Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas

Neuropharmacology

Volumn 55, Issue 5, 2008, Pages 743-754

  Perry, Kenneth W ^a   Falcone, Julie F ^a   Fell, Matthew J ^a   Ryder, John W ^a   Yu, Hong ^a   Love, Patrick L ^a   Katner, Jason ^a   Gordon, Kimberly D ^a   Wade, Mark R ^a   Man, Teresa ^b   Nomikos, George G ^a   Phebus, Lee A ^a   Cauvin, Annick J ^c   Johnson, Kirk W ^a   Jones, Carrie K ^a   Hoffmann, Beth J ^a   Sandusky, George E ^a   Walter, Magnus W ^b   Porter, Warren J ^a   Yang, Lijuan ^a   Merchant, Kalpana M ^a   Shannon, Harlan E ^a   Svensson, Kjell A ^a   more..

^a ELI LILLY AND COMPANY   (United States)

^b Eli Lilly Discovery Chemistry   (United Kingdom)

^c Eli Lilly Benelux   (Belgium)

Author keywords

cGMP; Glycine; Immuno staining; Microdialysis; NMDA; Respiration

Indexed keywords

7 CHLORO 4 HYDROXY 3 (3 PHENOXYPHENYL) 2 QUINOLONE; [[2 (4 BENZO[1,3]DIOXOL 5 YL 2 TERT BUTYLPHENOXY)ETHYL] METHYLAMINO]ACETIC ACID; ALX 5407; DRUG VEHICLE; GLYCINE; GLYCINE A RECEPTOR ANTAGONIST; GLYCINE B RECEPTOR ANTAGONIST; GLYCINE RECEPTOR ANTAGONIST; GLYCINE TRANSPORTER; GLYCINE TRANSPORTER ANTIBODY; GLYCINE TRANSPORTER INHIBITOR; LY 2365109; N METHYL DEXTRO ASPARTIC ACID; NEUROTRANSMITTER; STRYCHNINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRAIN STEM; BREATHING; CEREBELLUM; CONTROLLED STUDY; CORPUS STRIATUM; DRUG BRAIN LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG MEGADOSE; FRONTAL CORTEX; HIPPOCAMPUS; HUMAN; HUMAN CELL; IMMUNOHISTOCHEMISTRY; IMMUNOREACTIVITY; MALE; MICRODIALYSIS; MONKEY; MOTOR PERFORMANCE; MOUSE; NEUROTRANSMITTER RELEASE; NONHUMAN; PREFRONTAL CORTEX; PRIORITY JOURNAL; PROTEIN LOCALIZATION; RAT; SCHIZOPHRENIA; SPECIES DIFFERENTIATION; TISSUE DISTRIBUTION;

ANIMALS; BEHAVIOR, ANIMAL; BRAIN CHEMISTRY; CELL LINE, TUMOR; CEREBRAL CORTEX; CORPUS STRIATUM; CYCLIC GMP; DIOXOLES; DOSE-RESPONSE RELATIONSHIP, DRUG; EXCITATORY AMINO ACID ANTAGONISTS; GLYCINE; GLYCINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MALE; MICE; MICRODIALYSIS; MOTOR ACTIVITY; NEUROBLASTOMA; NEUROTRANSMITTER AGENTS; QUINOLONES; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; SARCOSINE; TIME FACTORS;

EID: 51049089047     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2008.06.016     Document Type: Article

References (38)

