Modulation of NMDA receptors by glycine - Introduction to some basic aspects and recent developments

Amino Acids

Volumn 14, Issue 1-3, 1998, Pages 207-216

  Parsons, C G ^a   Danysz, W ^a   Hesselink, M ^a   Hartmann, S ^a   Lorenz, B ^a   Wollenburg, C ^a   Quack, G ^a  

^a MERZ PHARMACEUTICALS GMBH   (Germany)

Author keywords

Antagonists; Desensitisation; Glycine site; NMDA receptors; Partial agonists; Subtypes

Indexed keywords

3 AMINO 1 HYDROXY 2 PYRROLIDINONE; ANTICONVULSIVE AGENT; ANXIOLYTIC AGENT; CYCLOSERINE; GLUTAMIC ACID; GLYCINE; MAGNESIUM; MDL 100458; MDL 102288; MRZ 2570; MRZ 2571; MRZ 2576; N METHYL DEXTRO ASPARTIC ACID; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; N METHYL DEXTRO ASPARTIC ACID RECEPTOR STIMULATING AGENT; NEUROLEPTIC AGENT; NEUROPROTECTIVE AGENT; POLYAMINE; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

BINDING SITE; CHRONIC PAIN; CONFERENCE PAPER; INJURY; ISCHEMIA; NERVE DEGENERATION; NONHUMAN; PRIORITY JOURNAL; PSYCHOSIS; RECEPTOR AFFINITY; RECEPTOR DOWN REGULATION;

ANIMALS; GLYCINE; HUMANS; RECEPTORS, N-METHYL-D-ASPARTATE;

EID: 0031985974     PISSN: 09394451     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF01345264     Document Type: Conference Paper

References (87)

