Neuroprotective effects of NMDA receptor glycine recognition site antagonism: Dependence on glycine concentration

Journal of Neurochemistry

Volumn 70, Issue 5, 1998, Pages 2012-2019

  Pearlstein, Robert D ^a   Beirne, Joshua P ^a   Massey, Gary W ^a   Warner, David S ^a  

^a DUKE UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

ACEA 1021, in vitro; Excitotoxin; Glycine antagonist; Ischemia; NMDA receptor complex

Indexed keywords

6,7 DICHLORO 5 NITRO 2,3 QUINOXALINEDIONE; DIZOCILPINE; GLUTAMIC ACID; GLYCINE RECEPTOR ANTAGONIST; KAINIC ACID; LACTATE DEHYDROGENASE; N METHYL DEXTRO ASPARTIC ACID; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; BRAIN ISCHEMIA; BRAIN PROTECTION; CONCENTRATION RESPONSE; CONTROLLED STUDY; NERVE CELL CULTURE; NERVE CELL LESION; NEUROTOXICITY; NEUROTRANSMISSION; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALIA; STRYCHNOS TOXIFERA;

EID: 0031959128     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.1998.70052012.x     Document Type: Article

References (42)

1. Albers G. W., Clark W. M., Atkinson R. P., Madden K., Barbut D., Lechtenberg R., and Whitehouse M. J. (1997) Dose escalation study of the NMDA glycine-site antagonist ACEA 1021 in acute ischemic stroke [Abstr.]. Stroke 28, 223.
2. Amador E., Dorfman L. E., and Wacker W. E. C. (1963) Serum lactic dehydrogenase activity: an analytical assessment of current assays. Clin. Chem. 9, 391-394.
3. Baker A. J., Zornow M. H., Scheller M. S., Yaksh T. L., Skilling S. R., Smullin D. H., Larson A. A., and Kuczenski R. (1991) Changes in extracellular concentrations of glutamate, aspartate. glycine, dopamine, serotonin, and dopamine metabolites after transient global ischemia in the rabbit brain. J Neurochem. 57, 1370-1379.
4. Beirne J., Pearlstein R., Massey G. W., and Warner D. S. (1998) Neuroprotective effect of halothane in cortical cell cultures exposed to N-methyl-D-aspartate. Neurochem. Res. 23, 17-24.
5. Berg M., Bruhn T., Frandsen A., Schousboe A., and Diemer N. H. (1995) Kainic acid-induced seizures and brain damage in the rat: role of calcium homeostasis. J. Neurosci. Res. 40, 641-646.
6. Borowsky B., Mezey E., and Hoffman B. J. (1993) Two glycine transporter variants with distinct localization in the CNS and peripheral tissues are encoded by a common gene. Neuron 10, 851-863.
7. Cai S. X., Kher S. M., Zhou Z. L., Ilyin V., Espitia S. A., Tran M., Hawkinson J. E., Woodward R. M., Weber E., and Keana J. F. (1997) Structure-activity relationships of alkyl-and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor. J. Med. Chem. 40, 730-738.
8. Cheng Y. C. and Prusoff W. H. (1973) Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 percent inhibition (150) of an enzymatic reaction Biochem. Pharmacol. 22, 3099-3108.
9. Connick J. H. and Stone T. W. (1986) The effect of kainic, quinolinic and beta-kainic acids on the release of endogenous amino acids from rat brain slices. Biochem. Pharmacol. 35, 3631-3635.
10. Ferkany J. W. and Coyle J. T. (1983) Kainic acid selectively stimulates the release of endogenous excitatory acidic amino acids. J. Pharmacol. Exp. Ther. 225, 399-406.
11. Gill R., Hargreaves R. J., and Kemp J. A. (1995) The neuroprotective effect of the glycine site antagonist 3R-(+)-cis-4-methyl-HA966 (L-687,414) in a rat model of focal ischaemia. J. Cereb. Blood Flow Metab. 15, 197-204.
12. Globus M. Y.-T., Busto R., Martinez E., Valdés I., Dietrich W. D., and Ginsberg M. D. (1991) Comparative effect of transient global ischemia on extracellular levels of glutamate, glycine, and y-aminobutyric acid in vulnerable and nonvulnerable brain regions in the rat. J. Neurochem. 57, 470-478.
13. Hu P., Diemer N. H., Bruhn T., and Johansen F. F. (1997) Effects of the AMPA-receptor antagonist. NBQX, on neuron loss in dentate hilus of the hippocampal formation after 8, 10, or 12 min of cerebral ischemia in the rat. J. Cereb. Blood Flow Metab. 17, 147-152.
14. Johnson J. W. and Ascher P. (1987) Glycine potentiates the NMDA response in cultured mouse brain neurons. Nature 325, 529-531.
15. Kanthan R., Shuaib A., Griebel R., and Miyashita H. (1995) Intracerebral human microdialysis: in vivo study of an acute focal ischemic model of the human brain. Stroke 26, 870-872.
16. Kemp J. A. and Leeson P. D. (1993) The glycine site of the NMDA receptor - five years on. Trends Pharmacol. Sci. 14, 20-25.
17. Koh J. Y. and Choi D.W. (1987) Quantitative determination of glutamate mediated cortical neuronal injury in cell culture by lactate dehydrogenase efflux assay. J. Neurosci. Methods 20, 83-90.
18. Kulagowski J. J. (1996) Glycine-site NMDA receptor antagonists - an update. Expert Opin. Ther. Patents 6, 1069-1079.
