Characterization of [11C]RO5013853, a novel PET tracer for the glycine transporter type 1 (GlyT1) in humans

NeuroImage

Volumn 75, Issue , 2013, Pages 282-290

  Wong, Dean F ^a,b,c   Ostrowitzki, Susanne ^d   Zhou, Yun ^a   Raymont, Vanessa ^a   Hofmann, Carsten ^d   Borroni, Edilio ^d   Kumar, Anil ^a   Parkar, Nikhat ^d   Brašić, James R ^a   Hilton, John ^a   Dannals, Robert F ^a   Martin Facklam, Meret ^d  

^a JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b The Johns Hopkins University   (United States)

^c UNIVERSITY OF COPENHAGEN   (Denmark)

^d F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Glycine reuptake inhibitor (GRI); Glycine transporter type 1 (GlyT1); N methyl d aspartate (NMDA); Positron emission tomography (PET); Radioligand assays; Receptors; Schizophrenia

Indexed keywords

BITOPERTIN; CARBON [(5 METHANESULFONYL 2 2,2,2 TRIFLUORO 1 METHYLETHOXY)PHENYL] [5 (TETRAHYDROPYRAN 4 YL) 1,3 DIHYDROISOINDOL 2 YL]METHANONE C 11; GLYCINE TRANSPORTER 1; TRACER; UNCLASSIFIED DRUG; (4 (3 FLUORO 5 TRIFLUOROMETHYLPYRIDIN 2 YL)PIPERAZIN 1 YL)(5 METHANESULFONYL 2 (2,2,2 TRIFLUORO 1 METHYLETHOXY)PHENYL)METHANONE; (4-(3-FLUORO-5-TRIFLUOROMETHYLPYRIDIN-2-YL)PIPERAZIN-1-YL)(5-METHANESULFONYL-2-(2,2,2-TRIFLUORO-1-METHYLETHOXY)PHENYL)METHANONE; CARBON; DIAGNOSTIC AGENT; GLYCINE TRANSPORTER; PIPERAZINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT; SLC6A9 PROTEIN, HUMAN; SULFONE;

ADULT; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CEREBELLUM; CONTROLLED STUDY; DOSIMETRY; FEMALE; HUMAN; HUMAN EXPERIMENT; HUMAN TISSUE; MALE; MOUSE; NONHUMAN; NORMAL HUMAN; PONS; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PUTAMEN; RADIATION ABSORPTION; RADIATION HAZARD; RADIOASSAY; THALAMUS; WHOLE BODY RADIATION; BRAIN; CLINICAL TRIAL; METABOLISM; METHODOLOGY; REPRODUCIBILITY; SCINTISCANNING; TISSUE DISTRIBUTION; DIAGNOSTIC USE; PROCEDURES;

BRAIN; CARBON RADIOISOTOPES; GLYCINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MALE; PIPERAZINES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; REPRODUCIBILITY OF RESULTS; SULFONES; TISSUE DISTRIBUTION;

EID: 84876455629     PISSN: 10538119     EISSN: 10959572     Source Type: Journal    
DOI: 10.1016/j.neuroimage.2011.11.052     Document Type: Article

References (55)

