Simplified quantification of 5-HT2A receptors in the human brain with [11C]MDL 100,907 PET and non-invasive kinetic analyses

NeuroImage

Volumn 50, Issue 3, 2010, Pages 984-993

  Meyer, Philipp T ^a   Bhagwagar, Zubin ^b   Cowen, Philip J ^c   Cunningham, Vincent J ^d   Grasby, Paul M ^e   Hinz, Rainer ^f  

^a UNIVERSITY OF FREIBURG   (Germany)

^b YALE UNIVERSITY   (United States)

^c UNIVERSITY OF OXFORD   (United Kingdom)

^d GLAXOSMITHKLINE   (United Kingdom)

^e MEDICAL RESEARCH COUNCIL   (United Kingdom)

^f UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

5 HT2A receptor; 11C MDL 100,907; Positron emission tomography; Reference region; Tracer kinetic modelling

Indexed keywords

CARBON 11; MIRTAZAPINE; SEROTONIN 2A RECEPTOR; VOLINANSERIN;

ADULT; AMYGDALOID NUCLEUS; ARTICLE; BINDING KINETICS; CINGULATE GYRUS; COMPARTMENT MODEL; CONTROLLED STUDY; FEMALE; FRONTAL LOBE; HIPPOCAMPUS; HUMAN; IMAGE ANALYSIS; INSULA; MALE; NON INVASIVE MEASUREMENT; OCCIPITAL LOBE; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PUTAMEN; RECEPTOR OCCUPANCY; TEMPORAL LOBE; THALAMUS; VOLUNTEER;

ADULT; BRAIN; BRAIN MAPPING; CARBON RADIOISOTOPES; FEMALE; FLUOROBENZENES; HUMANS; KINETICS; LINEAR MODELS; MALE; MIANSERIN; MIDDLE AGED; MODELS, NEUROLOGICAL; PIPERIDINES; POSITRON-EMISSION TOMOGRAPHY; RECEPTOR, SEROTONIN, 5-HT2A; SEROTONIN AGENTS; SIGNAL PROCESSING, COMPUTER-ASSISTED;

EID: 77549087680     PISSN: 10538119     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuroimage.2010.01.037     Document Type: Article

References (48)

