Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment of schizophrenia

Neuropharmacology

Volumn 62, Issue 2, 2012, Pages 1152-1161

  Alberati, Daniela ^a   Moreau, Jean Luc ^a   Lengyel, Judith ^a   Hauser, Nicole ^a   Mory, Roland ^a   Borroni, Edilio ^a   Pinard, Emmanuel ^a   Knoflach, Frederic ^a   Schlotterbeck, Götz ^a   Hainzl, Dominik ^a   Wettstein, Joseph G ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Glutamate; Glycine; Glycine reuptake inhibitor; Neuropharmacology; NMDA; Schizophrenia

Indexed keywords

[4 (3 FLUORO 5 TRIFLUOROMETHYLPYRIDIN 2 YL)PIPERAZIN 1 YL] [5 METHANESULFONYL 2 (2,2,2 TRIFLUORO 1 METHYLETHOXY)PHENYL]METHANONE; GLYCINE; GLYCINE RECEPTOR ANTAGONIST; N METHYL DEXTRO ASPARTIC ACID; RG 1678; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING SITE; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG DOSE COMPARISON; DRUG MECHANISM; HYPERACTIVITY; IC 50; IN VITRO STUDY; IN VIVO STUDY; LONG TERM POTENTIATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; SCHIZOPHRENIA;

AMPHETAMINE; ANIMALS; CA1 REGION, HIPPOCAMPAL; CELL LINE; CENTRAL NERVOUS SYSTEM STIMULANTS; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; HALLUCINOGENS; HUMANS; LONG-TERM POTENTIATION; MICE; MOTOR ACTIVITY; PHENCYCLIDINE; PIPERAZINES; RATS; RATS, SPRAGUE-DAWLEY; SULFONES; SYNAPTIC TRANSMISSION;

EID: 84855979108     PISSN: 00283908     EISSN: 18737064     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2011.11.008     Document Type: Article

References (63)

