Inhibitors of GlyT1 affect glycine transport via discrete binding sites

Molecular Pharmacology

Volumn 74, Issue 6, 2008, Pages 1705-1715

  Mezler, Mario ^a   Hornberger, Wilfried ^a   Mueller, Reinhold ^a   Amberg, Martin Schmidt Willi ^a   Braje, Wilfried ^a   Ochse, Michael ^a   Schoemaker, Hans ^a   Behl, Berthold ^a  

^a ABBOTT GMBH AND CO KG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 CHLORO N [ALPHA (2 PIPERIDINYL)BENZYL] 3 TRIFLUOROMETHYLBENZAMIDE; ALX 5407; GLYCINE; GLYCINE DERIVATIVE; GLYCINE TRANSPORTER 1; N [3 (4' FLUOROPHENYL) 3 (4' PHENYLPHENOXY)PROPYL]SARCOSINE; N [3 PHENYL 3 [4' (4 TOLUOYL)PHENOXY]PROPYL]SARCOSINE; N METHYL N [(4 TRIFLUOROMETHYL)PHENOXY] 3 PHENYLPROPYLGLYCINE; ORG 24589; UNCLASSIFIED DRUG;

AMINO ACID TRANSPORT; ANIMAL CELL; ARTICLE; CELL MEMBRANE TRANSPORT; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG BINDING SITE; LIGAND BINDING; NONHUMAN; OOCYTE; PRIORITY JOURNAL; TRANSPORT KINETICS; XENOPUS LAEVIS;

ANIMALS; ASTROCYTES; BENZAMIDES; BINDING SITES; BINDING, COMPETITIVE; BIOLOGICAL TRANSPORT; CELL LINE; CRICETINAE; CRICETULUS; FEMALE; GLYCINE; GLYCINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MICE; MICE, INBRED C57BL; OOCYTES; PATCH-CLAMP TECHNIQUES; PIPERIDINES; RADIOLIGAND ASSAY; RECOMBINANT PROTEINS; SARCOSINE; STRUCTURE-ACTIVITY RELATIONSHIP; XENOPUS LAEVIS;

EID: 57349195659     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.108.049312     Document Type: Article

References (42)