1. Anderson J.J., Kuo S., and Chase T.N. Endogenous excitatory amino acids tonically stimulate striatal acetylcholine release through NMDA but not AMPA receptors. Neuroscience Letters 176 (1994) 264-268
2. Atkinson B.N., Bell S.C., De Vivo M., Kowalski L.R., Lechner S.M., Ognyanov V.I., Tham C.-S., Tsai C., Jia J., Ashton D., and Klitenick M.A. ALX5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. Molecular Pharmacology 60 (2001) 1414-1420
3. Bergeron R., Meyer T.M., Coyle J.T., and Greene R.W. Modulation of N-methyl-d-aspartate receptor function by glycine transport. Proceedings of the National Academy of Sciences 95 (1998) 15730-15734
4. Buchanan R.W., Gold J.M., Bilder R., Green M., Javitt D.C., Marder S.R., Schooler N.R., Heresco-Levy U., MacMahon R.P., and Carpenter W.T. Glutamatergic agents for the treatment of cognitive impairments in patients with schizophrenia. Proceedings from the International Meeting on Schizophrenia Research, Savannah, GA, April 2-5, 2005. Schizophrenia Bulletin 31 (2005) P477
5. Carlsson M., and Carlsson A. Interaction between glutamatergic and monoaminergic systems within the basal ganglia: implications for schizophrenia and Parkinson's disease. Trends in Neuroscience 13 (1990) 272-276
6. Chen L., Muhlhauser M., and Yang C.R. Glycine transporter-1 blockade potentiates NMDA-mediated responses in rat prefrontal cortical neurons in vitro and in vivo. Journal of Neurophysiology 89 (2003) 691-703
7. Cubelos B., Gimenez C., and Zafra F. Localization of the GlyT1 glycine transporter at glutamatergic synapses in the rat brain. Cerebral Cortex 15 (2005) 448-459
8. Depoortere R., et al. Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic. Neuropsychopharmacology 4 (2005) 1-23
9. Dunham N.W., and Miya T.S. A note on a simple apparatus for detecting neurological deficit in rats and mice. Journal of the American Pharmacology Association 46 (1957) 208-209
10. Fedele E., and Raiteri M. In vivo studies of the cerebral glutamate receptor/NO/cGMP pathway. Progress in Neurobiology 58 (1999) 89-120
11. Garthwaite J., Charles S.L., and Chess-Williams R. Endothelium-derived relaxing factor release on activation of NMDA receptors suggests role as intercellular messenger in the brain. Nature 336 (1988) 385-388
12. Gomeza J., Hulsmann S., Ohno K., Eulenburg V., Szoke K., Richter D., and Betz H. Inactivation of the glycine transporter 1 gene discloses vital role of glial glycine uptake in glycinergic inhibition. Neuron 40 (2003) 785-796
13. Hamelmann E., Schwarze J., Takeda K., Oshiba A., Larsen G.L., Irvin C.G., and Gelfand E.W. Non-invasive measurement of airway responsiveness in allergic mice using barometric plethysmography. American Journal of Respiratory and Critical Care Medicine 156 (1997) 766-775
14. Harsing L.G., Juranyi Z., Gacsalyi I., Tapollcsanyi P., Czompa A., and Matyus P. Glycine transporter type-1 and its inhibitors. Current Medicinal Chemistry 13 (2006) 1017-1044
15. Heresco-Levy U. Glutamatergic neurotransmission modulation and the mechanism of antipsychotic atypicality. Progress in Neuropsychopharmacology 27 (2003) 1113-1123
16. Javitt D.C., and Zukin S.R. Recent advances in the phencyclidine model of schizophrenia. American Journal of Psychiatry 151 (1991) 1301-1308
17. Javitt D.C. Is the glycine site half saturated or half unsaturated? Effects of glutamatergic drugs in schizophrenia patients. Current Opinion in Psychiatry 19 (2006) 151-157
18. Johnson K., Clemens-Smith A., Nomikos G., Davis R., Phebus L., Shannon H., Love P., Perry K., Katner J., Bymaster F., Yu H., and Hoffman B. Annals of the New York Academy of Sciences 1003 (2003) 412-414
19. Jursky F., Tamura S., Tamura A., Madiyan S., Nelson H., and Nelson N. Journal of Experimental Biology 196 (1994) 283-295
20. Kinney G., Sur C., Burno M., Mallorga P.J., Williams J.B., Figueros D.J., Wittmann M., Lemaire W., and Conn P.J. The glycine transporter type 1 inhibitor N-[3-(4′-fluorophenyl)-3(4″-phenylphenoxy)propyl]sarcosine potentiates NMDA receptor-mediated responses in vivo and produces an antipsychotic profile in rodent behavior. Journal of Neuroscience 23 (2003) 7586-7591
