In vivo assessment and dosimetry of 2 novel PDE10A PET radiotracers in humans: 18F-MNI-659 and 18F-MNI-654

Journal of Nuclear Medicine

Volumn 55, Issue 8, 2014, Pages 1297-1304

  Barret, Olivier ^a   Thomae, David ^a   Tavares, Adriana ^a   Alagille, David ^a   Papin, Caroline ^a   Waterhouse, Rikki ^b   McCarthy, Timothy ^b   Jennings, Danna ^a   Marek, Ken ^a   Russell, David ^a   Seibyl, John ^a   Tamagnan, Gilles ^a  

^a Molecular Neuroimaging   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Dosimetry; Kinetic modeling; PDE10A; PET imaging; Test retest

Indexed keywords

2 (2 (3 (1 (2 FLUOROETHYL) 1H INDAZOL 6 YL) 7 METHYL 4 OXO 3,4 DIHYDROQUINAZOLIN 2 YL)ETHYL) 4 ISOPROPOXYISOINDOLINE 1,3 DIONE; 2 [2 [3 (4 (2 FLUOROETHOXY)PHENYL) 7 METHYL 4 OXO 3,4 DIHYDROQUINAZOLIN 2 YL]ETHYL] 4 ISOPROPOXYISOINDOLINE 1,3 DIONE; PHOSPHODIESTERASE; PHOSPHODIESTERASE 10A; RADIOLIGAND; TRACER; UNCLASSIFIED DRUG; 2-(2-(3-(1-(2-FLUOROETHYL)-1H-INDAZOL-6-YL)-7-METHYL-4-OXO-3,4-DIHYDROQUINAZOLIN-2-YL)ETHYL)-4-ISOPROPOXYISOINDOLINE-1,3-DIONE; 2-(2-(3-(4-(2-FLUOROETHOXY)PHENYL)-7-METHYL-4-OXO-3,4-DIHYDROQUINAZOLIN-2-YL)ETHYL)-4-ISOPROPOXYISOINDOLINE-1,3-DIONE; INDOLE DERIVATIVE; PDE10A PROTEIN, HUMAN; PHTHALIMIDE DERIVATIVE; QUINAZOLINONE DERIVATIVE;

ADULT; ARTICLE; BRAIN REGION; CAUDATE NUCLEUS; CEREBELLUM; CEREBELLUM CORTEX; CONTROLLED STUDY; CORRELATION COEFFICIENT; DOSIMETRY; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; HUMAN TISSUE; IMAGE ANALYSIS; IN VIVO STUDY; MALE; NEUROIMAGING; NON INVASIVE PROCEDURE; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PUTAMEN; RADIATION DOSE DISTRIBUTION; STRUCTURE ANALYSIS; TEST RETEST RELIABILITY; WHOLE BODY PET; ANIMAL; BIOLOGICAL MODEL; BRAIN; DIAGNOSTIC USE; IMAGE PROCESSING; KINETICS; METABOLISM; PROCEDURES; RADIOMETRY; RAT; SCINTISCANNING; WHOLE BODY IMAGING;

ADULT; ANIMALS; BRAIN; FEMALE; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; INDOLES; KINETICS; MALE; MODELS, BIOLOGICAL; PHOSPHORIC DIESTER HYDROLASES; PHTHALIMIDES; POSITRON-EMISSION TOMOGRAPHY; QUINAZOLINONES; RADIOACTIVE TRACERS; RADIOMETRY; RATS; WHOLE BODY IMAGING;

EID: 84905449923     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.113.122895     Document Type: Article

References (40)

