High-affinity dopamine D2/D3 PET radioligands 18F-fallypride and 11C-FLB457: A comparison of kinetics in extrastriatal regions using a multiple-injection protocol

Journal of Cerebral Blood Flow and Metabolism

Volumn 30, Issue 5, 2010, Pages 994-1007

  Vandehey, Nicholas T ^a   Moirano, Jeffrey M ^a   Converse, Alexander K ^b   Holden, James E ^a   Mukherjee, Jogesh ^c   Murali, Dhanabalan ^b   Nickles, R Jerry ^a   Davidson, Richard J ^b   Schneider, Mary L ^d   Christian, Bradley T ^a,b  

^a UNIVERSITY OF WISCONSIN SCHOOL OF MEDICINE AND PUBLIC HEALTH   (United States)

^b UNIVERSITY OF WISCONSIN MADISON   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d UNIVERSITY OF WISCONSIN MADISON   (United States)

Author keywords

D2 D3; Dopamine; Fallypride; FLB457; Multiple injection; PET

Indexed keywords

DOPAMINE 2 RECEPTOR; DOPAMINE 3 RECEPTOR; FALLYPRIDE F 18; ISOREMOXIPRIDE; ISOREMOXIPRIDE C 11; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BRAIN CORTEX; BRAIN REGION; CEREBELLUM; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG RECEPTOR BINDING; LIGAND BINDING; MALE; MESENCEPHALON; NONHUMAN; PLASMA CLEARANCE; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RHESUS MONKEY;

ANIMALS; BENZAMIDES; BRAIN; CARBON RADIOISOTOPES; DOPAMINE ANTAGONISTS; FLUORINE RADIOISOTOPES; LIGANDS; MACACA MULATTA; POSITRON-EMISSION TOMOGRAPHY; PYRROLIDINES; RECEPTORS, DOPAMINE D2; RECEPTORS, DOPAMINE D3; SALICYLAMIDES;

EID: 77952011735     PISSN: 0271678X     EISSN: None     Source Type: Journal    
DOI: 10.1038/jcbfm.2009.270     Document Type: Article

References (39)

