Pharmacological characterisation of the GlyT-1 glycine transporter using two novel radioligands

Neuropharmacology

Volumn 59, Issue 6, 2010, Pages 558-565

  Herdon, Hugh J ^a   Roberts, Jennifer C ^a   Coulton, Steve ^a   Porter, Rod A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Glycine transporter; GlyT 1; Human brain; Radioligand binding; Rat brain

Indexed keywords

GLYCINE TRANSPORTER 1; GSK 931145; GSK 931145 H 3; PROTEIN INHIBITOR; SB 733993; SB 733993 H 3; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN CORTEX; CELL MEMBRANE; CONTROLLED STUDY; DISSOCIATION; DRUG ACTIVITY; DRUG POTENTIATION; DRUG PROTEIN BINDING; DRUG STRUCTURE; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN TISSUE; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; BINDING SITES; BINDING, COMPETITIVE; BRAIN; GLYCINE PLASMA MEMBRANE TRANSPORT PROTEINS; HEK293 CELLS; HUMANS; MALE; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY;

EID: 77956942872     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2010.07.023     Document Type: Article

References (27)

1. 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. 2001, 134:1429-1436.
2. Betz H., Laube B. Glycine receptors: recent insights into their structural organization and functional diversity. J. Neurochem 2006, 97:1600-1610.
3. Boulay D., Pichat P., Dargazanli G., Estenne-Bouhtou G., Terranova J.P., Rogacki N., Stemmelin J., Coste A., Lanneau C., Desvignes C., Cohen C., Alonso R., Vigé X., Biton B., Steinberg R., Sevrin M., Oury-Donat F., George P., Bergis O., Griebel G., Avenet P., Scatton B. Characterization of SSR103800, a selective inhibitor of the glycine transporter-1 in models predictive of therapeutic activity in schizophrenia. Pharmacol. Biochem. Behav. 2008, 91:47-58.
4. Bradford M.M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein dye binding. Anal. Biochem. 1976, 72:248-254.
5. Bridges T.M., Williams R., Lindsley C.W. Design of potent GlyT1 inhibitors: in vitro and in vivo profiles. Curr. Opin. Mol. Therapeut 2008, 10:591-601.
6. Coyle J.T., Tsai G. The NMDA receptor glycine modulatory site: a therapeutic target for improving cognition and reducing negative symptoms in schizophrenia. Psychopharmacology 2004, 174:32-38.
7. Depoortère R., Dargazanli G., Estenne-Bouhtou G., Coste A., Lanneau C., Desvignes C., Poncelet M., Heaulme M., Santucci V., Decobert M., Cudennec A., Voltz C., Boulay D., Terranova J.P., Stemmelin J., Roger P., Marabout B., Sevrin M., Vigé1 X., Biton B., Steinberg R., Françon D., Alonso R., Avenet P., Oury-Donat F., Perrault G., Griebel G., George P., Soubrié P., Scatton B. Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic. Neuropsychopharmacol 2005, 30:1963-1985.
8. Furukawa H., Singh S.K., Mancusso R., Gouaux E. Subunit arrangement and function in NMDA receptors. Nature 2005, 438:185-192.
9. Ge J., Hamilton M., Shahid D. The effects of Org 25935 on the extracellular levels of glycine in brain regions of freely moving rats using microdialysis. Br. J. Pharmacol. 2001, 133:135.
10. Gilfillan R., Kerr J., Walker G., Wishart G. Glycine transporters and their inhibitors. Top. Med. Chem. 2009, 4:223-247.
11. Gozzi A., Herdon H., Schwarz A., Bertani S., Crestan V., Turrini G., Bifone A. Pharmacological stimulation of NMDA receptors via co-agonist site suppresses fMRI response to phencyclidine in the rat. Psychopharmacol. 2008, 201:273-284.
12. 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. 2001, 41:88-96.
13. Javitt D.C. Glycine transport inhibitors for the treatment of schizophrenia: symptom and disease modification. Curr. Opin. Drug Discov. Devel. 2009, 12:468-478.
14. Kohr G. NMDA receptor function: subunit composition versus spatial distribution. Cell Tissue Res. 2006, 326:439-446.
15. Lipina T., Labrie V., Weiner I., Roder J. Modulators of the glycine site on NMDA receptors, D-serine and ALX 5407, display similar beneficial effects to clozapine in mouse models of schizophrenia. Psychopharmacol. 2005, 179:54-67.
16. Lisman J.E., Coyle J.T., Green R.W., Javitt D.C., Benes F.M., Heckers S., Grace A.A. Circuit-based framework for understanding neurotransmitter and risk gene interactions in schizophrenia. Trends Neurosci. 2008, 31:234-242.
17. Mallorga P.J., Williams J.B., Jacobson M., Marques R., Chaudhary A., Conn P.J., Pettibone D.J., Sur C. Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4′-fluorophenyl)-3-(4′phenylphenoxy)propyl]) sarcosine. Neuropharmacol. 2003, 45:585-593.
18. Mezler M., Hornberger W., Mueller R., Amberg M.S.W., Braje W., Ochse M., Schoemaker H., Behl B. Inhibitors of GlyT1 affect glycine transport via discrete binding sites. Mol. Pharmacol. 2008, 74:1705-1715.
19. 11C]GSK931145 as a novel ligand for imaging the type 1 glycine transporter with positron emission tomography. Synapse 2010, 64:542-549.
20. Rahman S.S., Coulton S., Herdon H.J., Joiner G.F., Jin J., Porter R.A. 1,3-Diaminopropan-2-ol Sulfonamides as potent and selective inhibitors of the glycine transporter type 1. Bioorg. Med. Chem. Lett. 2007, 17:1741-1745.
21. 3H]Resiniferatoxin autoradiography in the CNS of wild-type and TRPV1 null mice defines TRPV1 (VR-1) protein distribution. Brain Res. 2004, 995:176-183.
22. Shim S.S., Hammonds M.D., Kee B.S. Potentiation of the NMDA receptor in the treatment of schizophrenia: focused on the glycine site. Eur. Arch. Psychiat. Clin. Neurosci. 2007, 258:16-27.
23. Sur C., Kinney G.G. Glycine transporter 1 inhibitors and modulation of NMDA receptor-mediated excitatory neurotransmission. Curr. Drug Targets. 2007, 8:643-649.
24. Tsai G.E., Lim P.Y. Strategies to enhance N-methyl-D-aspartate receptor mediated neurotransmission in schizophrenia, a critical review and meta-analysis. Curr. Pharmaceut. Design. 2010, 16:522-537.
25. Webb T.I., Lynch J.W. Molecular pharmacology of the glycine receptor chloride channel. Curr. Pharmaceut. Design. 2007, 13:2350-2367.
26. Yang C.R., Svensson K.A. Allosteric modulation of NMDA receptor via elevation of brain glycine and D-serine: the therapeutic potentials for schizophrenia. Pharmacol. Therapeut. 2008, 120:317-332.
27. Zeng Z., O'Brien J.A., Lemaire W., O'Malley S.S., Miller P.J., Zhao Z., Wallace M.A., Raab C., Lindsley C., Sur C., Williams D.L. A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies. Nucl. Med. Biol. 2008, 35:315-325.