1. D. Alberati, J.-L. Moreau, R. Mory, E. Pinard, and J.G. Wettstein Pharmacological evaluation of a novel assay for detecting glycine transporter 1 inhibitors and their antipsychotic potential Pharmacol. Biochem. Behav. 97 2010 185 191
2. B.M. Angrist, and S. Gershon The phenomenology of experimentally induced amphetamine psychosis - preliminary observations Biol. Psychiatry 2 1970 95 107
3. D. Boulay, O. Bergis, P. Avenet, and G. Griebel The glycine transporter-1 inhibitor SSR103800 displays a selective and specific antipsychotic-like profile in normal and transgenic mice Neuropsychopharmacology 35 2010 416 427
4. A. Brown, I. Carlyle, J. Clark, W. Hamilton, S. Gibson, and G. McGarry Discovery and SAR of org 24598 - a selective glycine uptake inhibitor Bioorg. Med. Chem. Lett. 11 2001 2007 2009
5. A. Carlsson, N. Waters, and M.L. Carlsson Neurotransmitter interactions in schizophrenia - therapeutic implications Biol. Psychiatry 46 1999 1388 1395
6. A. Carlsson, N. Waters, S. Waters, and M.L. Carlsson Network interactions in schizophrenia - therapeutic implications Brain Res. Brain Res. Rev. 31 2000 342 349
7. W.L. Caulfield, I.T. Collie, R.S. Dickins, O. Epemolu, R. McGuire, and D.R. Hill The first potent and selective inhibitors of the glycine transporter type 2 J. Med. Chem. 44 2001 2679 2682
8. H.-X. Chen, N. Otmakhov, and J. Lisman Requirements for LTP induction by pairing in hippocampal CA1 pyramidal cells J. Neurophysiol. 82 1999 526 532
9. L. Chen, M. Muhlhauser, and C.R. Yang Glycine tranporter-1 blockade potentiates NMDA-mediated responses in rat prefrontal cortical neurons in vitro and in vivo J. Neurophysiol. 89 2003 691 703
10. M.C. Clugnet, and J.E. LeDoux Synaptic plasticity in fear conditioning circuits: induction of LTP in the lateral nucleus of the amygdala by stimulation of the medial geniculate body J. Neurosci. 10 1990 2818 2824
11. B. Cubelos, C. Giménez, and F. Zafra Localization of the GLYT1 glycine transporter at glutamatergic synapses in the rat brain Cereb. Cortex 15 2005 448 459
12. W. Danysz, and C.G. Parsons Glycine and N-methyl-d-aspartate receptors: physiological significance and possible therapeutic applications Pharmacol. Rev. 50 1998 597 664
13. B.A. Donzanti, and B.K. Yamamoto An improved and rapid HPLC-EC method for the isocratic separation of amino acid neurotransmitters from brain tissue and microdialysis perfusates Life Sci. 43 1988 913 922
14. P.J. Harrison, and D.R. Weinberger Schizophrenia genes, gene expression, and neuropathology: on the matter of their convergence Mol. Psychiatry 10 2005 40 68
15. L.G. Harsing Jr., Z. Juranyi, I. Gacsalyi, P. Tapolcsanyi, A. Czompa, and P. Matyus Glycine transporter type-1 and its inhibitors Curr. Med. Chem. 13 2006 1017 1044
16. H.J. Herdon, F.M. Godfrey, A.M. Brown, S. Coulton, J.R. Evans, and W.J. Cairns Pharmacological assessment of the role of the glycine transporter GlyT-1 in mediating high-affinity glycine uptake by rat cerebral cortex and cerebellum synaptosomes Neuropharmacology 41 2001 88 96
17. U. Heresco-Levy, D.C. Javitt, M. Ermilov, C. Mordel, A. Horowitz, and D. Kelly Double-blind, placebo-controlled, crossover trial of glycine adjuvant therapy for treatment-resistant schizophrenia Br. J. Psychiatry 169 1996 610 617
18. D.C. Javitt Negative schizophrenic symptomatology and the PCP (phencyclidine) model of schizophrenia Hillside J. Clin. Psychiatry 9 1987 12 35
19. D.C. Javitt Glutamate and schizophrenia: phencyclidine, N-methyl-d-aspartate receptors, and dopamine-glutamate interactions Int. Rev. Neurobiol. 78 2007 69 108
20. D.C. Javitt Glutamatergic theories of schizophrenia Isr. J. Psychiatry Relat. Sci. 47 2010 4 16
21. J.W. Johnson, and P. Ascher Glycine potentiates the NMDA response in cultured mouse brain neurons Nature 325 1987 529 531
22. P.B. Jones, T.R.E. Barnes, L. Davies, G. Dunn, H. Lloyd, and K.P. Hayhurst Randomized controlled trial of the effect on quality of life of second- vs first-generation antipsychotic drugs in schizophrenia: Cost Utility of the Latest Antipsychotic drugs in Schizophrenia Study (CUtLASS 1) 33 Arch. Gen. Psychiatry 63 2006 1079 1087
