The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey

Neuropharmacology

Volumn 64, Issue , 2013, Pages 215-223

  Smith, Sean M ^a   Uslaner, Jason M ^a   Cox, Christopher D ^a   Huszar, Sarah L ^a   Cannon, Christopher E ^a   Vardigan, Joshua D ^a   Eddins, Donnie ^a   Toolan, Dawn M ^a   Kandebo, Monika ^a   Yao, Lihang ^a   Raheem, Izzat T ^a   Schreier, John D ^a   Breslin, Michael J ^a   Coleman, Paul J ^a   Renger, John J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cognition; Phosphodiesterase 10A; Schizophrenia; Striatum

Indexed keywords

[2 (6 CHLOROPYRIDIN 3 YL) 4 (2 METHOXYETHOXY) 7,8 DIHYDROPYRIDO[4,3 D]PYRIMIDIN 6(5H)YL](IMIDAZO[1,5 A]PYRIDIN 1 YL)METHANONE; CYCLIC AMP RESPONSIVE ELEMENT BINDING PROTEIN; DONEPEZIL; GLUTAMATE RECEPTOR 1; MITOGEN ACTIVATED PROTEIN KINASE; PHOSPHODIESTERASE; PHOSPHODIESTERASE 10A; PHOSPHODIESTERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AVOIDANCE BEHAVIOR; COGNITION; CONTROLLED STUDY; CORPUS STRIATUM; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG EXPOSURE; DRUG POTENCY; EPISODIC MEMORY; EXECUTIVE FUNCTION; MALE; MEMORY DISORDER; NERVE CELL PLASTICITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; PSYCHOMOTOR ACTIVITY; RAT; RHESUS MONKEY;

ANIMALS; ANTIPSYCHOTIC AGENTS; BEHAVIOR, ANIMAL; COGNITION DISORDERS; CORPUS STRIATUM; DOSE-RESPONSE RELATIONSHIP, DRUG; EXECUTIVE FUNCTION; MACACA MULATTA; MALE; MEMORY, EPISODIC; MOLECULAR TARGETED THERAPY; NERVE TISSUE PROTEINS; NEURONS; NOOTROPIC AGENTS; PHOSPHODIESTERASE INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; PHOSPHORYLATION; PROTEIN PROCESSING, POST-TRANSLATIONAL; PYRIDINES; PYRIMIDINES; RANDOM ALLOCATION; RATS; RATS, WISTAR; SCHIZOPHRENIA;

EID: 84866379713     PISSN: 00283908     EISSN: 18737064     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2012.06.013     Document Type: Article

References (59)

