Pharmacology and expression analysis of glycine transporter GlyT1 with [ 3H]-(N-[3-(4′-fluorophenyl)-3-(4′phenylphenoxy)propyl]) sarcosine

Neuropharmacology

Volumn 45, Issue 5, 2003, Pages 585-593

  Mallorga, Pierre J ^a   Williams, Jacinta B ^a   Jacobson, Marlene ^a   Marques, Rosemary ^a   Chaudhary, Ashok ^a   Conn, P Jeffrey ^a   Pettibone, Douglas J ^a   Sur, Cyrille ^a,b  

^a MERCK RESEARCH LABORATORIES   (United States)

^b VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Brain expression; Glycine; Non competitive inhibition; Rat; Transporter; Uptake

Indexed keywords

ALX 5407; AMINO ACID TRANSPORTER; CHLORIDE; GLYCINE; GLYCINE TRANSPORTER; ION; SARCOSINE; SODIUM; UNCLASSIFIED DRUG; [N [3 (4' FLUOROPHENYL) 3 (4' PHENYLPHENOXY)PROPYL]]SARCOSINE;

AMINO ACID TRANSPORT; ARTICLE; BINDING SITE; CENTRAL NERVOUS SYSTEM; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG BINDING; FOREBRAIN; HUMAN; HUMAN CELL; IC 50; ISOTOPE LABELING; KINETICS; NONHUMAN; NUCLEOTIDE SEQUENCE; POPULATION; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT;

EID: 0041488749     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(03)00227-2     Document Type: Article

References (37)