23. F. Jursky, and N. Nelson Developmental expression of the glycine transporter GlyT1 and GlyT2 in mouse brain J. Neurochem. 67 1996 336 344
24. J.T. Kantrowitz, and D.C. Javitt Thinking glutamatergically: changing concepts of schizophrenia based upon changing neurochemical models Clin. Schizophr. Relat. Psychoses 4 2010 189 200
25. J.A. Kauer, and R.C. Malenka Synaptic plasticity and addiction Nat. Rev. Neurosci. 8 2007 844 858
26. L.S. Kegeles, A. Abi-Dargham, Y. Zea-Ponce, J. Rodenhiser-Hill, J.J. Mann, and R.L. Van Heertum Modulation of amphetamine-induced striatal dopamine release by ketamine in humans: implications for schizophrenia Biol. Psychiatry 48 2000 627 640
27. K.-M. Kim, S.F. Kingsmore, H. Han, T.L. Yang-Feng, N. Godinot, F.S. Seldin, M.G. Caron, and B. Giros Cloning of the human glycine transporter type 1: molecular and pharmacological characterization of novel isoform variants and chromosomal localization of the gene in the human and mouse genomes Mol. Pharmacol. 45 1994 608 617
28. N.W. Kleckner, and R. Dingledine Requirement for glycine in activation of NMDA-receptors expressed in Xenopus oocytes Science 241 1988 835 837
29. K. Kopec, D.G. Flood, M. Gasior, B.A.W. McKenna, E. Zuvich, J. Schreiber, J.M. Salvino, J.T. Durkin, M.A. Ator, and M.J. Marino Glycine transporter (GlyT1) inhibitors with reduced residence time increase prepulse inhibition without inducing hyperlocomotion in DBA/2 mice Biochem. Pharmacol. 80 2010 1407 1417
30. J.H. Krystal, L.P. Karper, J.P. Seibyl, G.K. Freeman, R. Delaney, and J.D. Bremner Subanesthetic effects of the noncompetitive NMDA antagonist, ketamine, in humans. Psychotomimetic, perceptual, cognitive, and neuroendocrine responses Arch. Gen. Psychiatry 51 1994 199 214
31. H.Y. Lane, Y.C. Chang, Y.C. Liu, C.C. Chiu, and G.E. Tsai Sarcosine or d-serine add-on treatment for acute exacerbation of schizophrenia: a randomized, double-blind, placebo-controlled study Arch. Gen. Psychiatry 62 2005 1196 1204
32. M. Laruelle, A. Abi-Dargham, C.H. van Dyck, R. Gil, C.D. D'Souza, and J. Erdos Single photon emission computerized tomography imaging of amphetamine-induced dopamine release in drug-free schizophrenic subjects Proc. Natl. Acad. Sci. USA 93 1996 9235 9240
33. M. Laruelle Imaging dopamine transmission in schizophrenia. A review and meta-analysis Q. J. Nucl. Med. 42 1998 211 221
34. S. Leucht, W. Kissling, and J.M. Davis Second-generation antipsychotics for schizophrenia: can we resolve the conflict? Psychol. Med. 39 2009 1591 1602
35. D.A. Lewis, and J.A. Lieberman Catching up on schizophrenia: natural history and neurobiology Neuron 28 2000 325 334
36. Q.-R. Liu, H. Nelson, S. Mandyian, B. López-Corcuera, and N. Nelson Cloning and expression of a glycine transporter from mouse brain FEBS Lett. 305 1992 110 114
37. J.M. Luque, N. Nelson, and J.G. Richards Cellular expression of glycine transporter 2 messenger RNA exclusively in rat hindbrain and spinal cord Neuroscience 64 1995 525 535
38. M. Martina, Y. Gorfinkel, S. Halman, J.A. Lowe, P. Periyalwar, and C.J. Schmidt Glycine transporter type 1 blockade changes NMDA receptor-mediated responses and LTP in hippocampal CA1 pyramidal cells by altering extracellular glycine levels J. Physiol. 557 2004 489 500
39. P. Milev, B.C. Ho, S. Arndt, and N.C. Andreasen Predictive values of neurocognition and negative symptoms on functional outcome in schizophrenia: a longitudinal first-episode study with 7-year follow-up Am. J. Psychiatry 162 2005 495 506
40. M.J. Millan N-methyl-d-aspartate receptors as a target for improved antipsychotic agents: novel insights and clinical perspectives Psychopharmacology (Berl.) 179 2005 30 53
41. J.A. Morrow, I.T. Collie, D.R. Dunbar, G.B. Walker, M. Shahid, and D.R. Hill Molecular cloning and functional expression of the human glycine transporter GlyT2 and chromosomal localization of the gene in the human genome FEBS Lett. 439 1998 334 340
