RECEPTORS, GABA;

EID: 84856806258     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.111.094565     Document Type: Article

References (38)

1. Papadopoulos V, Baraldi M, Guilarte TR, et al. Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function. Trends Pharmacol Sci. 2006;27:402-409. (Pubitemid 44069585)
2. Banati RB. Visualising microglial activation in vivo. Glia. 2002;40:206-217. (Pubitemid 35337378)
3. Cagnin A, Gerhard A, Banati RB. In vivo imaging of neuroinflammation. Eur Neuropsychopharmacol. 2002;12:581-586. (Pubitemid 35408707)
4. Scarf AM, Kassiou M. The translocator protein. J Nucl Med. 2011;52:677-680.
5. Weissman BA, Raveh L. Peripheral benzodiazepine receptors: on mice and human brain imaging. J Neurochem. 2003;84:432-437. (Pubitemid 36182241)
6. 11C]PK11195 challengers. Eur J Nucl Med Mol Imaging. 2008;35:2304-2319.
7. Dollé F, Luus C, Reynolds A, Kassiou M. Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Curr Med Chem. 2009;16:2899-2923.
8. Doorduin J, de Vries EF, Dierckx RA, Klein HC. PET imaging of the peripheral benzodiazepine receptor: monitoring disease progression and therapy response in neurodegenerative disorders. Curr Pharm Des. 2008;14:3297-3315.
9. Luus C, Hanani R, Reynolds A, Kassiou M. The development of PET radioligands for imaging the translocator protein (18 kDa): what have we learned? J Labelled Comp Rad. 2010;53:501-510.
10. James ML, Fulton RR, Henderson DJ, et al. Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand. Bioorg Med Chem. 2005;13:6188-6194. (Pubitemid 41400141)
11. Endres CJ, Pomper MG, James M, et al. Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans. J Nucl Med. 2009;50:1276-1282.
12. Owen DR, Gunn RN, Rabiner EA, et al. Mixed-affinity binding in humans with 18-kDa translocator protein ligands. J Nucl Med. 2011;52:24-32.
13. 3H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation. J Cereb Blood Flow Metab. 2010;30:1608-1618.
14. 11C]methyl triflate. Appl Radiat Isot. 2006;64:570-573.
15. 18F-FDG PET/CT. J Nucl Med. 2010;51:1501-1506.
16. Robb RA, Hanson DP, Karwoski RA, Larson AG, Workman EL, Stacy MC. Analyze: a comprehensive, operator-interactive software package for multidimensional medical image display and analysis. Comput Med Imaging Graph. 1989;13:433-454. (Pubitemid 20019803)
17. Stabin MG, Sparks RB, Crowe E. OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine. J Nucl Med. 2005;46:1023-1027. (Pubitemid 43733519)
18. International Commission on Radiological Protection (ICRP). Basic anatomical and physiological data for use in radiological protection reference values. ICRP publication 89. Ann ICRP. 2002;32:3-4.
19. Marine PM, Stabin MG, Fernald MJ, Brill AB. Changes in radiation dose with variations in human anatomy: larger and smaller normal-stature adults. J Nucl Med. 2010;51:806-811.
20. International Commission on Radiological Protection (ICRP). 1990 Recommendations of the International Commission on Radiological Protection. ICRP publication 60. Ann ICRP. 1991;21:1-3.
21. Anholt RR, De Souza EB, Oster-Granite ML, Snyder SH. Peripheral-type benzodiazepine receptors: autoradiographic localization in whole-body sections of neonatal rats. J Pharmacol Exp Ther. 1985;233:517-526. (Pubitemid 15122056)
22. Bribes E, Carriere D, Goubet C, Galiegue S, Casellas P, Simony-Lafontaine J. Immunohistochemical assessment of the peripheral benzodiazepine receptor in human tissues. J Histochem Cytochem. 2004;52:19-28. (Pubitemid 38032130)
23. Liu J, Matyakhina L, Han Z, et al. Molecular cloning, chromosomal localization of human peripheral-type benzodiazepine receptor and PKA regulatory subunit type 1A (PRKAR1A)-associated protein PAP7, and studies in PRKAR1A mutant cells and tissues. FASEB J. 2003;17:1189-1191.
24. Brown AK, Fujita M, Fujimura Y, et al. Radiation dosimetry and biodistribution in monkey and man of 11C-PBR28: a PET radioligand to image inflammation. J Nucl Med. 2007;48:2072-2079. (Pubitemid 350232319)
25. Fujita M, Imaizumi M, Zoghbi SS, et al. Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation. Neuroimage. 2008;40:43-52.
26. 11C-methyl- 4-piperidinyl-N-butyrate radiation dosimetry in humans by dynamic organ-specific evaluation. J Nucl Med. 2008;49:347-353.
27. 11C-(R)-PK11195, the prototypic PET ligand to image inflammation. Eur J Nucl Med Mol Imaging. 2010;37:606-612.
28. Food and Drug Administration. Radioactive Drugs for Certain Research Uses. Title 21 CFR 361.1. Washington, DC: National Archives and Records Administration; 2001.
29. International Commission on Radiological Protection (ICRP). The 2007 Recommendations of the International Commission on Radiological Protection. ICRP publication 103. Ann ICRP. 2007;37:2-4.
30. Ng HH. Intravenous Toxicity Study of DPA-713 in Sprague-Dawley Rats. Menlo Park, CA: SRI International; 2006. SRI study number M420-05.
31. 11C-NPA) determined from PET. J Nucl Med. 2009;50:814-817.
32. 11C]flumazenil (FMZ). Mol Imaging Biol. March 2, 2011 [Epub ahead of print].
33. 11C-raclopride determined from human wholebody PET. J Nucl Med. 2006;47:313-319.
34. 11C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: Implications for positron emission tomographic imaging of this inflammation biomarker. Neuroimage. 2010;49:2924-2932.
35. James ML, Fulton RR, Vercoullie J, et al. DPA-714, a new translocator proteinspecific ligand: synthesis, radiofluorination, and pharmacologic characterization. J Nucl Med. 2008;49:814-822. (Pubitemid 351717548)
36. 11C-PK11195 in a rat model of acute neuroinflammation. J Nucl Med. 2009;50:468-476.
37. 11C]-(R)-PK11195 in a rat model of herpes encephalitis. Mol Imaging Biol. 2009;11:386-398.
38. Reynolds A, Hanani R, Hibbs D, et al. Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). Bioorg Med Chem Lett. 2010;20:5799-5802.