1. Alghoul WM, Meeker RB, Greenwood (1997) Differential expression of five N-methyl-D-aspartate receptor subunit mRNAs in vasopressin and oxytocin neuroendocrine cells. Mol Brain Res 44: 262-272
2. Baran H, Loscher W, Mevissen M (1994) The glycine/NMDA receptor partial agonist D-cycloserine blocks kainate-induced seizures in rats. Comparison with MK-801 and diazepam. Brain Res 652: 195-200
3. Baron BM, Harrison BL, McDonald IA, Meldrum BS, Palfreyman MG, Salituro FG, Siegel BW, Slone AL, Turner JP, White HS (1992) Potent indoleline and quinolinecontaining N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site. J Pharmacol Exp Ther 262: 947-956
4. Berger P, Parrel D, Sharp F, Skolnick P (1994) Drugs acting at the strychnine-insensitive glycine receptor do not induce HSP-70 protein in the cingulate cortex. Neurosci Lett 168: 147-150
5. Bordi F, Pietra C, Ziviani L, Reggiani A (1997) The glycine antagonist GV 150526 protects somatosensory evoked potentials and reduces the infarct area in the MCAo model of focal ischemia in the rat. Exp Neurol 145: 425-433
6. Bristow LJ, Landon L, Saywell KL, Tricklebank MD (1995) The glycine/NMDA receptor antagonist, L-701,324 reverses isolation-induced deficits in prepulse inhibition in the rat. Psychopharmacology 118: 230-232
7. Bristow LJ, Flatman KL, Hutson PH, Kulagowski JJ, Leeson PD, Young L, Tricklebank MD (1996) The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents. J Pharmacol Exp Ther 277: 578-585
8. Bubser M, Keseberg U, Notz PK, Schmidt WJ (1992) Differential behavioural and neurochemical effects of competitive and non-competitive NMDA receptor antagonists in rats. Eur J Pharmacol 229: 75-82
9. Carling RW, Leeson PD, Moseley AM, Smith JD, Saywell K, Tricklebank MD, Kemp JA, Marshall GR, Foster AC, Grimwood S (1993) Anticonvulsant activity of glycine-siteNMDA antagonists. 2. Trans 2-carboxy-4-substituted tetrahydroquinolines. Bioorg Med Chem Lett 3: 65-70
10. Carter AJ (1992) Glycine antagonists: regulation of the NMDA receptor-channel complex by the strychnine-insensitive glycine site. Drugs Future 17: 595-613
11. Chapman AG, Durmuller N, Harrison BL, Baron BM, Parvez N, Meldrum BS (1995) Anticonvulsant activity of a novel NMDA/glycine site antagonist, MDL 104,653, against kindled and sound-induced seizures. Eur J Pharmacol 274: 83-88
12. Chen J, Graham S, Moroni F, Simon R (1993) A study of the dose dependency of a glycine receptor antagonist in focal ischemia. J Pharmacol Exp Ther 267: 937-941
13. Chiamulera C, Costa S, Reggiani A (1990) Effect of NMDA-insensitive and strychnine-insensitive glycine site antagonists on NMDA-mediated convulsions and learning. Psychopharmacology 102: 551-553
14. Chouinard ML, Gaitan D, Wood PL (1993) Presence of the N-methyl-D-aspartate-associated glycine receptor agonist, D-serine, in human temporal cortex-comparison of normal, Parkinson, and Alzheimer tissues. J Neurochem 61: 1561-1564
15. Danysz W, Wroblewski JT, Brooker G, Costa E (1987) Modulation of excitatory amino acid transmission by phencyclidine and glycine in the rat cerebellum in vivo. Soc Neurosci Abs 13:383
16. Danysz W, Ebmann U, Bresink I, Wilke R (1994) Glutamate antagonists have different effects on spontaneous locomotor activity in rats. Pharmacol Biochem Behav 48:111-118
17. Danysz W, Parsons CG, Bresink I, Quack G (1995) Glutamate in CNS disorders: a revived target for drug development? Drug News Perspect 8: 261-277
18. Danysz W, Parsons CG, Karcz-Kubicha M, Gold M, Kalvinch I, Piskunova I, Rozhkov E (1996) Novel systemically-active antagonists of the glycine site of the NMDA receptor-behavioural characterization. Soc Neurosci Abs 22: 1530
19. B antagonists as potential therapeutic agents. Previous hopes and present reality. Amino Acids 14: 235-239
20. Durand GM, Bennett MVL, Zukin RS (1993) Splice variants of the N-methyl-D-aspartate receptor NR1 identify domains involved in regulation by polyamines and protein kinase-C. Proc Natl Acad Sci USA 90: 6731-6735
21. Fadda E, Danysz W, Wroblewski JT, Costa E (1988) Glycine and D-serine increase the affinity of the N-methyl-D-aspartate sensitive glutamate binding sites in rat brain synaptic membranes. Neuropharmacology 27: 1183-1185