1. A.A. Baumeister, and J.L. Francis Historical development of the dopamine hypothesis of schizophrenia J. Hist. Neurosci. 11 2002 265 277
2. A.T. Bender, and J.A. Beavo Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use Pharmacol. Rev. 58 2006 488 520
3. F.G. Boess, M. Hendrix, F.J. van der Staay, C. Erb, R. Schreiber, W. van Staveren, J. de Vente, J. Prickaerts, A. Blokland, and G. Koenig Inhibition of phosphodiesterase 2 increases neuronal cGMP, synaptic plasticity and memory performance Neuropharmacology 47 2004 1081 1092
4. M.J. Breslin, P.J. Coleman, C.D. Cox, I.T. Raheem, and J.D. Schreier Alkoxy Tetrahydro-Pyridopryimidine PDE10 Inhibitors 2010 Merck Sharpe & Dohme W02010138430
5. O. Bruno, E. Fedele, J. Prickaerts, L. Parker, E. Canepa, C. Brullo, A. Cavallero, E. Gardella, A. Balbi, C. Domenicotti, E. Bollen, H. Gijselaers, T. Vanmierlo, K. Erb, C. Limebeer, F. Argellati, U. Marinari, M. Pronzato, and R. Ricciarelli GEBR-7b, a novel PDE4D selective inhibitor that improves memory in rodents at non-emetic doses Br. J. Pharmacol. 164 2011 2054 2063
6. S.Z. Chao, W. Lu, H.K. Lee, R.L. Huganir, and M.E. Wolf D(1) dopamine receptor stimulation increases GluR1 phosphorylation in postnatal nucleus accumbens cultures J. Neurochem. 81 2002 984 992
7. M.A. Cirillo, and L.J. Seidman Verbal declarative memory dysfunction in schizophrenia: from clinical assessment to genetics and brain mechanisms Neuropsychol. Rev. 13 2003 43 77
8. T.M. Coskran, D. Morton, F.S. Menniti, W.O. Adamowicz, R.J. Kleiman, A.M. Ryan, C.A. Strick, C.J. Schmidt, and D.T. Stephenson Immunohistochemical localization of phosphodiesterase 10A in multiple mammalian species J. Histochem. Cytochem. 54 2006 1205 1213
9. I. Creese, D.R. Burt, and S.H. Snyder Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs Science 192 1976 481 483
10. J. Delay, P. Deniker, and J.M. Harl Therapeutic use in psychiatry of phenothiazine of central elective action (4560 RP) Ann. Med. Psychol. (Paris) 110 1952 112 117
11. A. Diamond, S. Zola-Morgan, and L.R. Squire Successful performance by monkeys with lesions of the hippocampal formation on AB and object retrieval, two tasks that mark developmental changes in human infants Behav. Neurosci. 103 1989 526 537
12. R. Dias, T.W. Robbins, and A.C. Roberts Dissociation in prefrontal cortex of affective and attentional shifts Nature 380 1996 69 72
13. K. Fujishige, J. Kotera, H. Michibata, K. Yuasa, S. Takebayashi, K. Okumura, and K. Omori Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A) J. Biol. Chem. 274 1999 18438 18445
14. F. Fumagalli, A. Frasca, G. Racagni, and M.A. Riva Dynamic regulation of glutamatergic postsynaptic activity in rat prefrontal cortex by repeated administration of antipsychotic drugs Mol. Pharmacol. 73 2008 1484 1490
15. P.S. Goldman-Rakic Working memory dysfunction in schizophrenia J. Neuropsychiatry Clin. Neurosci. 6 1994 348 357
16. S.M. Grauer, V.L. Pulito, R.L. Navarra, M.P. Kelly, C. Kelley, R. Graf, B. Langen, S. Logue, J. Brennan, L. Jiang, E. Charych, U. Egerland, F. Liu, K.L. Marquis, M. Malamas, T. Hage, T.A. Comery, and N.J. Brandon Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia J. Pharmacol. Exp. Ther. 331 2009 574 590
17. M.F. Green What are the functional consequences of neurocognitive deficits in schizophrenia? Am. J. Psychiatry 153 1996 321 330
