Nuclear Medicine and Biology
Volume 35, Issue 3 , Pages 335-341 , April 2008

Validation of the reference tissue model for estimation of dopaminergic D2-like receptor binding with [18F](N-methyl)benperidol in humans

  • Jo Ann V. Antenor-Dorsey

      Affiliations

    • Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, MO, USA
  • ,
  • Joanne Markham

      Affiliations

    • Department of Radiology, Washington University School of Medicine, St. Louis, MO, USA
  • ,
  • Stephen M. Moerlein

      Affiliations

    • Department of Radiology, Washington University School of Medicine, St. Louis, MO, USA
  • ,
  • Tom O. Videen

      Affiliations

    • Department of Radiology, Washington University School of Medicine, St. Louis, MO, USA
    • Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA
  • ,
  • Joel S. Perlmutter

      Affiliations

    • Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, MO, USA
    • Department of Radiology, Washington University School of Medicine, St. Louis, MO, USA
    • Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA
    • Program in Physical Therapy, Washington University School of Medicine, St. Louis, MO, USA
    • Corresponding Author InformationCorresponding author. Campus Box 8225, St. Louis, MO 63110, USA. Tel.: +1 314 362 6026; fax: +1 314 362 0168.

Received 29 July 2007 ,Revised 20 November 2007 ,Accepted 23 December 2007.