22. Faiman CP, Viu E, Skolnick P, Trullas R (1994) Differential effects of compounds that act at strychnine-insensitive glycine receptors in a punishment procedure. J Pharmacol Exp Ther 270: 528-533
23. Fedele E, Bisaglia M, and Raiteri (1997) D-serine modulates the NMDA receptor/nitric oxide/CGMP pathway in the rat cerebellum during in vivo microdialysis. Naunyn-Schmiedebergs Arch Pharmacol 355: 43-47
24. Globus MYT, Ginsberg MD, Busto R (1991) Excitotoxic index-A biochemical marker of selective vulnerability. Neurosci Lett 127: 39-42
25. Grimwood S, Kulagowski JJ, Mawer IM, Rowley M, Leeson PD, Foster AC (1995a) Allosteric modulation of the glutamate site on the NMDA receptor by four novel glycine site antagonists. Eur J Pharmacol Mol Pharmacol Sect 290: 221-226
26. Grimwood S, Le Bourdelles B, Whiting PJ (1995b) Recombinant human NMDA homomeric NR1 receptors expressed in mammalian cells form a high-affinity glycine antagonist binding site. J Neurochem 64: 525-530
27. Haggerty GC, Charles V, Lanthorn TH (1993) Acute vacuolization study of subcutaneously administered D-cycloserine (DCS) in Sprague Dawley rats. Soc Neurosci Abs 19: 1888
28. Hargreaves RJ, Rigby M, Smith D, Hill RG (1993) Lack of effect of L-687,414 ((+)-cis4-methyl-HA-966), an NMDA receptor antagonist acting at the glycine site, on cerebral glucose metabolism and cortical neuronal morphology. Br J Pharmacol 110: 36-42
29. Hashimoto A, Nishikawa T, Oka T, Takahashi K (1993) Endogenous D-serine in rat brain-N-methyl-D-aspartate receptor-related distribution and aging. J Neurochem 60: 783-786
30. Hirai H, Kirsch J, Laube B, Betz H, Kuhse J (1996) The glycine binding site of the Nmethyl-D-aspartate receptor subunit NR1: identification of novel determinants of coagonist potentiation in the extracellular M3-M4 loop region. Proc Natl Acad Sci USA 93: 6031-6036
31. Ishmael JE, Franklin PH, Murray TF, Leid M (1996) High level expression of the NMDAR1 glutamate receptor subunit in electroporated COS cells. J Neurochem 67: 1500-1510
32. Javitt DC, Frusciante M (1997) Glycyldodecylamide, a phencyclidine behavioral antagonist, blocks cortical glycine uptake: implications for schizophrenia and substance abuse. Psychopharmacology 129: 96-98
33. Johnson JW, Ascher P (1987) Glycine potentiates the NMDA response in cultured mouse brain neurones. Nature 325: 529-531
34. Kehne JH, Baron BM, Harrison BL, Mccloskey TC, Palfreyman MG, Poirot M, Salituro FG, Siegel BW, Slone AL, Van Giersbergen PLM, White HS (1995) MDL 100,458 and MDL 102,288: two potent and selective glycine receptor antagonists with different functional profiles. Eur J Pharmacol 284: 109-118
35. Kemp JA, Leeson PD (1993) The glycine site of the NMDA receptor - five years on. Trends Pharmacol Sci 14: 20-25
36. Kemp JA, Priestley T (1991) Effects of (+)-HA-966 and 7-chlorokynurenic acid on the kinetics of N-methyl-D-asparatate receptor agonist responses in rat cultured cortical neurons. Mol Pharmacol 39: 666-670
37. Kleckner NW, Dingledine R (1988) Requirement for glycine in activation of NMDA receptors expressed in Xenopus oocytes. Science 214: 835-837
38. Koek W, Colpaert FC (1990) Selective blockade of N-methyl-D-aspartate NMDAinduced convulsions by antagonists and putative glycine antagonists relationship with phencyclidine-like behavioural effects. J Pharmacol Exp Ther 252: 349-357
39. Kulagowski JJ, Leeson PD (1995) Glycine-site NMDA receptor antagonists. Expert Opin Ther Pat 5: 1061-1075
40. Kumashiro S, Hashimoto A, Nishikawa T (1995) Free D-serine in post-mortem brains and spinal cords of individuals with and without neuropsychiatrie diseases. Brain Res 681: 117-125
41. Laird JMA, Mason GS, Webb J, Hill RG, Hargreaves RJ (1996) Effects of a partial agonist and a full antagonist acting at the glycine site of the NMDA receptor on inflammationinduced mechanical hyperalgesia in rats. Br J Pharmacol 117:1487-1492
42. Laube B, Hirai H, Sturgess M, Betz H, Kuhse (1997) Molecular determinants of agonist discrimination by NMDA receptor subunits: analysis of the glutamate binding site on the NR2B subunit. Neuron 18: 493-503
43. Laurie DJ, SeeburgPH (1994) Ligand affinities at recombinant N-methyl-D-aspartate receptors depend on subunit composition. Eur J Pharmacol Mol Pharmacol 268:335-345
44. Leeson PD, Iversen LL (1994) The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. J Med Chem 37: 4053-4067