1. Airaksinen AJ, Finnema SJ, Nag S, Mukherjee J, Gulyas B, Halldin C (2006) A new PET radioligand 11C cyclopropyl-FLB 457 for imaging extrastriatal dopamine D2 receptors: evaluation in monkey and comparison to 11C FLB 457 and 11C fallypride. Neuroimage 31: T15-T
2. Airaksinen AJ, Nag S, Finnema SJ, Mukherjee J, Chattopadhyay S, Gulyás B, Farde L, Halldin C (2008) [11C]Cyclopropyl-FLB 457: a PET radioligand for low densities of dopamine D2 receptors. Bioorg Med Chem 16:6467-73
3. Akaike H (1974) A new look at the statistical model identification. Automatic Control, IEEE Transact Biomed Eng 19:716-23
4. Asselin MC, Montgomery AJ, Grasby PM, Hume SP (2007) Quantification of PET studies with the very high-affinity dopamine D-2/D-3 receptor ligand [C-11]FLB 457: re-evaluation of the validity of using a cerebellar reference region. J Cereb Blood Flow Metab 27:378-92
5. Christian BT, Narayanan T, Shi B, Morris ED, Mantil J, Mukherjee J (2004) Measuring the in vivo binding parameters of [18F]-fallypride in monkeys using a PET multiple-injection protocol. J Cereb Blood Flow Metab 24:309-22
6. Christian BT, Vandehey NT, Fox AS, Murali D, Oakes TR, Converse AK, Nickles RJ, Shelton SE, Davidson RJ, Kalin NH (2009) The distribution of D2/D3 receptor binding in the adolescent rhesus monkey using small animal PET imaging. Neuroimage 44:1334-44
7. Delforge J, Syrota A, Mazoyer BM (1990) Identifiability analysis and parameter-identification of an in vivo ligand-receptor model from PET data. IEEE Transact Biomed Eng 37:653-61
8. Delforge J, Bottlaender M, Loc'h C, Guenther I, Fuseau C, Bendriem B, Syrota A, Mazière B (1999) Quantitation of extrastriatal D2 receptors using a very high-affinity ligand (FLB 457) and the multi-injection approach. J Cereb Blood Flow Metab 19:533-46
9. Delforge J, Bottlaender M, Pappata S, Loc0h C, Syrota A (2001) Absolute quantification by positron emission tomography of the endogenous ligand. J Cereb Blood Flow Metab 21:613-30
10. Eckelman WC, Kilbourn MR, Mathis CA (2009) Specific to nonspecific binding in radiopharmaceutical studies: it's not so simple as it seems!. Nucl Med Biol 36:235-7
11. Halldin C, Farde L, Högberg T, Mohell N, Hall H, Suhara T, Karlsson P, Nakashima Y, Swahn CG (1995) Carbon-11-FLB 457: a radioligand for extrastriatal D2 dopamine receptors. J Nucl Med 36:1275-81
12. Holden JE, Jivan S, Ruth TJ, Doudet DJ (2002) In vivo receptor assay with multiple ligand concentrations: an equilibrium approach. J Cereb Blood Flow Metab 22:1132-41
13. Innis RB, Cunningham VJ, Delforge J, Fujita M, Gjedde A, Gunn RN, Holden J, Houle S, Huang S-C, Ichise M, Iida H, Ito H, Kimura Y, Koeppe RA, Knudsen GM, Knuuti J, Lammertsma AA, Laruelle M, Logan J, Maguire RP, Mintun MA, Morris ED, Parsey R, Price JC, Slifstein M, Sossi V, Suhara T, Votaw JR, Wong DF, Carson RE (2007) Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab 27:1533-9
14. Kahn ZU, Mrzljak L, Gutierrez A, de la Calle A, Goldman-Rakic PS (1998) Prominence of the dopamine D2 short isoform in dopaminergic pathways. Proc Natl Acad Sci USA 95:7731-6
15. Larsen P, Ulin J, Dahlstrom K, Jensen M (1997) Synthesis of [11C]iodomethane by iodination of [11C]methane. Appl Radiat Isot 48:153-7
16. Logan J, Fowler JS, Volkow ND, Ding YS, Wang G-J, Alexoff DL (2001) A strategy for removing the bias in the graphical analysis method. J Cereb Blood Flow Metab 21:307-20
17. Lundkvist C, Sandell J, Nagren K, Pike VW, Halldin C (1998) Improved syntheses of the PET radioligands, [C-11]FLB457, [C-11]MDL100907 and [C-11]beta-CIT-FE, by the use of [C-11]methyl triflate. J Labelled Compounds Radiopharm 41:545-56
18. Morris E, Yoder K (2006) Positron emission tomography displacement sensitivity: predicting binding potential change for positron emission tomography tracers based on their kinetic characteristics. J Cereb Blood Flow Metab 27:606-17
19. Morris ED, Christian BT, Yoder KK, Muzic RF (2004) Estimation of local receptor density, B'max, and other parameters via multiple-injection positron emission tomography experiments. Methods Enzymol 385:184-213
20. Mukherjee J, Yang Z-Y, Das M, Brown T (1995) Fluorinated benzamide neuroleptics-III Development of (S)-N-[(1-allyl-2-pyrrolidinyl) methyl]-5 (3-[18F]fluoropropyl) 2, 3-dimethoxybenzamide as an improved dopamine D-2 receptor tracer. Nucl Med Biol 22:283-96