1. Anttila S.A., and Leinonen E.V. A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 7 (2001) 249-264
2. Bhagwagar Z., Hinz R., Taylor M., Fancy S., Cowen P., and Grasby P. Increased 5-HT(2A) receptor binding in euthymic, medication-free patients recovered from depression: a positron emission study with [(11)C]MDL 100,907. Am. J. Psychiatry 163 (2006) 1580-1587
3. Biver F., Goldman S., Luxen A., Monclus M., Forestini M., Mendlewicz J., and Lotstra F. Multicompartmental study of fluorine-18 altanserin binding to brain 5HT2 receptors in humans using positron emission tomography. Eur. J. Nucl. Med. 21 (1994) 937-946
4. Blin J., Pappata S., Kiyosawa M., Crouzel C., and Baron J.C. [18F]setoperone: a new high-affinity ligand for positron emission tomography study of the serotonin-2 receptors in baboon brain in vivo. Eur. J. Pharmacol. 147 (1988) 73-82
5. Carson R.E., Channing M.A., Blasberg R.G., Dunn B.B., Cohen R.M., Rice K.C., and Herscovitch P. Comparison of bolus and infusion methods for receptor quantitation: application to [18F]cyclofoxy and positron emission tomography. J. Cereb. Blood Flow. Metab. 13 (1993) 24-42
6. Cselényi Z., Olsson H., Farde L., and Gulyás B. Wavelet-aided parametric mapping of cerebral dopamine D2 receptors using the high affinity PET radioligand [11C]FLB 457. Neuroimage 17 (2002) 47-60
7. Farde L., Hall H., Ehrin E., and Sedvall G. Quantitative analysis of D2 dopamine receptor binding in the living human brain by PET. Science 231 (1986) 258-261
8. Gunn R.N., Sargent P.A., Bench C.J., Rabiner E.A., Osman S., Pike V.W., Hume S.P., Grasby P.M., and Lammertsma A.A. Tracer kinetic modeling of the 5-HT1A receptor ligand [carbonyl-11C]WAY-100635 for PET. Neuroimage 8 (1988) 426-440
9. Hall H., Farde L., Halldin C., Lundkvist C., and Sedvall G. Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907. Synapse 38 (2000) 421-431
10. Hammers A., Koepp M.J., Free S.L., Brett M., Richardson M.P., Labbé C., Cunningham V.J., Brooks D.J., and Duncan J. Implementation and application of a brain template for multiple volumes of interest. Hum. Brain Mapp. 15 (2002) 165-174
11. Hinz R., Bhagwagar Z., Cowen P.J., Cunningham V.J., and Grasby P.M. Validation of a tracer kinetic model for the quantification of 5-HT(2A) receptors in human brain with [(11)C]MDL 100,907. J. Cereb. Blood Flow. Metab. 27 (2007) 161-172
12. Hirani E., Sharp T., Sprakes M., Grasby P., and Hume S. Fenfluramine evokes 5-HT2A receptor-mediated responses but does not displace [11C]MDL 100907: small animal PET and gene expression studies. Synapse 50 (2003) 251-260
13. Holden J.E., Sossi V., Chan G., Doudet D.J., Stoessl A.J., and Ruth T.J. Effect of population k2 values in graphical estimation of DV ratios of reversible ligands. In: Gjedde A., Hansen S.B., Knudsen G.M., and Paulson O.B. (Eds). Physiological imaging of the brain with PET (2001), Academic Press, Inc., San Diego 127-129
14. Ichise M., Toyama H., Innis R.B., and Carson R.E. Strategies to improve neuroreceptor parameter estimation by linear regression analysis. J. Cereb. Blood Flow. Metab. 22 (2002) 1271-1281
15. Ichise M., Liow J.S., Lu J.Q., Takano A., Model K., Toyama H., Suhara T., Suzuki K., Innis R.B., and Carson R.E. Linearized reference tissue parametric imaging methods: application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brain. J. Cereb. Blood Flow. Metab. 23 (2003) 1096-1112
16. Innis R.B., Cunningham V.J., Delforge J., Fujita M., Gjedde A., Gunn R.N., Holden J., Houle S., Huang S.C., Ichise M., Iida H., Ito H., Kimura Y., Koeppe R.A., Knudsen G.M., Knuuti J., Lammertsma A.A., Laruelle M., Logan J., Maguire R.P., Mintun M.A., Morris E.D., Parsey R., Price J.C., Slifstein M., Sossi V., Suhara T., Votaw J.R., Wong D.F., and Carson R.E. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J. Cereb. Blood Flow. Metab. 27 (2007) 1533-1539
17. Ito H., Nyberg S., Halldin C., Lundkvist C., and Farde L. PET imaging of central 5-HT2A receptors with carbon-11-MDL 100,907. J. Nucl. Med. 39 (1998) 208-214
18. Jones B.J., and Blackburn T.P. The medical benefit of 5-HT research. Pharmacol. Biochem. Behav. 71 (2002) 555-568
19. Kakiuchi T., Nishiyama S., Sato K., Ohba H., Nakanishi S., and Tsukada H. Age-related reduction of [11C]MDL100,907 binding to central 5-HT(2A) receptors: PET study in the conscious monkey brain. Brain Res. 883 (2000) 135-142
20. Kinahan P.E., and Rogers J.G. Analytic 3D image reconstruction using all detected events. IEEE Trans. Nucl. Sci. 36 (1998) 964-968
21. Koeppe R.A., Holthoff V.A., Frey K.A., Kilbourn M.R., and Kuhl D.E. Compartmental analysis of [11C]flumazenil kinetics for the estimation of ligand transport rate and receptor distribution using positron emission tomography. J. Cereb. Blood Flow. Metab. 11 (1991) 735-744
22. Lammertsma A.A., and Hume S.P. Simplified reference tissue model for PET receptor studies. Neuroimage 4 (1996) 153-158
23. Landolt H.P., and Wehrle R. Antagonism of serotonergic 5-HT2A/2C receptors: mutual improvement of sleep, cognition and mood. Eur. J. Neurosci. 29 (2009) 1795-1809
24. Leysen J.E. 5-HT2 receptors. Curr. Drug. Targets CNS Neurol. Disord. 3 (2004) 11-26