45. Lerma J, Zukin RS, Bennett MVL (1990) Glycine decreases desensitization of N-methyl-D-aspartate (NMDA) receptors expressed in Xenopus oocytes and is required for NMDA responses. Proc Natl Acad Sci USA 87: 2354-2358
46. Loscher W, Wlaz P, Rundfeldt C, Baran H, Honack D (1994) Anticonvulsant effects of the glycine/NMDA receptor ligands D-cycloserine and D-serine but not R-(+)-HA966 in amygdala-kindled rats. Br J Pharmacol 112: 97-106
47. Malandro MS, Kilberg MS (1996) Molecular biology of mammalian amino acid transporters. Ann Rev Biochem 65: 305-336
48. Matsui T, A, Sekiguchi M, Hashimoto A, Tomita U, Nishikawa T, Wada K (1995) Functional comparison of D-serine and glycine in rodents: the effect on cloned NMDA receptors and the extracellular concentration. J Neurochem 65: 454-458
49. Mayer ML, Vyklicky LJ, Clements J (1989) Regulation of NMDA receptor desensitization in mouse hippocampal neurons by glycine. Nature 338: 425-427
50. Mccabe RT, Wasterlain CG, Kucharczyk N, Sofia RD, Vogel JR (1993) Evidence for anticonvulsant and neuroprotectant action of felbamate mediated by strychnineinsensitive glycine receptors. J Pharmacol Exp Ther 264: 1248-1252
51. McClean M, Chizh BA, Headley PM (1998) Effects of NMDA receptor antagonists on nociceptive responses in vivo: comparison of antagonists acting at the glycine site with uncompetitive antagonists. Amino Acids 14: 217-221
52. Millan MJ, Seguin L (1994) Chemically-diverse ligands at the glycineB site coupled to N-methyl-D-aspartate (NMDA) receptors selectively block the late phase of formalininduced pain in mice. Neurosci Lett 178: 139-143
53. 2+-insensitive mutants. Neuropharmacology 34: 347-355
54. Molnar P, Erdo SL (1996) Differential effects of five glycine site antagonists on NMDA receptor desensitisation. Eur J Pharmacol 311: 311-314
55. Monyer H, Sprengel R, Schoepfer R, Herb A, Higuchi M, Lomeli H, Burnashev N, Sakmann B, Seeburg PH (1992) Heteromeric NMDA receptors-molecular and functional distinction of subtypes. Science 256: 1217-1221
56. Moroni F, Alesiani M, Galli A, Mori F, Pecorari R, Carla V, Cherici G, Pellicciari R (1991) Thiokynurenates: a new group of antagonists of the glycine modulatory site of the NMDA receptor. Eur J Pharmacol 199: 227-232
57. Moroni F, Alesiani M, Facci L, Fadda E, Skaper SD, Galli A, Lombardi G, Mori F, Ciuffi M, Natalini B, Pellicciari R (1992) Thiokynurenates prevent excitotoxic neuronal death in vitro and in vivo by acting as glycine antagonists and as inhibitors of lipid peroxidation. Eur J Pharmacol 218: 145-151
58. Murata S, Kawasaki K (1993) Common and uncommon behavioural effects of antagonists for different modulatory sites in the NMDA receptor/channel complex. Eur J Pharmacol 239: 9-15
59. Obrenovitch TP, Zilkha E (1996) Inhibition of cortical spreading depression by L-701,324, a novel antagonist at the glycine site of the N-methyl-D-aspartate receptor complex. Br J Pharmacol 117:931-937
60. Obrenovitch TP, Hardy AM, Urenjak J (1997) High extracellular glycine does not potentiate N-methyl-D-aspartate-evoked depolarization in vivo. Brain Res 746:190-194
61. O'Connor AJ, Vlachogiannis G, Moskal J, Kelso SR (1996) Subunit specific effects of D-cycloserine on NMDA receptors expressed in Xenopus oocytes. Soc Neurosci Abs 22:1530
62. Parsons CG, Zong XG, Lux HD (1993) Whole cell and single channel analysis of the kinetics of glycine-sensitive N-methyl-D-aspartate receptor desensitization. Br J Pharmacol 109: 213-221
63. Peeters BWMM, Vanderheyden PML (1992) In vitro and in vivo characterization of the NMDA receptor-linked strychnine-insensitive glycine site. Epilepsy Res 12: 157-162
64. Pellegrinigiampietro DE, Cozzi A, Moroni F (1994) The glycine antagonist and free radical scavenger 7-cl-thio-kynurenate reduces CA1 ischemic damage in the gerbil. Neuroscience 63: 701-709
65. Planellscases R, Sun W, Ferrermontiel AV, Montal M (1993) Molecular cloning, functional expression, and pharmacological characterization of an N-methyl-D-aspartate receptor subunit from human brain. Proc Natl Acad Sci USA 90: 5057-5061
