Initial characterization of a PDE10A selective positron emission tomography tracer [11C]AMG 7980 in non-human primates

Nuclear Medicine and Biology

Volumn 41, Issue 4, 2014, Pages 343-349

  Hwang, Dah Ren ^a   Hu, Essa ^a   Rumfelt, Shannon ^a   Easwaramoorthy, Balu ^b,c   Castrillon, John ^c   Davis, Carl ^a   Allen, Jennifer R ^a   Chen, Hang ^a   Treanor, James ^a   Abi Dargham, Anissa ^b,c   Slifstein, Mark ^b,c  

^a AMGEN INC   (United States)

^b Och Spine at New York Presbyterian Hospitals   (United States)

^c NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

Author keywords

AMG 7980; Carbon 11; PDE10A; PET

Indexed keywords

CARBON 5 (6,7 DIMETHOXYCINNOLIN 4 YL) N ISOPROPYL 3 METHYLPYRIDIN 2 AMINE C 11; TRACER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BABOON; BINDING AFFINITY; BRAIN REGION; CAUDATE NUCLEUS; CONTROLLED STUDY; CORPUS STRIATUM; GLOBUS PALLIDUS; MALE; NEUROIMAGING; NONHUMAN; PET SCANNER; POSITRON EMISSION TOMOGRAPHY; PUTAMEN; RADIOCHEMISTRY; REACTION ANALYSIS;

AMG 7980; CARBON-11; PDE10A; PET;

AMINOPYRIDINES; ANIMALS; BRAIN; CARBON RADIOISOTOPES; FEASIBILITY STUDIES; KINETICS; MALE; PAPIO; PHOSPHORIC DIESTER HYDROLASES; POSITRON-EMISSION TOMOGRAPHY; PYRIDAZINES; RADIOCHEMISTRY;

EID: 84895456097     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2014.01.007     Document Type: Article

References (29)