42. K. Nagy, B. Marko, G. Zsilla, P. Matyus, K. Pallagi, and G. Szabo Alterations in brain extracellular dopamine and glycine levels following combined administration of the glycine transporter type-1 inhibitor Org-24461 and risperidone Neurochem. Res. 35 2010 2096 2106
43. J.M. Narvaez, E.W. Twamley, C.L. McKibbin, R.K. Heaton, and T.L. Patterson Subjective and objective quality of life in schizophrenia Schizophr. Res. 98 2008 201 208
44. J.C. Neill, S. Barnes, S. Cook, B. Grayson, N.F. Idris, and S.L. McLean Animal models of cognitive dysfunction and negative symptoms of schizophrenia: focus on NMDA receptor antagonism Pharmacol. Ther. 128 2010 419 432
45. Y. Nong, Y.-Q. Huang, W. Ju, L.V. Kalia, G. Ahmadian, and Y.T. Wang Glycine binding primes NMDA receptor internalization Nature 422 2003 302 307
46. K.W. Perry, J.F. Falcone, M.J. Fell, J.W. Ryder, H. Yu, and P.L. Love Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas Neuropharmacology 55 2008 743 754
47. E. Pinard, S. Burner, P. Cueni, F. Montavon, and D. Zimmerli A short and efficient synthesis of the NMDA glycine site antagonist: (3R,4R)-3-amino-1- hydroxy-4-methyl pyrrolidin-2-one (L-687,414) Tetrahedron Lett. 49 2008 6079 6080
48. E. Pinard, A. Alanine, D. Alberati, M. Bender, E. Borroni, and P. Bourdeaux 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. 53 2010 4603 4614
49. D.J. Sanger The search for novel antipsychotics: pharmacological and molecular targets Expert Opin. Ther. Targets 8 2004 631 641
50. P. Saranssari, and S.S. Oja Glycine release from hippocampal slices in developing and aged mice: modulation by glutamatergic receptors Mech. Ageing Dev. 76 1994 113 124
51. P. Saranssari, and S.S. Oja Mechanism of glycine release in mouse brain stem slices Neurochem. Res. 34 2009 286 294
52. N.B. Saul'skaya, and N.A. Solov'eva Tetrodotoxin-dependent glycine release in the rat nucleous accumbens during correction of feeding behavior Neurosci. Behav. Physiol. 35 2005 815 819
53. P. Seeman, T. Lee, M. Chau-Wong, and K. Wong Antipsychotic drug doses and neuroleptic/dopamine receptors Nature 261 1976 717 719
54. P. Singer, J. Feldon, and B.K. Yee Interactions between the glycine transporter 1(GlyT1) inhibitor SSR504734 and psychoactive drugs in mouse motor behaviour Eur. Neuropsychopharmacol. 19 2009 571 580
55. S. Smith, and T. Sharp Measurement of GABA in rat brain microdialysates using o-phthaldialdehyde-sulphite derivatization and high-performance liquid chromatography with electrochemical detection J. Chromatogr. B Biomed. Sci. Appl. 652 1994 228 233
56. J.M. Stone Imaging the glutamate system in humans: relevance to drug discovery for schizophrenia Curr. Pharm. Des. 15 2009 2594 2602
57. C. Sur, and G.G. Kinney The therapeutic potential of glycine transporter-1 inhibitors Expert Opin. Investig. Drugs 13 2004 515 521
58. 1H-NMR spectroscopy of human cerebrospinal fluid: effects of sample manipulation and assignment of resonances J. Pharm. Biomed. Anal. 11 1993 651 664
59. C. Tek, B. Kirkpatrick, and R.W. Buchanan A five-year follow up study of deficit and nondeficit schizophrenia Schizophr. Res. 49 2001 253 260
60. M.D. Tricklebank, L.J. Bristow, P.H. Hutson, P.D. Leeson, M. Rowley, and K. Saywell The anticonvulsant and behavioural profile of L-687,414, a partial agonist acting at the glycine modulatory site on the N-methyl-d-aspartate (NMDA) receptor complex Br. J. Pharmacol. 113 1994 729 736
61. G. Tsai, P. Yang, L.C. Chung, N. Lange, and J.T. Coyle d-serine added to antipsychotics for the treatment of schizophrenia Biol. Psychiatry 44 1998 1081 1089
62. G. Tsai, H.-Y. Lane, P. Yang, M.-Y. Chong, and N. Lange Glycine transporter I inhibitor, N-methylglycine (sarcosine), added to antipsychotics for the treatment of schizophrenia Biol. Psychiatry 55 2004 452 456
63. L. Wilbrecht, A. Holtmaat, N. Wright, K. Fox, and K. Svoboda Structural plasticity underlies experience-dependent functional plasticity of cortical circuits J. Neurosci. 30 2010 4927 4932