18. M.F. Green, K.H. Nuechterlein, J.M. Gold, D.M. Barch, J. Cohen, S. Essock, W.S. Fenton, F. Frese, T.E. Goldberg, R.K. Heaton, R.S. Keefe, R.S. Kern, H. Kraemer, E. Stover, D.R. Weinberger, S. Zalcman, and S.R. Marder Approaching a consensus cognitive battery for clinical trials in schizophrenia: the NIMH-MATRICS conference to select cognitive domains and test criteria Biol. Psychiatry 56 2004 301 307
19. P. Greengard, P.B. Allen, and A.C. Nairn Beyond the dopamine receptor: the DARPP-32/protein phosphatase-1 cascade Neuron 23 1999 435 447
20. P.D. Harvey, M.F. Green, R.S. Keefe, and D.I. Velligan Cognitive functioning in schizophrenia: a consensus statement on its role in the definition and evaluation of effective treatments for the illness J. Clin. Psychiatry 65 2004 361 372
21. W. Huang, Y. Zhang, and J.R. Sportsman A fluorescence polarization assay for cyclic nucleotide phosphodiesterases J. Biomol. Screen. 7 2002 215 222
22. P.H. Hutson, E.N. Finger, B.C. Magliaro, S.M. Smith, A. Converso, P.E. Sanderson, D. Mullins, L.A. Hyde, B.K. Eschle, Z. Turnbull, H. Sloan, M. Guzzi, X. Zhang, A. Wang, D. Rindgen, R. Mazzola, J.A. Vivian, D. Eddins, J.M. Uslaner, R. Bednar, C. Gambone, W. Le-Mair, M.J. Marino, N. Sachs, G. Xu, and S. Parmentier-Batteur The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1- (tetrahydr o-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents Neuropharmacology 61 2011 665 676
23. J.D. Jentsch, and R.H. Roth The neuropsychopharmacology of phencyclidine: from NMDA receptor hypofunction to the dopamine hypothesis of schizophrenia Neuropsychopharmacology 20 1999 201 225
24. J.D. Jentsch, R.H. Roth, and J.R. Taylor Object retrieval/detour deficits in monkeys produced by prior subchronic phencyclidine administration: evidence for cognitive impulsivity Biol. Psychiatry 48 2000 415 424
25. R.S. Keefe, R.M. Bilder, S.M. Davis, P.D. Harvey, B.W. Palmer, J.M. Gold, H.Y. Meltzer, M.F. Green, G. Capuano, T.S. Stroup, J.P. McEvoy, M.S. Swartz, R.A. Rosenheck, D.O. Perkins, C.E. Davis, J.K. Hsiao, and J.A. Lieberman Neurocognitive effects of antipsychotic medications in patients with chronic schizophrenia in the CATIE Trial Arch. Gen. Psychiatry 64 2007 633 647
26. R.S. Kern, M.F. Green, K.H. Nuechterlein, and B.H. Deng NIMH-MATRICS survey on assessment of neurocognition in schizophrenia Schizophr. Res. 72 2004 11 19
27. Y.F. Li, Y.F. Cheng, Y. Huang, M. Conti, S.P. Wilson, J.M. O'Donnell, and H.T. Zhang Phosphodiesterase-4D knock-out and RNA interference-mediated knock-down enhance memory and increase hippocampal neurogenesis via increased cAMP signaling J. Neurosci. 31 2011 172 183
28. K. Loughney, P.B. Snyder, L. Uher, G.J. Rosman, K. Ferguson, and V.A. Florio Isolation and characterization of PDE10A, a novel human 3', 5'-cyclic nucleotide phosphodiesterase Gene 234 1999 109 117
29. A. Markou, C. Chiamulera, M.A. Geyer, M. Tricklebank, and T. Steckler Removing obstacles in neuroscience drug discovery: the future path for animal models Neuropsychopharmacology 34 2009 74 89
30. F.S. Menniti, T.A. Chappie, J.M. Humphrey, and C.J. Schmidt Phosphodiesterase 10A inhibitors: a novel approach to the treatment of the symptoms of schizophrenia Curr. Opin. Investig. Drugs 8 2007 54 59