1. Fujishige K., Kotera J., Michibata H., Yuasa K., Takebayashi S., Okumura K., et al. Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A). J Biol Chem 1999, 274:18438-18445.
2. Nishi A., Snyder G.L. Advanced research on dopamine signaling to develop drugs for the treatment of mental disorders: biochemical and behavioral profiles of phosphodiesterase inhibition in dopaminergic neurotransmission. J Pharmacol Sci 2010, 114:6-16.
3. Greengard P. The neurobiology of slow synaptic transmission. Science 2001, 294:1024-1030.
4. Nishi A., et al. Glutamate regulation of DARPP-32 phosphorylation in neostriatal neurons involves activation of multiple signaling cascades. Proc Natl Acad Sci U S A 2005, 102:1199-1204.
5. Bollen E., Prickaerts J. Phosphodiesterases in neurodegenerative disorders. IUBMB Life 2012, 64:965-970.
6. Giampa C., Laurenti D., Anzilotti S., Bernardi G., Menniti F.S., Fusco F.R. Inhibition of the striatal specific phosphodiesterase PDE10A ameliorates striatal and cortical pathology in R6/2 mouse model of Huntington's disease. PLoS ONE 2010, 5:e13417.
7. Seeger T.F., Bartlett B., Coskran T.M., Culp J.S., James L.C., Krull D.L., et al. Immunohistochemical localization of PDE10A in the rat brain. Brain Res 2003, 985:113-126.
8. Coskran T.M., Morton D., Menniti F.S., Adamowicz W.O., Kleiman R.J., Ryan A.M., et al. Immunohistochemical localization of phosphodiesterase 10A in multiple mammalian species. J Histochem Cytochem 2006, 54:1205-1213.
9. Laruelle M., Kegeles L.S., Abi-Dargham A. Glutamate, dopamine, and schizophrenia: from pathophysiology to treatment. Ann N Y Acad Sci 2003, 1003:138-158.
10. Menniti F.S., Chappie T.A., Humphrey J.M., Schmidt C.J. Phosphodiesterase 10A inhibitors: a novel approach to the treatment of the symptoms of schizophrenia. Curr Opin Investig Drugs 2007, 8:54-59.
11. Tu Z., Xu J., Jones L.A., Li S., Mach R.H. 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.
12. Tu Z., Fan J., Li S., Jones L.A., Cui J., Padakanti P.K., et al. Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain. Bioorg Med Chem 2011, 19:1666-1673.
13. Plisson C., Salinas C., Weinzimmer D., Labaree D., Lin S.-F., Ding Y.-S., et al. Radiosynthesis and in vivo evaluation of [11C]MP-10 as a positron emission tomography radioligand for phosphodiesterase 10A. Nucl Med Biol 2011, 38:875-884.
14. Van Laere K., Ahmad R.U., Hudyana H., Celen S., Dubois K., Schmidt M.E., et al. Human biodistribution and dosimetry of 18F-JNJ42259152, a radioligand for phosphodiesterase 10A imaging. Eur J Nucl Med Mol Imaging 2013, 40:254-261.
15. Andres J.-I., De Angelis M., Alcazar J., Iturrino L., Langlois X., Dedeurwaerdere S., et al. Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging. Journal Medicinal Chemistry 2011, 54:5820-5835.
16. Hu E., Ma J., Biorn C., Lester-Zeiner D., Cho R., Rumfelt S., et al. Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer. J Med Chem 2012, 55:4776-4787.
17. Verhoest P.R., Chapin D.S., Corman M., Fonseca K., Harms J.F., Hou X., et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem 2009, 52:5188-5196.
18. Guide for the care and use of laboratory animals. National Research Council (U.S.) Committee for the Update of the Guide for the Care and Use of Laboratory Animals 2011, The National Academies Press, Washington, D.C. 8th ed.
19. Carson R.E., Channing M.A., Blasberg R.G., Dunn B.B., Cohen R.M., Rice K.C., et al. 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.
20. Brix G., Zaers J., Adam L., Bellemann M., Ostertag H., Trojan H., et al. Performance evaluation of a whole-body PET scanner using the NEMA protocol. National Electrical Manufacturers Association. J Nucl Med 1997, 38:1614-1623.
21. Gandelman M., Baldwin R., Zoghbi S., Zea-Ponce Y., Innis R. Evaluation of ultrafiltration for the free fraction determination of single photon emission computerized tomography (SPECT) radiotracers: b-CIT, IBF, and iomazenil. J Pharm Sci 1994, 83:1014-1019.
22. Mintun M., Raichle M., Kilbourn M., Wooten G., Welch M. A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann Neurol 1984, 15:217-227.
23. Lammertsma A.A., Hume S.P. Simplified Reference Tissue Model for PET Receptor Studies. Neuroimage 1996, 4:153-158.
24. Logan J. A review of graphical methods for tracer studies and strategies to reduce bias. Nucl Med Biol 2003, 30:833-844.
25. Cunningham V.J., Rabiner E.A., Slifstein M., Laruelle M., Gunn R.N. Measuring drug occupancy in the absence of a reference region: the Lassen plot re-visited. J Cereb Blood Flow Metab 2010, 30:46-50.
26. Lassen N.A., Bartenstein P.A., Lammertsma A.A., Prevett M.C., Turton D.R., Luthra S.K., et al. Benzodiazepine receptor quantification in vivo in humans using [11C]flumazenil and PET: application of the steady-state principle. J Cereb Blood Flow Metab 1995, 15:152-165.
27. Carson R.E. PET parameter estimation using linear integration methods: bias and variability. Quantification of brain function. Tracer kinetic and image analysis in brain PET 1993, 499-507. Elsevier Science Publishers. K. Uemura, N.A. Lassen, T. Jones, I. Kanno (Eds.).
28. Slifstein M. Revisiting an old issue: The discrepancy between tissue ratio-derived binding parameters and kinetic modeling-derived parameters after a bolus of the serotonin transporter radioligand I-123-ADAM. J Nucl Med 2008, 49:176-178.
29. Gunn R.N., Murthy V., Catafau A.M., Searle G., Bullich S., Slifstein M., et al. Translational Characterization of [11C]GSK931145, a PET Ligand for the Glycine Transporter Type 1. Synapse 2011, 65:1319-1332.