25. Logan J., Fowler J.S., Volkow N.D., Wolf A.P., Dewey S.L., Schlyer D.J., MacGregor R.R., Hitzemann R., Bendriem B., Gatley S.J., and Christman D.R. 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. 10 (1990) 740-747
26. Logan J., Fowler J.S., Volkow N.D., Wang G.J., Ding Y.S., and Alexoff D.L. Distribution volume ratios without blood sampling from graphical analysis of PET data. J. Cereb. Blood Flow. Metab. 16 (1996) 834-840
27. Logan J., Fowler J.S., Volkow N.D., Ding Y.S., Wang G.J., and Alexoff D.L. A strategy for removing the bias in the graphical analysis method. J. Cereb. Blood Flow. Metab. 21 (2001) 307-320
28. Lundkvist C., Halldin C., Ginovart N., Nyberg S., Swahn C.G., Carr A.A., Brunner F., and Farde L. [11C]MDL 100907, a radioligand for selective imaging of 5-HT(2A) receptors with positron emission tomography. Life Sci. 58 (1996) 187-192
29. Lyon R.A., Titeler M., Frost J.J., Whitehouse P.J., Wong D.F., Wagner Jr. H.N., Dannals R.F., Links J.M., and Kuhar M.J. 3H-3-N-methylspiperone labels D2 dopamine receptors in basal ganglia and S2 serotonin receptors in cerebral cortex. J. Neurosci. 6 (1986) 2941-2949
30. Meyer P.T., Elmenhorst D., Matusch A., Winz O., Zilles K., and Bauer A. 18F-CPFPX PET: on the generation of parametric images and the effect of scan duration. J. Nucl. Med. 47 (2006) 200-207
31. Meyer P.T., Sattler B., Winz O.H., Fundke R., Oehlwein C., Kendziorra K., Hesse S., Schaefer W.M., and Sabri O. Kinetic analyses of [123I]IBZM SPECT for quantification of striatal dopamine D2 receptor binding: a critical evaluation of the single-scan approach. Neuroimage 15 (2008) 548-558
32. Parsey R.V., Ogden R.T., and Mann J.J. Determination of volume of distribution using likelihood estimation in graphical analysis: elimination of estimation bias. J. Cereb. Blood Flow. Metab. 23 (2003) 1471-1478
33. Perani D., Garibotto V., Gorini A., Moresco R.M., Henin M., Panzacchi A., Matarrese M., Carpinelli A., Bellodi L., and Fazio F. In vivo PET study of 5HT(2A) serotonin and D(2) dopamine dysfunction in drug-naive obsessive-compulsive disorder. Neuroimage 42 (2008) 306-314
34. Pinborg L.H., Adams K.H., Svarer C., Holm S., Hasselbalch S.G., Haugbøl S., Madsen J., and Knudsen G.M. Quantification of 5-HT2A receptors in the human brain using [18F]altanserin-PET and the bolus/infusion approach. J. Cereb. Blood Flow. Metab. 23 (2003) 985-996
35. Ranicar A.S., Williams C.W., Schnorr L., Clark J.C., Rhodes C.G., Bloomfield P.M., and Jones T. The on-line monitoring of continuously withdrawn arterial blood during PET studies using a single BGO/photomultiplier assembly and non-stick tubing. Med. Prog. Technol. 17 (1991) 259-264
36. Slifstein M., and Laruelle M. Effects of statistical noise on graphic analysis of PET neuroreceptor studies. J. Nucl. Med. 41 (2000) 2083-2088
37. Slifstein M., Parsey R.V., and Laruelle M. Derivation of [11C]WAY-100635 binding parameters with reference tissue models: effect of violations of model assumptions. Nucl. Med. Biol. 27 (2000) 487-492
38. Spinks T.J., Jones T., Bloomfield P.M., Bailey D.L., Miller M., Hogg D., Jones W.F., Vaigneur K., Reed J., Young J., Newport D., Moyers C., Casey M.E., and Nutt R. Physical characteristics of the ECAT EXACT3D positron tomograph. Phys. Med. Biol. 45 (2000) 2601-2618
39. Talvik-Lotfi M., Nyberg S., Nordström A.L., Ito H., Halldin C., Brunner F., and Farde L. High 5HT2A receptor occupancy in M100907-treated schizophrenic patients. Psychopharmacology (Berl) 148 (2000) 400-403
40. Timmer C.J., Sitsen J.M., and Delbressine L.P. Clinical pharmacokinetics of mirtazapine. Clin. Pharmacokinet. 38 (2000) 461-474
41. Tomasi G., Edison P., Bertoldo A., Roncaroli F., Singh P., Gerhard A., Cobelli C., Brooks D.J., and Turkheimer F.E. Novel reference region model reveals increased microglial and reduced vascular binding of 11C-(R)-PK11195 in patients with Alzheimer's disease. J. Nucl. Med. 49 (2008) 1249-1256
42. Turkheimer F.E., Hinz R., Gunn R.N., Aston J.A., Gunn S.R., and Cunningham V.J. Rank-shaping regularization of exponential spectral analysis for application to functional parametric mapping. Phys. Med. Biol. 48 (2003) 3819-3841
43. Varga J., and Szabo Z. Modified regression model for the Logan plot. J. Cereb. Blood Flow. Metab. 22 (2002) 240-244
44. Watabe H., Channing M.A., Der M.G., Adams H.R., Jagoda E., Herscovitch P., Eckelman W.C., and Carson R.E. Kinetic analysis of the 5-HT2A ligand [11C]MDL 100,907. J. Cereb. Blood Flow. Metab. 20 (2000) 899-909
45. Watabe H., Carson R.E., and Iida H. The reference tissue model: three compartments for the reference region. Neuroimage 11 (2000) S12
46. Wong D.F., Wagner Jr. H.N., Dannals R.F., Links J.M., Frost J.J., Ravert H.T., Wilson A.A., Rosenbaum A.E., Gjedde A., Douglass K.H., Petronis J.D., Folstein M.F., Toung J.K.T., Burns H.D., and Kuhar M.J. Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain. Science 226 (1984) 1393-1396
47. Wu Y., and Carson R.E. Noise reduction in the simplified reference tissue model for neuroreceptor functional imaging. J. Cereb. Blood Flow. Metab. 22 (2002) 1440-1452
48. Zhou Y., Ye W., Brasić J.R., Crabb A.H., Hilton J., and Wong D.F. A consistent and efficient graphical analysis method to improve the quantification of reversible tracer binding in radioligand receptor dynamic PET studies. Neuroimage 44 (2009) 661-670