References 

  1. Reisine TD, Fields JZ, Stern LZ, Johnson PC, Bird ED, Yamamura HI. Alterations in dopaminergic receptors in Huntington's disease. Life Sci. 1977;21:1123–1128
  2. Lee T, Seeman P, Rajput A, Farley IJ, Hornykiewicz O. Receptor basis for dopaminergic supersensitivity in Parkinson's disease. Nature. 1978;273:59–61
  3. Strange PG. Dopamine receptors in the basal ganglia: relevance to Parkinson's disease. Mov Disord. 1993;8:263–270
  4. Burt DR, Creese I, Snyder SH. Antischizophrenic drugs: chronic treatment elevates dopamine receptor binding in brain. Science. 1977;196:326–328
  5. Owen F, Cross AJ, Crow TJ, Longden A, Poulter M, Riley GJ. Increased dopamine-receptor sensitivity in schizophrenia. Lancet. 1978;2:223–226
  6. Lee T, Seeman P, Tourtellotte WW, Farley IJ, Hornykeiwicz O. Binding of 3H-neuroleptics and 3H-apomorphine in schizophrenic brains. Nature. 1978;274:897–900
  7. Perlmutter JS, Stambuk MK, Markham J, Black KJ, McGee-Minnich L, Jankovic J, et al. Decreased [18F]spiperone binding in putamen in idiopathic focal dystonia. J Neurosci. 1997;17:843–850
  8. Reisine TD, Fields JZ, Yamamura HI. Neurotransmitter receptor alterations in Parkinson's disease. Life Sci. 1977;21:335–343
  9. In:  Baron JC,  Comar D,  Farde L,  Martinot JL,  Mazoyer B editor. Brain dopaminergic systems: imaging with positron emission tomography. Boston: Kluwer Academic Publishers, Boston Academic Publishers; 1991;p. 5–38
  10. Frost JJ, Smith AC, Kuhar MJ, Dannals RF, Wagner HN. In vivo binding of 3H-N-methylspiperone to dopamine and serotonin receptors. Life Sci. 1987;40:987–995
  11. Coenen HH, Wienhard K, Stocklin G, Laufer P, Hebold I, Pawlik G, et al. PET measurement of D2 and S2 receptor binding of 3-N-[(2′-18F]fluoroethyl)spiperone in baboon brain. Eur J Nucl Med. 1988;14:80–87
  12. Perlmutter JS, Moerlein SM, Huang DR, Todd R. Non-steady state measurement of in vivo radioligand binding with positron emission tomography: comparison with in vitro binding. J Neurosci. 1991;11:1381–1389
  13. Seeman P, Guan HC, Niznik HB. Endogenous dopamine lowers the dopamine D2 receptor density as measured by [3H]raclopride: implications for positron emission tomography of the human brain. Synapse. 1989;3:96–97
  14. Dewey SL, Smith GS, Logan J, Brodie JD, Fowler JS, Wolf AP. Striatal binding of the PET ligand 11C-raclopride is altered by drugs that modify synaptic dopamine levels. Synapse. 1993;13:350–356
  15. Riccardi P, Li R, Ansari MS, Zald D, Park S, Dawant B, et al. Amphetamine-induced displacement of [18F] fallypride in striatum and extrastriatal regions in humans. Neuropsychopharmacology. 2006;31:1016–1026
  16. In:  Reynolds JEF editors. Martindale the extra pharmacopeia. 30th ed. London: The Pharmaceutical Press; 1993;p. 567
  17. Peroutka SJ, Synder SH. Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency. Am J Psychiatry. 1980;137:1518–1522
  18. Arnett CD, Wolf AP, Shiue CY, Fowler JS, MacGregor RR, Christman DR, et al. Improved delineation of human dopamine receptors using [18F]-N-methylspiroperidol and PET. J Nucl Med. 1986;27:1878–1882
  19. Moerlein SM, Laufer P, Stocklin G, Pawlik G, Wienhard K, Heiss WD. Evaluation of 75Br-labelled butyrophenone neuroleptics for imaging cerebral dopaminergic receptor areas using positron emission tomography. Eur J Nucl Med. 1986;12:211–216
  20. Suehiro M, Dannals RF, Scheffel U, Stathis M, Wilson AA, Ravert HT, et al. In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol. J Nucl Med. 1990;31:2015–2021
  21. Moerlein SM, Perlmutter JS. Specific binding of 3N-(2′-[18F]fluoroethyl)benperidol to primate cerebral dopaminergic D2 receptors demonstrated in vivo by PET. Neurosci Lett. 1992;148:97–100
  22. Moerlein SM, Perlmutter JS, Welch MJ. Specific, reversible binding of [18F]benperidol to baboon D2 receptors: PET evaluation of an improved 18F-labeled ligand. Nucl Med Biol. 1995;22:809–815
  23. Moerlein SM, Perlmutter JS, Markham J, Welch MJ. In vivo kinetics of [18F](N-methyl)benperidol: a novel PET tracer for assessment of dopaminergic D2-like receptor binding. J Cereb Blood Flow Metab. 1997;17:833–845
  24. Logan J, Fowler JS, Volkow ND, Wolf AP, Dewey SL, Schlyer DJ, et al. Graphical analysis of reversible radioligand binding from time–activity measurements applied to [N-11C-methyl]-(−)-cocaine PET studies in human subjects. J Cereb Blood Flow Metab. 1990;10:740–747
  25. Logan J, Fowler JS, Volkow ND, Wang GJ, Ding YS, Alexoff DL. Distribution volume ratios without blood sampling from graphical analysis of PET data. J Cereb Blood Flow Metab. 1996;16:834–840
  26. Logan J. Graphical analysis of PET data applied to reversible and irreversible tracers. Nucl Med Biol. 2000;27:661–670
  27. Moerlein SM, Banks WR, Parkinson D. Production of fluorine-18 labeled (3-N-methyl)benperidol for PET investigation of cerebral dopaminergic receptor binding. Appl Radiat Isot. 1992;43:913–917
  28. Welch MJ, Kilbourn MR. A remote system for the routine production of oxygen-15 radiopharmaceuticals. J Lab Comp Radiopharm. 1985;22:1193–1200