21. Mukherjee J, Yang Z-Y, Brown T, Lew R, Wernick M, Ouyang X, Yasillo N, Chen C-T, Mintzer R, Cooper M (1999) Preliminary assessment of extrastriatal dopamine d-2 receptor binding in the rodent and nonhuman primate brains using the high affinity radioligand, 18F-fallypride. Nucl Med Biol 26:519-27
22. Mukherjee J, Christian BT, Narayanan TK, Shi B, Collins D (2005) Measurement of d-amphetamine-induced effects on the binding of dopamine D-2/D-3 receptor radioligand, 18F-fallypride in extrastriatal brain regions in non-human primates using PET. Brain Res 1032:77-84
23. Muzic RF, Cornelius S (2001) COMKAT: compartment model kinetic analysis tool. J Nucl Med 42:636-45
24. Muzic RF, Christian BC (2006) Evaluation of objective functions for estimation of kinetic parameters. Med Phys 33:342-53
25. Narendran R, Frankle WG, Mason NS, Rabiner EA, Gunn RN, Searle GE, Vora S, Litschge M, Kendro S, Cooper TB, Mathis CA, Laruelle M (2009) Positron emission tomography imaging of amphetamine-induced dopamine release in the human cortex: a comparative evaluation of the high affinity dopamine D2/3 radiotracers [11C]FLB 457 and [11C]fallypride. Synapse 63:447-61
26. Okauchi T, Suhara T, Maeda J, Kawabe K, Obayashi S, Suzuki K (2001) Effect of endogenous dopamine on endogenous dopamine on extrastriated [(11) C]FLB 457 binding measured by PET. Synapse 41:87-95
27. Olsson H, Halldin C, Swahn CG, Farde L (1999) Quantification of [11C]FLB 457 binding to extrastriatal dopamine receptors in the human brain. J Cereb Blood Flow Metab 19:1164-73
28. Olsson H, Farde L (2001) Potentials and pitfalls using high affinity radioligands in PET and SPET determinations on regional drug induced D2 receptor occupancy-a simulation study based on experimental data. Neuroimage 14:936-45
29. Olsson H, Halldin C, Farde L (2004) Differentiation of extrastriatal dopamine D2 receptor density and affinity in the human brain using PET. Neuroimage 22:794-803
30. Riccardi P, Baldwin R, Salomon R, Anderson S, Ansari MS, Li R, Dawant B, Bauernfeind A, Schmidt D, Kessler R (2008) Estimation of baseline dopamine D2 receptor occupancy in striatum and extrastriatal regions in humans with positron emission tomography with [18F] fallypride. Biol Psychiatry 63:241-4
31. Salinas C, Muzic JRF, Ernsberger P, Saidel GM (2007) Robust experiment design for estimating myocardial beta adrenergic receptor concentration using PET. Med Phys 34:151-65
32. Schmidt DE, Votaw JR, Kessler RM, Depaulis T (1994) Aromatic and amine substituent effects on the apparent lipophilicities of N-(2-pyrrolidinyl) methyl-substituted benzamides. J Pharm Sci 83:305-15
33. Slifstein M, Hwang D-R, Huang Y, Guo N, Sudo Y, Narendran R, Talbot P, Laruelle M (2004 a) In vivo affinity of [18F]fallypride for striatal and extrastriatal dopamine D 2 receptors in nonhuman primates. Psychopharmacology 175:274-86
34. Slifstein M, Narendran R, Hwang DR, Sudo Y, Talbot PS, Huang Y, Laruelle M (2004 b) Effect of amphetamine on [(18) F]fallypride in vivo binding to D (2) receptors in striatal and extrastriatal regions of the primate brain: single bolus and bolus plus constant infusion studies. Synapse 54:46-63
35. Smith SM, Jenkinson M, Woolrich MW, Beckmann CF, Behrens TE, Johansen-Berg H, Bannister PR, De Luca M, Drobnjak I, Flitney DE, Niazy RK, Saunders J, Vickers J, Zhang Y, De Stefano N, Brady JM, Matthews PM (2004) Advances in functional and structural MR image analysis and implementation as FSL. Neuroimage 23 (Suppl 1) : S208-19
36. Suhara T, Sudo Y, Okauchi T, Maeda J, Kawabe K, Suzuki K, Okubo Y, Nakashima Y, Ito H, Tanada S, Halldin C, Farde L (1999) Extrastriatal dopamine D2 receptor density and affinity in the human brain measured by 3D PET. Int J Neuropsychopharmacol 2:73-82
37. Stark D, Piel M, Hubner H, Gmeiner P, Grunder G, Rosch F (2007) In vitro affinities of various halogenated benzamide derivatives as potential radioligands for noninvasive quantification of D-2-like dopamine receptors. Bioorg Med Chem 15:6819-29
38. Tai YC, Chatziioannou A, Siegel S, Young J, Newport D, Goble RN, Nutt RE, Cherry SR (2001) Performance evaluation of the microPET P4: a PET system dedicated to animal imaging. Phys Med Biol 46:1845-62 (Pubitemid 32677543)
39. Tetko IV, Tanchuk VY (2005) ALOGPS (http://www.vcclab.org) is a free online program to predict lipophilicity and aqueous solubility of chemical compounds. Proceedings of the 229th National Meeting of the American Chemical Society, San Diego, CA, 13-17 March 2005