31. Millan, M.J.; Agid, Y.; Brune, M.; Bullmore, E.T.; Carter, C.S.; Clayton, N.S.; Connor, R.; Davis, S.; Deakin, B.; DeRubeis, R. J.; Dubois, B.; Geyer, M.A.; Goodwin, G.M.; Gorwood, P.; Jay, T.M.; Joels, M.; Mansuy, I.M.; Meyer-Lindenberg, A.; Murphy, D.; Rolls, E.; Saletu, B.; Spedding, M.; Sweeney, J.; Whittington, M.; Young, L.J.; 2012. Cognitive dysfunction in psychiatric disorders: characteristics, causes and the quest for improved therapy. Nat. Rev. Drug Discov. 11, 141-168.
32. S.D. Mosser, S.L. Gaul, B. Bednar, K.S. Koblan, and R.A. Bednar Automation of in vitro dose-inhibition assays utilizing the tecan genesis and as integrated software package to support the drug discovery process J. Assoc. Lab. Automation 8 2003 54 63
33. A. Nishi, M. Kuroiwa, and T. Shuto Mechanisms for the modulation of dopamine d(1) receptor signaling in striatal neurons Front. Neuroanat. 5 2011 1 10
34. A. Nishi, and G.L. Snyder 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. Pharm. Sci. 114 2010 6 16
35. E. Perez-Costas, M. Melendez-Ferro, and R.C. Roberts Basal ganglia pathology in schizophrenia: dopamine connections and anomalies J. Neurochem. 113 2010 287 302
36. J.S. Rodefer, E.R. Murphy, and M.G. Baxter PDE10A inhibition reverses subchronic PCP-induced deficits in attentional set-shifting in rats Eur. J. Neurosci. 21 2005 1070 1076
37. J.S. Rodefer, S.K. Saland, and S.J. Eckrich Selective phosphodiesterase inhibitors improve performance on the ED/ID cognitive task in rats Neuropharmacology 62 2011 1182 1190
38. C.J. Schmidt, D.S. Chapin, J. Cianfrogna, M.L. Corman, M. Hajos, J.F. Harms, W.E. Hoffman, L.A. Lebel, S.A. McCarthy, F.R. Nelson, C. Proulx-LaFrance, M.J. Majchrzak, A.D. Ramirez, K. Schmidt, P.A. Seymour, J.A. Siuciak, F.D. Tingley 3rd, R.D. Williams, P.R. Verhoest, and F.S. Menniti Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia J. Pharmacol. Exp. Ther. 325 2008 681 690
39. T.F. Seeger, B. Bartlett, T.M. Coskran, J.S. Culp, L.C. James, D.L. Krull, J. Lanfear, A.M. Ryan, C.J. Schmidt, C.A. Strick, A.H. Varghese, R.D. Williams, P.G. Wylie, and F.S. Menniti Immunohistochemical localization of PDE10A in the rat brain Brain Res. 985 2003 113 126
40. P. Seeman, M. Chau-Wong, J. Tedesco, and K. Wong Brain receptors for antipsychotic drugs and dopamine: direct binding assays Proc. Natl. Acad. Sci. U S A 72 1975 4376 4380
41. J.D. Shepherd, and R.L. Huganir The cell biology of synaptic plasticity: AMPA receptor trafficking Annu. Rev. Cell Dev. Biol. 23 2007 613 643
42. E.H. Simpson, C. Kellendonk, and E. Kandel A possible role for the striatum in the pathogenesis of the cognitive symptoms of schizophrenia Neuron 65 2010 585 596
43. J.A. Siuciak, D.S. Chapin, J.F. Harms, L.A. Lebel, S.A. McCarthy, L. Chambers, A. Shrikhande, S. Wong, F.S. Menniti, and C.J. Schmidt Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis Neuropharmacology 51 2006 386 396
44. J.A. Siuciak, S.A. McCarthy, D.S. Chapin, R.A. Fujiwara, L.C. James, R.D. Williams, J.L. Stock, J.D. McNeish, C.A. Strick, F.S. Menniti, and C.J. Schmidt Genetic deletion of the striatum-enriched phosphodiesterase PDE10A: evidence for altered striatal function Neuropharmacology 51 2006 374 385
45. S.M. Smith, R.A. Bednar, M.J. Breslin, P.J. Coleman, C.D. Cox, J. Fuerst, P.H. Hutson, M. Kandebo, A.J. Kemmerer, S.H. Kim, W. Lemaire, B. Ma, G. McGaughey, I.T. Raheem, J.D. Schreier, L. Yao, and J.J. Renger Characterization of a Novel Small Molecule Phosphodiesterase 10 (PDE10A) Inhibitor Program No. 900.26. 2011 Neuroscience Meeting Planner 2011 Society for Neuroscience Washington, DC (Online)