1. Atkinson BN, Bell SC, De Vivo M, Kowalski LR, Lechner SM, Ognyanov VI, Tham CS, Tsai C, Jia J, Ashton D, and Klitenick MA (2001) ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. Mol Pharmacol 60:1414-1420.
2. Aubrey KR and Vandenberg RJ (2001) N[3-(4′-fluorophenyl)-3- (4′-phenylphenoxy) propyl]sarcosine (NFPS) is a selective persistent inhibitor of glycine transport. Br J Pharmacol 134:1429-1436.
3. Aubrey KR, Vandenberg RJ, and Clements JD (2005) Dynamics of forward and reverse transport by the glial glycine transporter, glyt1b. Biophys J 89:1657-1668.
4. Bergeron R, Meyer TM, Coyle JT, and Greene RW (1998) Modulation of N-methyl-D-aspartate receptor function by glycine transport. Proc Natl Acad Sci U S A 95:15730-15734.
5. Betz H, Gomeza J, Armsen W, Scholze P, and Eulenburg V (2006) Glycine transporters: essential regulators of synaptic transmission. Biochem Soc Trans 34:55-58.
6. Chen L, Muhlhauser M, and Yang CR (2003) Glycine tranporter-1 blockade potentiates NMDA-mediated responses in rat prefrontal cortical neurons in vitro and in vivo. J Neurophysiol 89:691-703.
7. Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
8. Coyle JT (2006) Glutamate and Schizophrenia: Beyond the Dopamine Hypothesis. Cell Mol Neurobiol 26:365-384.
9. Cubelos B, Giménez C, and Zafra F (2005) Localization of the GLYT1 glycine transporter at glutamatergic synapses in the rat brain. Cereb Cortex 15:448-459.
10. Dargazanli G, Estenne-Bouhtou G, Magat P, Marabout B, Medaisko F, Roger P, Sevrin M, and Veronique C (2003), inventors; Sanofi-Aventis, Dargazanli G, Estenne-Bouhtou G, Magat P, Marabout B, Medaisko F, Roger P, Sevrin M, and Veronique C, assignees. Derivatives of N-[phenyl(piperidin-2-yl)methyl] benzamide, the preparation method thereof and application of same in therapeutics. World Patent no. WO2003089411. 2003 Oct 30.
11. De Lean A, Hancock AA, and Lefkowitz RJ (1982) Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. Mol Pharmacol 21:5-16.
12. Depoortère R, Dargazanli G, Estenne-Bouhtou G, Coste A, Lanneau C, Desvignes C, Poncelet M, Heaulme M, Santucci V, Decobert M, et al. (2005) Neurochemical, electrophysiological and pharamcological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic. Neuropsychopharmacology 30:1963-1985.
13. Harrison PJ and Weinberger DR (2005) Schizophrenia genes, gene expression, and neuropathology: on the matter of their convergence. Mol Psychiatry 10:40-68.
14. Harsing LG Jr, Gacsalyi I, Szabo G, Schmidt E, Sziray N, Sebban C, Tesolin-Decros B, Matyus P, Egyed A, Spedding M, et al. (2003) The glycine transporter-1 inhibitors NFPS and Org 24461: a pharmacological study. Pharmacol Biochem Behav 74:811-825.
15. Harsing LG Jr, Juranyi Z, Gacsalyi I, Tapolcsanyi P, Czompa A, and Matyus P (2006) Glycine transporter type-1 and its inhibitors. Curr Med Chem 13:1017-1044.
16. Javitt DC and Zukin SR (1991) Recent advances in the phencyclidine model of schizophrenia. Am J Psychiatry 148:1301-1308.
17. M, Kingsmore SF, Han H, Yang-Feng TL, Godinot N, Seldin MF, Caron MG, and Giros B (1994) 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 45:608-617.
18. Kinney GG, Sur C, Burno M, Mallorga PJ, Williams JB, Figueroa DJ, Wittmann M, Lemaire W, and Conn PJ (2003) The glycine transporter type 1 inhibitor N-[3-(4-fluorophenyl)-3-(4-phenylphenoxy)propyl]sarcosine potentiates NMDA receptormediated responses in vivo and produces an antipsychotic profile in rodent behavior. J Neurosci 23:7586-7591.
19. Lahti AC, Koffel B, LaPorte D, and Tamminga CA (1995) Subanesthetic doses of ketamine stimulate psychosis in schizophrenia. Neuropsychopharmacology 13:9-19.
20. Lazareno S and Birdsall NJ (1993) Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng-Prusoff equations. Br J Pharmacol 109:1110-1119.
21. Lechner SM (2006) Glutamate-based therapeutic approaches: inhibitors of glycine transport. Curr Opin Pharmacol 6:75-81.
22. + channel determined by construction of multimeric cDNAs. Neuron 9:861-871.
23. Lindsley CW, Wolkenberg SE, and Kinney GG (2006) Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors. Curr Top Med Chem 6:1883-1896.
24. Lowe JA (2002), inventor; Lowe JA, and Pfizer Inc., assignees. Benzophenones and sulfones as inhibitors of glycine uptake. World Patent no. WO2002000602. 2002 Jan 3.
25. 3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter. Bioorg Med Chem Lett 13:1291-1292.
26. 3H]-(N-[3-(4′-fluorophenyl)-3- (4′phenylphenoxy)propyl])-sarcosine. Neuropharmacology 45:585-593.
27. Methfessel C, Witzemann V, Takahashi T, Mishina M, Numa S, and Sakmann B (1986) Patch clamp measurements on Xenopus laevis oocytes: currents through endogenous channels and implanted acetylcholine receptor and sodium channels. Pflugers Arch 407:577-588.
28. Mezler M, Müller T, and Raming K (2001) Cloning and functional expression of GABA(B) receptors from Drosophila. Eur J Neurosci 13:477-486.
29. Millan MJ (2005) N-Methyl-D-aspartate receptors as a target for improved antipsychotic agents: novel insights and clinical perspectives. Psychopharmacology 179: 30-53.
30. Morris BJ, Cochran SM, and Pratt JA (2005) PCP: from pharmacology to modelling schizophrenia. Curr Opin Pharmacol 5:101-106.
31. Morrison PD and Pilowsky LS (2007) Schizophrenia: more evidence for less glutamate. Expert Rev Neurother 7:29-31.
32. Munson PJ and Rodbard D (1980) Ligand: a versatile computerized approach for characterization of ligand-binding systems. Anal Biochem 107:220-239.
33. Núñez E, Martínez-Maza R, Geerlings A, Aragón C, and López-Corcuera B (2005) Transmembrane domains 1 and 3 of the glycine transporter GLYT1 contain structural determinants of N[3-(4′-fluorophenyl)-3-(4′-phenylphenoxy)-propyl]sarcosine specificity. Neuropharmacology 49:922-934.
34. Roux MJ and Supplisson S (2000) Neuronal and glial glycine transporters have different stoichiometries. Neuron 25:373-383.
35. Sanderson DJ and Bannerman DM (2007) Supersmart mice: surprising or surprised? Theoretical comment on Singer, Boison, Möhler, Feldon, and Yee. Behav Neurosci 121:1137-1139.
36. Singer P, Boison D, Möhler H, Feldon J, and Yee BK (2007) Enhanced recognition memory following glycine transporter 1 deletion in forebrain neurons. Behav Neurosci 121:815-825.
37. Soriano FX, Papadia S, Hofmann F, Hardingham NR, Bading H, and Hardingham GE (2006) Preconditioning doses of NMDA promote neuroprotection by enhancing neuronal excitability. J Neurosci 26:4509-4518.
38. Supplisson S and Roux MJ (2002) Why glycine transporters have different stoichiometries. FEBS Lett 529:93-101.
39. Szabo L (2005) Differential effect of GlyT1 inhibitors on the development of ischemic cerebral infarction. International Symposium on Cerebral Blood Flow, Metabolism and Function. J Cereb Blood Flow Metab 25:S15.
40. Vandenberg RJ (2006) Mutational analysis of glutamate transporters. Handb Exp Pharmacol 175:113-135.
41. Yee BK, Balic E, Singer P, Schwerdel C, Grampp T, Gabernet L, Knuesel I, Benke D, Feldon J, Mohler H, et al. (2006) Disruption of glycine transporter 1 restricted to forebrain neurons is associated with a procognitive and antipsychotic phenotypic profile. J Neurosci 26:3169-3181.
42. Zhang SJ, Steijaert MN, Lau D, Schütz G, Delucinge-Vivier C, Descombes P, and Bading H (2007) Decoding NMDA receptor signaling: identification of genomic programs specifying neuronal survival and death. Neuron 53:549-562.