  29. Mazoyer B, Trebossen R, Deutch R, Casey M, Blohm K. Physical characteristics of the ECAT 953B/31: a new high resolution brain positron tomograph. IEEE Trans Med Imaging. 1991;10:499–504
  30. Spinks TJ, Jones T, Bailey DL, Townsend DW, Grootoonk S, Bloomfield PM, et al. Physical performance of a positron tomograph for brain imaging with retractable septa. Phys Med Biol. 1992;37:1637–1655
  31. Ollinger JM. Model-based scatter correction for fully 3D PET. Phys Med Biol. 1996;41:153–176
  32. Martin WR, Powers WJ, Raichle ME. Cerebral blood volume measured with inhaled C15O and positron emission tomography. J Cereb Blood Flow Metab. 1987;7:421–426
  33. Raichle M, Martin W, Herscovitch P, Mintun M, Markham J. Brain blood flow measured with intravenous H215O. II. Implementation and validation. J Nucl Med. 1983;24:790–798
  34. Videen TO, Perlmutter JS, Herscovitch P, Raichle ME. Brain blood volume, flow and oxygen utilization measured with O-15 radiotracers and positron emission tomography: revised metabolic computations. J Cereb Blood Flow Metab. 1987;7:513–516
  35. Woods RP, Cherry SR, Mazziota JC. Rapid automated algorithm for aligning and reslicing PET images. J Comput Assist Tomogr. 1992;16:620–633
  36. Andersson JL. How to obtain high-accuracy image registration: application to movement correction of dynamic positron emission tomography data. Eur J Nucl Med. 1998;25:575–586
  37. Woods RP, Mazziotta JC, Cherry SR. MRI-PET registration with automated algorithm. J Comput Assist Tomogr. 1993;14:536–546
  38. Mintun MA, Raichle ME, Kilbourn MR, Wooten GF, Welch MJ. A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann Neurol. 1984;15:217–227
  39. Perlmutter JS, Larson KB, Raichle ME, Markham J, Mintun MA, Kilbourn MR, et al. Strategies for in vivo measurement of receptor binding using positron emission tomography. J Cereb Blood Flow Metab. 1986;6:154–169
  40. Parsey RV, Slifstein M, Hwang DR, Abi-Dargham A, Simpson N, Mawlawi O, et al. Validation and reproducibility of measurement of 5-HT1A receptor parameters with [carbonyl-11C]WAY-100635 in humans: comparison of arterial and reference tissue input functions. J Cereb Blood Flow Metab. 2000;20:1111–1133
  41. Hwang DR, Narendran R, Huang Y, Slifstein M, Talbot PS, Sudo Y, et al. Quantitative analysis of (−)-N-(11)C-propyl-norapomorphine in vivo binding in nonhuman primates. J Nucl Med. 2004;45:338–346
  42. Siessmeier T, Zhou Y, Buchholz HG, Landvogt C, Vernaleken I, Piel M, et al. Parametric mapping of binding in human brain of D2 receptor ligands of different affinities. J Nucl Med. 2005;46:964–972
  43. Varga J, Szabo Z. Modified regression model for the Logan plot. J Cereb Blood Flow Metab. 2002;22:240–244
  44. Ghaemi M, Hiker R, Rudolf J, Sobesky J, Heiss W-D. Differentiating multiple system atrophy from Parkinson's disease: contribution of striatal and midbrain MRI volumetry and multi-tracer PET imaging. J Neuro Neurosurg Psych. 2002;73:517–523
  45. Thobois S, Fraix V, Savasta M, Costes N, Pollak P, et al. Chronic subthalamic nucleus stimulation and striatal D2 dopamine receptors in Parkinson's disease. A [11C]-raclopride PET study. J Neurol. 2003;250:1219–1223
  46. Schreckenberger M, Hagele S, Siessmeier T, Buchholz HG, Armbrust-Henrich H, et al. The dopamine D2 receptor ligand 18F-desmethoxyfallypride: an appropriate fluorinated PET tracer for the differential diagnosis of parkinsonism. Eur J Nucl Med Mol Imaging. 2004;31:1128–1135
  47. Kaasinen V, Ruottinen HM, Nagren K, Lehikoinen P, Oikonen V, et al. Upregulation of putaminal dopamine D2 receptors in early Parkinson's disease: a Comparative PET study with [11C]raclopride and [11C]N-methylspiperone. J Nucl Med. 2000;41:65–70
  48. Lammertsma AA, Hume SP. Simplified reference tissue model for PET receptor studies. Neuroimage. 1996;4:153–158
  49. Ichise M, Toyama H, Innis RB, Carson RE. Strategies to improve neuroreceptor parameter estimation by linear regression analysis. J Cereb Blood Flow Metab. 2002;22:1271–1281
  50. Sossi V, Holden JE, Chan G, Krzywinski M, Stoessl AJ, Ruth TJ. Analysis of four dopaminergic tracers kinetics using two different tissue input function methods. J Cereb Blood Flow Metab. 2000;20:653–660
  51. Suzuki A, Tashiro M, Kimura Y, Mochizuki H, Ishii K, Watabe H, et al. Use of reference tissue models for quantification of histamine H1 receptors in human brain by using positron emission tomography and [11c]doxepin. Ann Nucl Med. 2005;19:425–433
  52. Moerlein SM, Perlmutter JS, Cutler PD, Welch MJ. Radiation dosimetry of [18F](N-methyl) benperidol as determined by whole-body PET imaging of primates. Nucl Med Biol. 1997;24:311–318

 Supported by NINDS Grants NS41509, NS50425 and NS31001; Greater St. Louis Chapter of the American Parkinson Disease Association (APDA); APDA Advanced Research Center at Washington University; Barnes Jewish Hospital Foundation (Jack Buck Fund for PD research and Elliot H. Stein Family Fund); and the Murphy Fund and the Kopolow Fund.

PII: S0969-8051(08)00002-4

doi: 10.1016/j.nucmedbio.2007.12.004

Nuclear Medicine and Biology
Volume 35, Issue 3 , Pages 335-341 , April 2008