19. Matsui T., Sekiguchi M., Hashimoto A., Tomita U., Nishikawa T., and 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.
20. McNamara R. K. and Routtenberg A. (1995) NMDA receptor blockade prevents kainate induction of protein F1/GAP-43 mRNA in hippocampal granule cells and subsequent mossy fiber sprouting in the rat. Brain Res. Mol. Brain Res. 33, 22-28.
21. Mies G., Kohno K., and Hossmann K. A. (1994) Prevention of periinfarct direct current shifts with glutamate antagonist NBQX following occlusion of the middle cerebral artery in the rat. J. Cereb. Blood Flow Metab. 14, 802-807.
22. Nellgård B. and Wieloch T. (1992) Postischemic blockade of AMPA but not NMDA receptors mitigates neuronal damage in the rat brain following transient severe cerebral ischemia. J. Cereb. Blood Flow Metab. 12, 2-11.
23. Newell D.W., Barth A., and Malouf A. T. (1995) Glycine site NMDA receptor antagonists provide protection against ischemia-induced neuronal damage in hippocampal slice cultures. Brain Res. 675, 38-44.
24. Park C. K., Nehls D. G., Graham D. I., Teasdale G. M., and McCulloch J. (1988) Focal cerebral ischaemia in the cat: treatment with the glutamate antagonist MK-801 after induction of ischaemia. J. Cereb. Blood Flow Metab. 8, 757-762.
25. Patel J., Zinkand W. C., Thompson C., Keith R., and Salama A. (1990) Role of glycine in the N-methyl-D-aspartate-mediated neuronal cytotoxicity. J. Neurochem. 54, 849-854.
26. Patel M., Day B., Crapo J., Fridovich I., and McNamara J. (1996) Requirement for Superoxide in excitotoxic cell death. Neuron 16, 345-355.
27. Planas A. M., Soriano M. A., Ferrer I., and Rodriguez Farre E. (1995) Kainic acid-induced heat shock protein-70 mRNA and protein expression is inhibited by MK-801 in certain rat brain regions. Eur. J. Neurosci. 7, 293-304.
28. Simon R. and Shiraishi K. (1990) N-Methyl-D-aspartate antagonist reduces stroke size and regional glucose metabolism. Ann. Neurot. 27, 606-611.
29. Simon R. P., Swan J. H., Griffiths T., and Meldrum B. S. (1984) Blockade of N-methyl-D-aspartate receptors may protect against ischemic damage in the brain. Science 226, 850-852.
30. Steinberg G. K., Saleh J., and Kunis D. (1988) Delayed treatment with dextromethorphan and dextrorphan reduces cerebral damage after transient focal ischemia. Neurosci. Lett. 89, 193-197.
31. Sucher N. J., Aizenman E., and Lipton S. A. (1991) N-Methyl-D-aspartate antagonists prevent kainate neurotoxicity in rat retinal ganglion cells in vitro. J. Neurosci. 11, 966-971.
32. Takagi K., Ginsberg M. D., Globus M. Y.-T., Dietrich W. D., Martinez E., Kraydieh S., and Busto R. (1993) Changes in amino acid neurotransmitters and cerebral blood flow in the ischemic penumbral region following middle cerebral artery occlusion in the rat - correlation with histopathology. J. Cereb. Blood Flow Metab. 13, 575-585.
33. Takano K., Tatlisumak T., Formato J. E., Carano R. A., Bergman A. G., Pullan L. M., Bare T. M., Sotak C. H., and Fisher M. (1997) Glycine site antagonist attenuates infarct size in experimental focal ischemia. Postmortem and diffusion mapping studies. Stroke 28, 1255-1262.
34. Takaoka S., Bart R. D., Pearlstein R., Warner D. S., and Brinkhous A. (1997) Neuroprotective effect of NMDA receptor glycine recognition site antagonism persists when brain temperature is controlled. J. Cereb. Blood Flow Metab. 17, 161-167.
35. Tsuchida E. and 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.
36. Virgili M., Migani P., Contestabile A., and Barnabei O. (1992) Protection from kainic acid neuropathological syndrome by NMDA receptor antagonist: effect of MK-801 and CGP 39551 on neurotransmitter and glial markers. Neuropharmacology 31, 469-474.
37. Warner D. S., Martin H. J., Ludwig P., McAllister A., Keana J. F. W., and 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.
38. Wilcox K. S., Fitzsimonds M., Johnson B., and Dichter M. A. (1996) Glycine regulation of synaptic NMDA receptors in hippocampal neurons. J Neurophysiol. 76, 3415-3424.
39. Wong E. H. F. and Kemp J. A. (1991) Sites for antagonism on the N-methyl-D-aspartate receptor channel complex. Annu. Rev. Pharmacol. Toxicol. 31, 401-425.
40. Woodward R. M., Huettner J. E., Guastella J., Keana J. F. W., and 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.
41. Woodward R. M., Huettner J. E., Tran M., Guastella J., Keana J. F. W., and Weber E. (1995b) Pharmacology of 5-chloro-7-trifluoromethyl-1,4-dihydro-2,3-quinoxalinedione: a novel systemically active ionotropic glutamate receptor antagonist. J. Pharmacol. Exp. Ther. 275, 1209-1218.
42. 2+ dependent. Neuroreport 5, 1477-1480.