21. Kinney G.G., and Sur C. Glycine site modulators and glycine transporter-1 inhibitors as novel therapeutic targets for schizophrenia. Current Neuropharmacology 3 (2005) 35-43
22. Knauber J., Kischka U., Roth M., Schmidt W.J., Hennerici M., and Fassbender K. Modulation of striatal acetylcholine concentrations by NMDA and the competitive NMDA receptor-antagonist AP-5: an in vivo microdialysis study. Journal of Neural Transmission 106 (1999) 35-45
23. Koch S., Perry K.W., Nelson D.L., Conway R.G., Threlkeld P.G., and Bymaster F.P. R-fluoxetine increases extracellular DA, NE, as well as 5-HT in rat prefrontal cortex and hypothalamus: an in vivo microdialysis and receptor binding study. Neuropsychopharmacology 27 (2002) 949-959
24. Krystal J.H., Karper L.P., Seibyl J.P., Freeman G.K., Delaney R., Bremner J.D., Heninger G.R., Bowers Jr. M.B., and Charney D.S. Subanesthetic effects on the noncompetitive NMDA antagonist ketamine in human. Psychotomimetic, perceptual, cognitive and neuroendocrine responses. Archives of General Psychiatry 51 (1994) 199-214
25. Legendre P. The glycinergic inhibitory synapse. Cellular and Molecular Life Science 58 (2001) 760-793
26. Lipina T., Labrie V., Weiner I., and Roder J. Modulators of the glycine site on NMDA receptors, d-serine and ALX5407, display similar beneficial effects onto clozapine in mouse models of schizophrenia. Psychopharmacology 179 (2005) 54-67
27. Lieberman J.A., Stroup T.S., McEvoy J.P., Swartz M.S., Rosenheck R.A., Perkins D.O., Keefe R.S., Davis S.M., Davis C.E., Lebowitz B.D., Severe J., and Hsiao J.K. Clinical antipsychotic trials of intervention effectiveness (CATIE) investigators. Effectiveness of antipsychotic drugs in patients with chronic schizophrenia. New England Journal of Medicine 353 (2005) 1209-1223
28. Man, T., Milot, G., Porter, W.J., Reel, J.K., Rudyk, H.C.E, Valli, M.J., Walter, M.W., 2005. 2-Aryloxyethyl Glycine Derivatives and Their Use as Glycine Transport Inhibitors. International Patent Application, WO 2005/100301.
29. Millan M.J. N-Methyl-d-aspartate receptors as a target for improved antipsychotic agents: novel insights and clinical perspectives. Psychopharmacology 179 (2005) 30-53
30. Ohno M., Rai I., and Watanabe S. N-Methyl-d-aspartate stimulates dopamine through nitric oxide formation in the nucleus accumbens of rats. Brain Research 699 (1995) 332-335
31. Paxinos G., and Watson C. The Rat Brain in Stereotaxic Coordinates (1986), Academic Press, San Diego
32. Tingley III, F.D., Lebel, L.A., Lebel, Lu Y., Harms, J.F., Ward, K.M., Strick, C.A., Fisher, K.E., Wong, S., McHardy, S., Sakya, S.M., Schmidt, C.J., 2005. The Piperidinebenzamide, PF-3, 311945, is a Selective Antagonist of the GlyT-1 Transporter in Rodents. Society for Neuroscience Meeting, Washington DC, Abstract # 1022.4.
33. Tsai G., and Coyle J.T. Glutamatergic mechanisms in schizophrenia. Annual Reviews of Pharmacology and Toxicology 42 (2001) 165-179
34. Tsai G., Lane H.Y., Yang P., Chong M.Y., and Lange N. Glycine transporter 1 inhibitor, N-methylglycine (sarcosine), added to antipsychotics for the treatment of schizophrenia. Biological Psychiatry 55 (2004) 452-456
35. Tsai G., Ralph-Williams R.J., Marzia M., Bergeron R., Berger-Sweeney J., Dunham K.S., Jiang Z., Caine B., and Coyle J.T. Gene knockout of glycine transporter 1: characterization of the behavioral phenotype. Proceedings of the National Academy of Sciences 101 (2004) 8485-8490
36. Tzavara E.T., Davis R.J., Perry K.W., Li X., Salhoff C., Bymaster F.P., Witkin J.M., and Nomikos G.G. The CB1 receptor antagonist SR141716A selectively increases monoaminergic neurotransmission in the medial prefrontal cortex: implications for therapeutic actions. British Journal of Pharmacology 138 (2003) 544-553
37. Walter M.W., Hoffman B.J., Gordon K., Johnson K.W., Love P.L., Jones M., Man T., Phebus L., Reel J.K., Rudyk H., Shannon H.E., Svensson K.A., Yu H., Valli M., and Porter W.J. Discovery and SAR of novel GlyT1 inhibitors. Bioorganic Medicinal Chemistry Letters (2007) 10.1016/j.bmcl.2007.06.074
38. Zafra F., Gomeza J., Olivares L., Aragon C., and Gimenez C. Regional distribution and developmental variation of the glycine transporters GLYT1 and GYT2 in the rat CNS. European Journal of Neuroscience 7 (1995) 1342-1352