66. Rowley M, Leeson PD, Stevenson GI, Moseley AM, Stansfield I, Sanderson I, Robinson L, Baker R, Kemp JA, Marshall GR, Foster AC, Grimwood S, Tricklebank MD, Saywell KL (1993) 3-Acyl-4-hydroxyquinolin-2(1h)-ones-systemically active anticon-vulsants acting by antagonism at the glycine site of the N-methl-D-aspartate receptor complex. J Med Chem 36: 3386-3396
67. Salituro FG, Tomlinson RC, Baron BM, Palfreyman MG, McDonald IA, Schmidt W, Wu HQ, Guidetti P, Schwarcz R (1994) Enzyme-activated antagonists of the strychnineinsensitive glycine NMDA receptor. J Med Chem 37: 334-336
68. Schell MJ, Brady RO, Molliver ME, Snyder SH (1997) D-Serine as a neuromodulator: regional and developmental localizations in rat brain glia resemble NMDA receptors. J Neurosci 17: 1604-1615
69. Smith RD, Grzelak ME, Coffin VL (1994) Felbamate, a novel antiepileptic agent, does not affect cognition in rodents. Behav Pharmacol 5: 365-368
70. Supplison, S, Bergman, C (1996) Control of NMDA receptor activation by a glycine transporter. Soc Neurosci Abs 22: 365
71. Tortella FCa, RG (1996) EEG seizure activity and behavioral neurotoxicity produced by (+)-MK801, but not the glycine site antagonist L-687,414, in the rat. Neuropharmacology 35: 441-448
72. Tsuchida E, Bullock R (1995) The effect of the glycine site-specific N-methyl-D-aspartate antagonist ACEA1021 on ischemic brain damage caused by acute subdural hematoma in the rat. J Neurotrauma 12: 279-288
73. Vaccarino AL, Marek P, Kest B, Weber E, Keana JFW, Liebeskind JC (1993) NMDA receptor antagonists, MK-801 and ACEA-1011, prevent the development of tonic pain following subcutaneous formalin. Brain Res 615: 331-334
74. Virgo L, De Belleroche J (1995) Induction of the immediate early gene c-jun in human spinal cord in amyotrophic lateral sclerosis with concomitant loss of NMDA receptor NR-1 and glycine transporter mRNA. Brain Res 676: 196-204
75. Vyklicky L Jr, Benveniste M, Mayer ML (1990) Modulation of N-methyl-D-aspartic acid receptor desensitization by glycine in mouse cultured hippocampal neurones. J Physiol London 428: 313-331
76. Wafford KA, Bain CJ, Lebourdelles B, Whiting PJ, Kemp JA (1993) Preferential co-assembly of recombinant NMDA receptors composed of three different subunits. Neuroreport 4: 1347-1349
77. Wang JKT, Thukral V (1996) Presynaptic NMDA receptors display physiological characteristics of homomeric complexes of NR1 subunits that contain the exon 5 insert in the N-terminal domain. J Neurochem 66: 865-868
78. Wang LY, Macdonald JF (1995) Modulation by magnesium of the affinity of NMDA receptors for glycine in murine hippocampal neurones. J Physiol London 486: 83-95
79. Warner DS, Martin H, Ludwig P, McAllister A, Keana JFW, Weber E (1995) In vivo models of cerebral ischemia: effects of parenterally administered NMDA receptor glycine site antagonists. J Cereb Blood Flow Metab 15: 188-196
80. Williams K, Zappia AM, Pritchett DB, Shen YM, Molinoff PB (1994) Sensitivity of the N-methyl-D-aspartate receptor to polyamines is controlled by NR2 subunits. Mol Pharmacol 45: 803-809
81. Wong EHF, Knight AR, Ransom R (1987) Glycine modulates MK-801 binding to the NMDA receptor in the rat brain. Eur J Pharmacol 142: 487-488
82. Wood MW, Vandongen HMA, Vandongen AMJ (1997) An alanine residue in the M3-M4 linker lines the glycine binding pocket of the N-methyl-D-aspartate receptor. J Biol Chem 272: 3532-3537
83. Wood PL (1995) The co-agonist concept: is the NMDA-associated glycine receptor saturated in vivo? Life Sci 57: 301-310
84. Woodward RM, Huettner JE, Guastella J, Keana JFW, Weber E (1995a) In vitro pharmacology of ACEA-1021 and ACEA-1031: systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites. Mol Pharmacol 47: 568-581
85. Woodward RM, Huettner JE, Tran M, Guastella J, Keana JFW, Weber E (1995b) Pharmacology of 5-chloro-7-trifluoromethyl-l,4-dihydro-2,3-quinoxalinedione: a novel systemically active ionotropic glutamate receptor antagonist. J Pharmacol Exp Ther 275: 1209-1218
86. Zapata A, Capdevila JL, Tarrason G, Adan J, Martinez JM, Piulats J, Trullas R (1997) Effects of NMDA-R1 antisense oligodeoxynucleotide administration: behavioral and radioligand binding studies. Brain Res 745: 114-120
87. Zhang L, Zheng X, Paupard MC, Wang AP, Santchi L, Friedman LK, Zukin RS, Bennett MVL (1994) Spermine potentiation of recombinant N-methyl-D-aspartate receptors is affected by subunit composition. Proc Natl Acad Sci USA 91: 10883-10887