1. Akaike H. An information criteria (AIC). Math. Sci. 1976, 14:5-9.
2. Alberati D., Moreau J.-L., Mory R., Pinard E., Wettstein J.G. Pharmacological evaluation of a novel assay for detecting glycine transporter 1 inhibitors and their antipsychotic potential. Pharmacol. Biochem. Behav. 2010, 97:185-191.
3. 11C]R05013853 as a novel radiotracer for imaging of the glycine transporter type 1 by positron emission tomography. NeuroImage 2013, 75:291-300. (this issue).
4. Bullich S., Slifstein M., Passchier J., Murthy N.V., Kegeles L.S., Kim J.H., Xu X., Gunn R.N., Herance R., Gispert J.D., Gutierrez A., Farre M., Laruelle M., Catafau A.M. Biodistribution and radiation dosimetry of the glycine transporter-1 ligand 11C-GSK931145 determined from primate and human whole-body PET. Mol. Imaging Biol. 2010, (Aug 21. [Epub ahead of print]).
5. Carson R.E., Channing M.A., Blasberg R.G., Dunn B.B., Cohen R.M., Rice K.C., Herscovitch P. Comparison of bolus and infusion methods for receptor quantitation: application to [18F]cyclofoxy and positron emission tomography. J. Cereb. Blood Flow Metab. 1993, 13:24-42.
6. 11C raclopride binding with continuous infusion. J. Cereb. Blood Flow Metab. 1997, 17:437-447.
7. Cubelos B., Gimenez C., Zafra F. Localization of the GLYT1 glycine transporter at glutamatergic synapses in the rat brain. Cereb. Cortex 2005, 15:448-459.
8. Cunningham V.J., Matthews J.C., Gunn R.N., Rabiner E.A., Gee A.D. Identification and interpretation of microparameters in neuroreceptor compartmental models. Neuroimage 2004, 22:T13-T14.
9. Food and Drug Administration Guidance for Industry, Investigators, and Reviewers: Exploratory IND Studies 2006, (Last accessed: 21st June, 2011). http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM078933.pdf.
10. Friston K. Statistical parametric mapping 2 2002, (Last accessed: 21st June, 2011). http://www.fil.ion.ucl.ac.uk/spm/software/spm2/.
11. Frost J.J., Wagner H.N., Dannals R.F., Ravert H.T., Links J.M., Wilson A.A., Burns H.D., Wong D.F., McPherson R.W., Rosenbaum A.E. Imaging opiate receptors in the human brain by positron tomography. J. Comput. Assist. Tomogr. 1985, 9:231-236.
12. Gjedde A. High- and low-affinity transport of D-Glucose from blood to brain. J. Neurochem. 1981, 36:1463-1471.
13. Gunn R.N., Gunn S.R., Cunningham V.J. Positron emission tomography compartmental models. J. Cereb. Blood Flow Metab. 2001, 21:635-652.
14. Gunn R.N., Murthy V., Catafau A.M., Searle G., Bullich S., Slifstein M., Ouellet D., Zamuner S., Herance R., Salinas C., Pardo-Lozano R., Rabiner E.A., Farre M., Laruelle M. Translational characterization of [(11) C]GSK931145, a PET ligand for the glycine transporter type 1 (GlyT-1). Synapse 2011, 65:1319-1332. (Electronic publication ahead of print 2011 Aug 12).
15. Hamill T.G., Eng W., Jennings A., Lewis R., Thomas S., Wood S., Street L., Wisnoski D., Wolkenberg S., Lindsley C., Sanabria-Bohorquez S.M., Patel S., Riffel K., Ryan C., Cook J., Sur C., Burns H.D., Hargreaves R. The synthesis and preclinical evaluation in rhesus monkey of [(1)F]MK-6577 and [(1)(1)C]CMPyPB glycine transporter 1 positron emission tomography radiotracers. Synapse 2011, 65:261-270.
16. Harrison P.J., Weinberger D.R. Schizophrenia genes, gene expression, and neuropathology: on the matter of their convergence. Mol. Psychiatry 2005, 10:40-68.
17. Hashimoto K. Glycine transporter-1: a new potential therapeutic target for schizophrenia. Curr. Pharm. Des. 2011, 17:112-120.
18. Hilton J., Yokoi F., Dannals R.F., Ravert H.T., Szabo Z., Wong D.F. Column-switching HPLC for the analysis of plasma in PET imaging studies. Nucl. Med. Biol. 2000, 27:627-630.
19. Horti A.G., Fan H., Kuwabara H., Hilton J., Ravert H.T., Holt D.P., Alexander M., Kumar A., Rahmim A., Scheffel U., Wong D.F., Dannals R.F. 11C-JHU75528: a radiotracer for PET imaging of CB1 cannabinoid receptors. J. Nucl. Med. 2006, 47:1689-1696.
20. Huang S.C., Barrio J.R., Phelps M.E. Neuroreceptor assay with positron emission tomography: equilibrium versus dynamic approaches. J. Cereb. Blood Flow Metab. 1986, 6:515-521.