1. Aprison M.H. The discovery of the neurotransmitter role of glycine. Ottersen O.P., Storm-Mathisen J. Glycine Neurotransmission. 1990;1-23 John Wiley and Sons.
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., Klitenick M.A. ALX 5407: A potent, selective inhibitor of the hGlyT1 glycine transporter. Mol Pharmacol 60. 60:2001;1414-1420.
3. Atwell D., Barbour B., Szatkowski M. Nonvesicular release of neurotransmitter. Neuron. 11:1993;401-407.
4. Aubrey K.R., Vandenberg R.J. N[3-(4'-fluorophenyl)-3(4'-phenylphenoxy)propyl]sarcosine (NFPS) is a selective persistent inhibitor of glycine transport. Br J Pharmacol. 134:2001;1429-1436.
5. Aubrey K.R., Mitrovic A.D., Vandenberg R.J. Molecular basis for proton regulation of glycine transport by glycine transporter subtype 1b. Mol Pharmacol. 58:2000;129-135.
6. Berger A.J., Dieudonne S., Ascher P. Glycine uptake governs glycine site occupancy at NMDA receptors of excitatory synapses. J Neurophysiol. 80:1998;3336-3340.
7. Bergeron R., Meyer T.M., Coyle J.T., Greene R.W. Modulation of N-methyl-D-aspartate receptor function by glycine transport. PNAS USA. 95:1998;15730-15734.
8. Betz H. Ligand-gated ion channels in the brain: the amino acid receptor superfamilly. Neuron. 5:1990;383-392.
9. Borowsky B., Mezey E., Hoffman B.J. Two glycine transporter variants with distinct localization in the CNS and peripheral tissues are encoded by a common gene. Neuron. 10:1993;851-863.
10. Brown A., Carlyle I., Clark J., Hamilton W., Gibson S., McGarry G., McEachen S., Rae D., Thorn S., Walker G. Discovery and SAR of Org 24598-A selective glycine uptake inhibitor. Bioorg Med Chem Lett. 11:2001;2007-2009.
11. Chen L., Mulhauser M., Yang C.R. Glycine transporter-1 blockade potentiates NMDA mediated responses in rat prefrontal cortical neurons in vitro and in vivo. J Neurophysiol. 89:2003;691.
12. 3H]imipramine. J Pharmacol Exp Ther. 242:1987;364-371.
13. Danysz W., Parsons A.C.G. Glycine and N-methyl-D-aspartate receptors: physiological significance and possible therapeutic applications. Pharmacol Rev. 50:1998;597-664.
14. Grimwood S., LeBourdelles B., Atack J.R., Barton C., Cockett W., Cook S.M., Gilbert E., Hutson P.H., McKernan R.M., Myers J., Ragan C.I., Wingrove P.B., Whiting P.J. Generation and characterisation of stable cell lines expressing recombinant human N-methyl-D-aspartate receptor subtypes. J Neurochem. 66:1996;2239-2247.
15. Herdon H.J., Godfrey F.M., Brown A.M., Coulton S., Evans J.R., Cairns W.J. Pharmacological assessment of the role of the glycine transporter GlyT-1 in mediating high-affinity glycine uptake by rat cerebral cortex and cerebellum synaptosomes. Neuropharmacol. 41:2001;88-96.
16. Heresco-Levy U., Javitt D.C., Ermilov M., Mordel C., Horowitz A., Kelly D. Double blind, placebo-controlled, crossover trial of glycine adjuvant therapy for treatment-resistant schizophrenia. Br J Psychiatry. 169:1996;610-617.
17. Heresco-Levy U. N-methyl-D-aspartate (NMDA) receptor-based treatment approaches in schizophrenia: the first decade. Int J Neuropsychopharmacol. 3:2000;243-258.
18. Hollmann M., Heinemann S. Cloned glutamate receptors. Annu Rev Neurosci. 17:1994;31-108.
19. Javitt D.C., Zylberman I., Zukin S.R., Heresco-Levy U., Lindenmayer J.P. Amelioration of negative symptoms in schizophrenia by glycine. Am J Psychiatry. 151:1994;1234-1236.
20. Johnson J.W., Ascher P. Glycine potentiates the NMDA response in cultured mouse brain neurons. Nature. 325:1987;529-531.
21. Kim K.M., Kingsmore S.F., Han H., Yang-Feng T.L., Godinot N., Seldin M.F., Caron M.G., Giros B. 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.
22. Kinney G.G., Sur C., Burno M., Wittmann M., Mallorga P.J., Conn P.J. Effect of glycine transport type-1 (GlyT1) inhibitors on phencyclidine and amphetamine induced hyperlocomotion in BALB/c mice. Fed Eur Neurosc Soc Abstr. 1:2002;16. A084.
23. Liu Q.-R., Lopez-Corcuera B., Mandiyan S., Nelson H., Nelson N. Cloning and expression of a spinal cord- and brain-specific glycine transporter with novel structural features. J Biol Chem. 268:1993;22802-22808.
24. Liu W., Leibach F.H., Ganapathy V. Characterization of the glycine transport system GLYT1 in human placental choriocarcinoma cells (JAR). Biochim Biophys Acta. 1194:1994;176-184.
25. Matsui T., Sekiguchi M., Hashimoto A., Tomita U., Nishikawa T., Wada K. Functional comparison of D-serine and glycine in rodents: the effect on cloned NMDA receptors and the extracellular concentration. J Neurochem. 65:1995;454-458.
26. Morrow J.A., Collie I.T., Dunbar D.R., Walker G.B., Shahid M., Hill D.R. Molecular cloning and functional expression of the human glycine transporter GlyT2 and chromosomal localisation of the gene in the human genome. FEBS Lett. 439:1998;334-340.
27. - neurotransmitter transporters. J Neurochem. 71:1998;1785-1803.
28. Nunez E., Lopez-Corcuera B., Vazquez J., Gimenez C., Aragon C. Differential effects of the tricyclic antidepressant amoxapine on glycine uptake mediated by the recombinant GLYT1 and GLYT2 glycine transporter. Br J Pharmacol. 129:2000;200-206.
29. A receptors which contain the α5 subunit. Neuropharmacol. 35:1996;1331-1335.
30. Rothman R.B., Carroll F.I., Morales M., Rowley D.L., Rice K.C., Dersch C.M., Donovan D.M. Studies of the biogenic amine transporters. 10. Characterization of a novel cocaine binding site in brain membranes prepared from dopamine transporter knockout mice. Synapse. 44:2002;94-105.
31. Roux M.J., Supplisson S. Neuronal and glial glycine transporters have different stoichiometries. Neuron. 25:2000;373-383.
32. Smith K.E., Borden L.A., Hartig P.R., Branchek T., Weinsbank R.L. Cloning and expression of a glycine transporter reveal colocalization with NMDA receptors. Neuron. 8:1992;927-935.
33. Supplisson S., Bergman C. Control of NMDA receptor activation by a glycine transporter co-expressed in xenopus oocyte. J Neurosci. 17:1997;4580-4590.
34. A receptor subtype in the brain is not lethal in mice. J Neurosci. 21:2001;3409-3418.
35. Vandenberg R.J., Aubrey K.R. Glycine transport inhibitors as potential antipsychotic drugs. Exp Opin Ther Targ. 5:2001;507-518.
36. Zafra F., Aragon C., Olivares L., Danbolt N.C., Gimenez C., Storm-Mathisen J. Glycine transporters are differentially expressed among CNS cells. J Neurosci. 15:1995;3952-3969.
37. Zafra F., Gomeza J., Olivares L., Aragon C., Gimenez C. Regional distribution and developmental variation of the glycine transporters GLYT1 and GLYT2 in the rat CNS. Eur J Neurosci. 7:1995;1342-1352.