1. Reneerkens OA, Rutten K, Steinbusch HW, Blokland A, Prickaerts J. Selective phosphodiesterase inhibitors: a promising target for cognition enhancement. Psychopharmacology (Berl). 2009;202:419-443.
2. Conti M, Beavo J. Biochemistry and physiology of cyclic nucleotide phosphodiesterases: essential components in cyclic nucleotide signaling. Annu Rev Biochem. 2007;76:481-511.
3. Francis SH, Blount MA, Corbin JD. Mammalian cyclic nucleotide phosphodiesterases: molecular mechanisms and physiological functions. Physiol Rev. 2011;91:651-690.
4. Menniti FS, Faraci WS, Schmidt CJ. Phosphodiesterases in the CNS: targets for drug development. Nat Rev Drug Discov. 2006;5:660-670.
5. Xie Z, Adamowicz WO, Eldred WD, et al. Cellular and subcellular localization of PDE10A, a striatum-enriched phosphodiesterase. Neuroscience. 2006;139:597-607.
6. Lakics V, Karran EH, Boess FG. Quantitative comparison of phosphodiesterase mRNA distribution in human brain and peripheral tissues. Neuropharmacology. 2010;59:367-374.
7. Fujishige K, Kotera J, Michibata H, et al. Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A). J Biol Chem. 1999;274:18438-18445.
8. Siuciak JA, McCarthy SA, Chapin DS, et al. Genetic deletion of the striatumenriched phosphodiesterase PDE10A: evidence for altered striatal function. Neuropharmacology. 2006;51:374-385.
9. Hebb AL, Robertson HA. Role of phosphodiesterases in neurological and psychiatric disease. Curr Opin Pharmacol. 2007;7:86-92.
10. Giorgi M, Melchiorri G, Nuccetelli V, et al. PDE10A and PDE10A-dependent cAMP catabolism are dysregulated oppositely in striatum and nucleus accumbens after lesion of midbrain dopamine neurons in rat: a key step in parkinsonism physiopathology. Neurobiol Dis. 2011;43:293-303.
11. Kleiman RJ, Kimmel LH, Bove SE, et al. Chronic suppression of phosphodiesterase 10A alters striatal expression of genes responsible for neurotransmitter synthesis, neurotransmission, and signaling pathways implicated in Huntington's disease. J Pharmacol Exp Ther. 2011;336:64-76.
12. Rising AC, Xu J, Carlson A, Napoli VV, Denovan-Wright EM, Mandel RJ. Longitudinal behavioral, cross-sectional transcriptional and histopathological characterization of a knock-in mouse model of Huntington's disease with 140 CAG repeats. Exp Neurol. 2011;228:173-182.
13. Grauer SM, Pulito VL, Navarra RL, et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther. 2009;331:574-590.
14. Strick CA, James LC, Fox CB, Seeger TF, Menniti FS, Schmidt CJ. Alterations in gene regulation following inhibition of the striatum-enriched phosphodiesterase, PDE10A. Neuropharmacology. 2010;58:444-451.
15. Rutten K, Van Donkelaar EL, Ferrington L, et al. Phosphodiesterase inhibitors enhance object memory independent of cerebral blood flow and glucose utilization in rats. Neuropsychopharmacology. 2009;34:1914-1925.
16. Piccart E, Gantois I, Laeremans A, et al. Impaired appetitively as well as aversively motivated behaviors and learning in PDE10A-deficient mice suggest a role for striatal signaling in evaluative salience attribution. Neurobiol Learn Mem. 2011;95:260-269.
17. Bahn A, Hagos Y, Reuter S, et al. Identification of a new urate and high affinity nicotinate transporter, hOAT10 (SLC22A13). J Biol Chem. 2008;283:16332-16341.
18. Threlfell S, Sammut S, Menniti FS, Schmidt CJ, West AR. Inhibition of phosphodiesterase 10A increases the responsiveness of striatal projection neurons to cortical stimulation. J Pharmacol Exp Ther. 2009;328:785-795.
19. 11C]MP-10 as a positron emission tomography radioligand for phosphodiesterase 10A. Nucl Med Biol. 2011;38:875-884.
20. 18F-JNJ42259152, a radioligand for phosphodiesterase 10A imaging. Eur J Nucl Med Mol Imaging. 2013;40:254-261.
21. Hu E, Ma J, Biorn C, et al. Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer. J Med Chem. 2012;55:4776-4787.
22. Tu Z, Xu J, Jones LA, Li S, Mach RH. Carbon-11 labeled papaverine as a PET tracer for imaging PDE10A: radiosynthesis, in vitro and in vivo evaluation. Nucl Med Biol. 2010;37:509-516.
23. 18FJNJ41510417 as a radioligand for PET imaging of phosphodiesterase-10A in the brain. J Nucl Med. 2010;51:1584-1591.
24. 11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain. Bioorg Med Chem. 2011;19:1666-1673.
25. 18F-JNJ-42259152, a novel phosphodiesterase 10A PET tracer: kinetic modeling and test-retest study in human brain. J Nucl Med. 2013;54:1285-1293.
26. 18F]MNI-659 [abstract]. J Nucl Med. 2012;53(suppl 1):110P.
27. Slifstein M, Laruelle M. Models and methods for derivation of in vivo neuroreceptor parameters with PET and SPECT reversible radiotracers. Nucl Med Biol. 2001;28:595-608.
28. Logan J. A review of graphical methods for tracer studies and strategies to reduce bias. Nucl Med Biol. 2003;30:833-844.
29. Innis RB, Cunningham VJ, Delforge J, et al. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab. 2007;27:1533-1539.
30. Lammertsma AA, Hume SP. Simplified reference tissue model for PET receptor studies. Neuroimage. 1996;4:153-158.
31. Akaike H. A new look at the statistical model identification. IEEE Trans Automat Contr. 1974;19:716-723.
32. 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.
33. Carson RE. Parameter estimation in positron emission tomography. In: Phelps ME, Mazziotta JC, Schelbert HR, eds. Positron Emission Tomography and Autoradiography: Principles and Applications for the Brain and Heart. New York, NY: Raven Press; 1986:347-390.
34. International Commission on Radiological Protection (ICRP). 1990 recommendations of the International Commission on Radiological Protection. ICRP publication 60. Annals of the ICRP. 1991;21.
35. International Commission on Radiological Protection (ICRP). Limits for intakes of radionuclides by workers. ICRP publication 30 (Part 1). Annals of the ICRP. 1979;2.
36. Cunningham VJ, Jones T. Spectral analysis of dynamic PET studies. J Cereb Blood Flow Metab. 1993;13:15-23.
37. 11C]FLB 457: re-evaluation of the validity of using a cerebellar reference region. J Cereb Blood Flow Metab. 2007;27:378-392.
38. 11C] GSK931145, a PET ligand for the glycine transporter type 1. Synapse. 2011;65:1319-1332.
39. 11C]-DASB as an example. J Cereb Blood Flow Metab. 2012;32:70-80.
40. Wu Y, Carson RE. Noise reduction in the simplified reference tissue model for neuroreceptor functional imaging. J Cereb Blood Flow Metab. 2002;22:1440-1452.