21. 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., Carson R.E. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J. Cereb. Blood Flow Metab. 2007, 27:1533-1539.
22. Koeppe R.A., Holthoff V.A., Frey K.A., Kilbourn M.R., 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. 1991, 11:735-744.
23. Krystal J.H., Karper L.P., Seibyl J.P., Freeman G.K., Delaney R., Bremner J.D., Heninger G.R., Bowers M.B., Charney D.S. Subanesthetic effects of the noncompetitive NMDA antagonist, ketamine, in humans. Psychotomimetic, perceptual, cognitive, and neuroendocrine responses. Arch. Gen. Psychiatry 1994, 51:199-214.
24. Lammertsma A.A., Hume S.P. Simplified reference tissue model for PET receptor studies. Neuroimage 1996, 4:153-158.
25. Millan M.J. N-methyl-D-aspartate receptors as a target for improved antipsychotic agents: novel insights and clinical perspectives. Psychopharmacology 2005, 179:30-53.
26. Murthy N.V., Passchier J., Gunn R.N., Searle G.E., Bullich S., Suarez M., Herance R., Farre M., Herdon H., Porter R., Sutherland S., Fagg R., Neve M., Slifstein M., Laruelle M., Catafaui A.M. [11C]GSK931145: a new pet ligand for glycine transporter 1. Neuroimage 2008, 41:T21.
27. Passchier J., Gentile G., Porter R., Herdon H., Salinas C., Jakobsen S., Audrain H., Laruelle M., Gunn R.N. Identification and evaluation of [11C]GSK931145 as a novel ligand for imaging the type 1 glycine transporter with positron emission tomography. Synapse 2010, 64:542-549.
28. Patlak C.S., Blasberg R.G., Fenstermacher J.D. Graphical evaluation of blood-to-brain transfer constants from multiple-time uptake data. J. Cereb. Blood Flow Metab. 1983, 3:1-7.
29. Patlak C.S., Blasberg R.G. Graphical evaluation of blood-to-brain transfer constants from multiple-time uptake data. Generalizations. J. Cereb. Blood Flow Metab. 1985, 5:584-590.
30. Pinard E., Alanine A., Alberati D., Bender M., Borroni E., Bourdeaux P., Brom V., Burner S., Fischer H., Hainzl D., Halm R., Hauser N., Jolidon S., Lengyel J., Marty H.P., Meyer T., Moreau J.L., Mory R., Narquizian R., Nettekoven M., Norcross R.D., Puellmann B., Schmid P., Schmitt S., Stalder H., Wermuth R., Wettstein J.G., Zimmerli D. Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-(( S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia. J. Med. Chem. 2010, 53:4603-4614.
31. Pinard E., Burner S., Cueni P., Hartung T., Norcross R.D., Schmid P., Waldmeier P., Zielinski G., Ravert H.T., Holt D.P., Dannals R.F. Radiosynthesis of [5-[11C]methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[5-(tetrahydro-pyran-4-yl)-1,3-dihydro-isoindol-2-yl]-methanone ([11C]RO5013853), a novel PET tracer for the glycine transporter type I (GlyT1). J. Labeled Comp. Rad. 2011, 54:702-707.
32. Rahmim A., Lenox M., Reader A.J., Michel C., Burbar Z., Ruth T.J., Sossi V. Statistical list-mode image reconstruction for the high resolution research tomograph. Phys. Med. Biol. 2004, 49:4239-4258.
33. Sanabria-Bohorquez S., Van Laere K., Hamill T., Koole M., Bormans G., De Lepeleire I., Reynders T., Pickett C., Van Hecken A., Burns D. Evaluation of the novel glycine transporter 1 (GlyT1) tracer [18F]CFpyPB: Dosimetry and brain quantification in human. J. Nucl. Med. 2009, 50:S1211.
34. Sanger D.J. The search for novel antipsychotics: pharmacological and molecular targets. Expert Opin. Ther. Targets 2004, 8:631-641.
35. Schmidt K.C., Turkheimer F.E. Kinetic modeling in positron emission tomography. Q. J. Nucl. Med. 2002, 46:70-85.
36. Stabin M.G., Siegel J.A. Physical models and dose factors for use in internal dose assessment. Health Phys. 2003, 85:294-310.
37. Stabin M.G., Sparks R.B., Crowe E. OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine. J. Nucl. Med. 2005, 46:1023-1027.
38. Stone J.M. Imaging the glutamate system in humans: relevance to drug discovery for schizophrenia. Curr. Pharm. Des. 2009, 15:2594-2602.
39. Szabo Z., Kao P.F., Scheffel U., Suehiro M., Mathews W.B., Ravert H.T., Musachio J.L., Marenco S., Kim S.E., Ricaurte G.A. Positron emission tomography imaging of serotonin transporters in the human brain using [11C](+)McN5652. Synapse 1995, 20:37-43.
