Differential effects of five glycine site antagonists on NMDA receptor desensitisation

European Journal of Pharmacology

Volumn 311, Issue 2-3, 1996, Pages 311-314

  Molnár, Péter ^a,b   Erdõ, Sándor L ^a  

^a Chinoin Pharmaceutical and Chemical Works Ltd   (Hungary)

^b DUKE UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

5,7 Dichlorokynurenic acid; ACEA 1021; Desensitization; Glycine coagonist site; L 695,902; LY 294,619; NMDA receptor; RPR 104,632

Indexed keywords

5,7 DICHLOROKYNURENIC ACID; 6,7 DICHLORO 5 NITRO 2,3 QUINOXALINEDIONE; L 695902; LY 294619; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; RPR 104632; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BRAIN CORTEX; CONTROLLED STUDY; DESENSITIZATION; FETUS; NONHUMAN; PATCH CLAMP; POTENTIAL DIFFERENCE; PRIORITY JOURNAL; RAT;

EID: 0030581471     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/0014-2999(96)00587-0     Document Type: Article

References (14)

1. Erdõ, S.L., A. Michler, J.R. Wolff and H. Tytko, 1990, Lack of excitotoxic cell death in serum-free cultures of rat cerebral cortex, Brain Res. 526, 328.
2. Foster, A.C., J.A. Kemp, P.D. Leeson, S. Grimwood, A.E. Donald, G.R. Marshall, T. Priestley, J.D. Smith and R.W. Carling, 1992, Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain, Mol. Pharmacol. 41, 914.
3. Grimwood, S., M. Rowley, P.D. Leeson and A.C. Foster, 1993, L-695,902, an antagonist at the glycine site on N-methyl-D-aspartate receptor allosterically modulates the glutamate site, J. Neurochem. 61 (Suppl.), s281.
4. Jimonet, P., F. Audiau, J.C. Aloup, M. Barreau, J.C. Blanchard, A. Bohme, A. Boireau, M. Chéve, D. Damour, A. Dobie, J. Lavyare, G. Dutruc-Rosset, J.C.R. Randle, J. Rataud, J.M. Stutzmann and S. Mignani, 1994, Synthesis and SAR of 2H-1,2,4-benzothiadiazine-1,1-dioxide-3-carboxylic acid derivatives as novel potent glycine antagonists of the NMDA receptor-channel complex, Bioorg. Med. Chem. Lett. 4, 2735.
5. Johnson, J.W. and P. Ashen, 1987, Glycine potentiates the NMDA response in cultured mouse brain neurones, Nature 325, 529.
6. Kehne, J.H., B.M. Baron, B.L. Harrison, T.C. McCloskey, M.G. Palfreyman, M. Poirot, F.G. Salituro, B.W. Siegel, A.L. Slone, P.L.M. Van Giersbergen and H.S. White, 1995, MDL-100,485 and MDL-102,228: two potent and selective glycine receptor antagonists with different functional profiles, Eur. J. Pharmacol. 284, 109.
7. Lakics, V., P. Molnár and S.L. Erdõ, 1995, Vinpocetine is a highly potent neuroprotectant against veratridine-induced cell death in primary cultures of rat cerebral cortex, Neurosci. Lett. 185, 127.
8. Leeson, P.D. and L.L. Iversen, 1994, The glycine site on the NMDA receptor: structure activity relationships and therapeutic potential, J. Med. Chem. 37, 4053.
9. Maksay G., P. Molnár and L. Gruber, 1994, Common modes of action of γ-butyrolactones and pentylenetetrazol on the convulsant and benzodiazepine sites and channel activity of the GABA receptor-ionophore complex, Eur. J. Pharmacol. Mol. Pharmacol. Sect. 288, 61.
10. Mayer, M.L., L. Vyklicky Jr and J. Clements, 1989, Regulation of NMDA receptor desensitization in mouse hippocampal neurons by glycine, Nature 338, 425.
11. McQuaid, L.A., E.C.R. Smith, D. Lodge, E. Pralong, M.G. Jones and A. Bond, 1993, 3-Phenyl 4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex. J. Neurochem. 61 (Suppl.), s282.
12. Parsons, C.G., X. Zong and H.D. Lux, 1993, Whole cell and single channel analysis of the kinetics of glycine-sensitive N-methyl-D-aspartate receptor desensitisation, Br. J. Pharmacol. 109, 213.
13. Vyklicky, L., 1993, Calcium-mediated modulation of N-methyl-D-aspartate (NMDA) responses in cultured rat hippocampal neurones, J. Physiol. 470, 575.
14. Woodward, R.M., J.E. Huettner, J. Guastella, J.F.W. Keana and E. Weber, 1995, In vitro pharmacology of ACEA-1021 and ACEA-1031: systemically active quinoxaline-diones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites, Mol. Pharmacol. 47, 568.