46. G.L. Snyder, P.B. Allen, A.A. Fienberg, C.G. Valle, R.L. Huganir, A.C. Nairn, and P. Greengard Regulation of phosphorylation of the GluR1 AMPA receptor in the neostriatum by dopamine and psychostimulants in vivo J. Neurosci. 20 2000 4480 4488
47. S.H. Soderling, S.J. Bayuga, and J.A. Beavo Isolation and characterization of a dual-substrate phosphodiesterase gene family: PDE10A Proc. Natl. Acad. Sci. U S A 96 1999 7071 7076
48. J.R. Taylor, J.D. Elsworth, R.H. Roth, T.J. Collier, J.R. Sladek Jr.; and D.E. Redmond Jr. Improvements in MPTP-induced object retrieval deficits and behavioral deficits after fetal nigral grafting in monkeys Prog. Brain Res. 82 1990 543 559
49. J.R. Taylor, R.H. Roth, J.R. Sladek Jr.; and D.E. Redmond Jr. Cognitive and motor deficits in the performance of an object retrieval task with a barrier-detour in monkeys (Cercopithecus aethiops sabaeus) treated with MPTP: long-term performance and effect of transparency of the barrier Behav. Neurosci. 104 1990 564 576
50. S. Threlfell, S. Sammut, F.S. Menniti, C.J. Schmidt, and A.R. West Inhibition of phosphodiesterase 10A increases the responsiveness of striatal projection neurons to cortical stimulation J. Pharmacol. Exp. Ther. 328 2009 785 795
51. C. Tsutsumi, H. Uchida, T. Suzuki, K. Watanabe, H. Takeuchi, S. Nakajima, Y. Kimura, Y. Tsutsumi, K. Ishii, Y. Imasaka, and S. Kapur The evolution of antipsychotic switch and polypharmacy in natural practice - a longitudinal perspective Schizophr. Res. 130 2011 40 46
52. J. van Os, and S. Kapur Schizophrenia Lancet 374 2009 635 645
53. M.L. Wadenberg, S. Kapur, A. Soliman, C. Jones, and F. Vaccarino Dopamine D2 receptor occupancy predicts catalepsy and the suppression of conditioned avoidance response behavior in rats Psychopharmacology (Berl) 150 2000 422 429
54. M.L. Wadenberg, A. Soliman, S.C. VanderSpek, and S. Kapur Dopamine D(2) receptor occupancy is a common mechanism underlying animal models of antipsychotics and their clinical effects Neuropsychopharmacology 25 2001 633 641
55. H. Wan, J.P. Aggleton, and M.W. Brown Different contributions of the hippocampus and perirhinal cortex to recognition memory J. Neurosci. 19 1999 1142 1148
56. L.S. Wilkinson, R. Dias, K.L. Thomas, S.J. Augood, B.J. Everitt, T.W. Robbins, and A.C. Roberts Contrasting effects of excitotoxic lesions of the prefrontal cortex on the behavioural response to D-amphetamine and presynaptic and postsynaptic measures of striatal dopamine function in monkeys Neuroscience 80 1997 717 730
57. O. Witczak, E.M. Aandahl, and K. Tasken Role of A-kinase anchoring proteins in the compartmentation in cyclic nucleotide signaling J.A. Beavo, S.H. Francis, M.D. Houslay, Cyclic Nucleotide Phosphodiesterases in Health and Disease 2007 CRC Press Boca Raton 377 394
58. Z. Xie, W.O. Adamowicz, W.D. Eldred, A.B. Jakowski, R.J. Kleiman, D.G. Morton, D.T. Stephenson, C.A. Strick, R.D. Williams, and F.S. Menniti Cellular and subcellular localization of PDE10A, a striatum-enriched phosphodiesterase Neuroscience 139 2006 597 607
59. J.W. Young, S.B. Powell, V. Risbrough, H.M. Marston, and M.A. Geyer Using the MATRICS to guide development of a preclinical cognitive test battery for research in schizophrenia Pharmacol. Ther. 122 2009 150 202