40. Toyohara J., Ishiwata K., Sakata M., Wu J., Nishiyama S., Tsukada H., Hashimoto K. In vivo evaluation of carbon-11-labelled non-sarcosine-based glycine transporter 1 inhibitors in mice and conscious monkeys. Nucl. Med. Biol. 2011, 38:517-527.
41. Turkheimer F.E., Hinz R., Cunningham V.J. On the undecidability among kinetic models: from model selection to model averaging. J. Cereb. Blood Flow Metab. 2003, 23:490-498.
42. Umbricht D., Yoo K., Youssef E., Dorflinger E., Martin-Facklam M., Bausch A., Arrowsmith R., Alberati D., Marder S., Santarelli L. Glycine transporter type 1 (GLYT1) inhibitor RG1678: positive results of the proof-of-concept study for the treatment of negative symptoms in schizophrenia. Neuropsychopharmacology 2010, 35:S320-S321.
43. Umbricht D., Martin-Facklam M., Pizzagalli E., Youssef K., Yoo K., Dorflinger E., Bausch A., Arrowsmith R., Alberati D., Santarelli L. Glycine transporter type 1 (GlyT1) inhibitor RG1678: results of the proof-of-concept study for the treatment of negative symptoms in schizophrenia. Schizophr. Bull. 2011, 37:S324.
44. Wagner H.N., Burns H.D., Dannals R.F., Wong D.F., Langstrom B., Duelfer T., Frost J.J., Ravert H.T., Links J.M., Rosenbloom S.B., Lukas S.E., Kramer A.V., Kuhar M.J. Imaging dopamine receptors in the human brain by positron tomography. Science 1983, 221:1264-1266.
45. Wilcox K.M., Zhou Y., Wong D.F., Alexander M., Rahmim A., Hilton J., Weed M.R. Blood levels and DA transporter occupancy of orally administered methylphenidate in juvenile rhesus monkeys measured by high resolution PET. Synapse 2008, 62:950-952.
46. Williams D.L., Jennings A., Lewis R., Street L., Paten S., Wisnoski D.D., Wolkenberg S.E., Lindsey C.W., Zhao Z., Krause S.M., Ryan C., Michener M.S., Zeng Z., Miller P.A., Riffel K., O'Malley S.S., Sanabria S., Eng W., Gibson R.E., Sur C., Cook J.J., Hargreaves R., Burns D., Hamill T.G. A novel glycine transporter-1 PET tracer: from discovery to clinic. Abstr. Neurosci. 2008, 885:15.
47. Wong D.F., Wagner 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. Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain. Science 1984, 226:1393-1396.
48. Wong D.F., Yung B., Dannals R.F., Shaya E.K., Ravert H.T., Chen C.A., Chan B., Folio T., Scheffel U., Ricaurte G.A. In vivo imaging of baboon and human dopamine transporters by positron emission tomography using [11C]WIN 35,428. Synapse 1993, 15:130-142.
49. Wong D.F., Kuwabara H., Horti A.G., Raymont V., Brasic J., Guevara M., Ye W., Dannals R.F., Ravert H.T., Nandi A., Rahmim A., Ming J.E., Grachev I., Roy C., Cascella N. Quantification of cerebral cannabinoid receptors subtype 1 (CB1) in healthy subjects and schizophrenia by the novel PET radioligand [11C]OMAR. Neuroimage 2010, 52:1505-1513.
50. Zafra F., Gomeza J., Olivares L., Aragon C., Gimenez C. Regional distribution and developmental variation of the glycine transporters GLYT1 and GLYT2 in the rat CNS. Eur. J. Neurosci. 1995, 7:1342-1352.
51. Zeng Z., O'Brien J.A., Lemaire W., O'Malley S.S., Miller P.J., Zhao Z., Wallace M.A., Raab C., Lindsley C.W., Sur C., Williams D.L. A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies. Nucl. Med. Biol. 2008, 35:315-325.
52. Zhou Y., Endres C.J., Brašic J.R., Huang S.C., Wong D.F. Linear regression with spatial constraint to generate parametric images of ligand-receptor dynamic PET studies with a simplified reference tissue model. Neuroimage 2003, 18:975-989.
53. Zhou Y., Resnick S.M., Ye W., Fan H., Holt D.P., Klunk W.E., Mathis C.A., Dannals R., Wong D.F. Using a reference tissue model with spatial constraint to quantify [11C]Pittsburgh compound B PET for early diagnosis of Alzheimer's disease. Neuroimage 2007, 36:298-312.
54. Zhou Y., Ye W., Brašic J.R., Crabb A.H., Hilton J., 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 2009, 44:661-670.
55. Zhou Y., Ye W., Brašic J.R., Wong D.F. Multi-graphical analysis of dynamic PET. Neuroimage 2010, 49:2947-2957.