Electrophysiological characterisation of the antagonist properties of two novel NMDA receptor glycine site antagonists, L-695,902 and L-701,324

Neuropharmacology

Volumn 35, Issue 11, 1996, Pages 1573-1581

  Priestley, Tony ^b   Laughton, Petra ^b   Macaulay, Alison J ^b   Hill, Raymond G ^b   Kemp, John A ^a,b  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

Antagonist; Electrophysiology; Glycine; Neurone; NMDA; Receptor; Recombinant

Indexed keywords

7 CHLORO 4 HYDROXY 3 (3 PHENOXYPHENYL) 2 QUINOLONE; 7 CHLOROKYNURENIC ACID; GLYCINE; GLYCINE RECEPTOR ANTAGONIST; L 695902; N METHYL DEXTRO ASPARTIC ACID; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; RECEPTOR SUBTYPE; RECEPTOR SUBUNIT; RECOMBINANT RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BRAIN NERVE CELL; CONTROLLED STUDY; ELECTROPHYSIOLOGY; FETUS; HUMAN; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; CELLS, CULTURED; CEREBRAL CORTEX; ELECTROPHYSIOLOGY; EXCITATORY AMINO ACID ANTAGONISTS; HUMANS; KINETICS; KYNURENIC ACID; MEMBRANE POTENTIALS; MICE; NEURONS; PATCH-CLAMP TECHNIQUES; QUINOLONES; RATS; RECEPTORS, GLYCINE; RECEPTORS, N-METHYL-D-ASPARTATE;

EID: 0342541393     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(96)00141-4     Document Type: Article

References (37)

1. Benveniste M. and Mayer M. L. (1991) Kinetic analysis of antagonist action at N-methyl-D-aspartic acid receptors. Biophys. J. 59: 560-573.
2. Benveniste M., Clements J., Vyklicky L. and Mayer M. L. (1990) A kinetic analysis of the modulation of N-methyl-D-aspartic acid receptors by glycine in mouse cultured hippocampal neurones. J. Physiol. 428: 333-357.
3. Cheng Y. C. and Prusoff W. H. (1973) Relationship between the inhibition constant (Ki) and the concentration of an inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol. 22: 3099-3108.
4. Clements J. D. and Westbrook G. L. (1991) Activation kinetics reveal the number of glutamate and glycine binding sites on the N-methyl-D-aspartate receptor. Neuron 7: 605-613.
5. Collingridge G. L. and Bliss T. V. P. (1995) Memories of NMDA receptors and LTP. Trends Neurosci. 18: 54-56.
6. Danysz W., Parsons C. G., Bresink I. and Quack G. (1995) Glutamate in CNS disorders. Drugs News Persp. 5: 261-277.
7. Forsythe I. D. and Westbrook G. L. (1988) Slow excitatory postsynaptic currents mediated by N-methyl-D-aspartate receptors on cultured mouse central neurones. J. Physiol. 396: 515-533.
8. Gibb A. J. and Colquhoun D. C. (1991) Glutamate activation of a single NMDA receptor-channel produces a cluster of channel openings. Proc. Roy. Soc. Lond. B. 243: 39-45.
9. Gibb A. J. and Colquhoun D. C. (1992) Activation of N-methyl-D-aspartate receptors by L-glutamate in cells dissociated from adult rat hippocampus. J. Physiol. 456: 143-179.
10. Grimwood S., Kulagowski J. J., Mawer I. M., Rowley M., Leeson P. D. and Foster A. C. (1995) Allosteric modulation of the glutamate site on the NMDA receptor by four novel glycine site antagonists. Eur. J. Pharmacol. Mol. Pharmacol. 290: 221-226.
11. Jahr C. E. and Stevens C. F. (1993) Calcium permeability of the N-methyl-D-aspartate receptor channel in hippocampal neurons in culture. Proc. Natl. Acad. Sci. U.S.A. 90: 11573-11577.
12. Johnson J. W. and Ascher P. (1992) Equilibrium and kinetic study of glycine action on the N-methyl-D-aspartate receptor in cultured mouse brain neurons. J. Physiol. 455: 339-365.
13. Kemp J. A. and Priestley T. (1991) Effects of (+)-HA-966 and 7-Chorokynurenic acid on the kinetics of N-methyl-D-aspartate receptor agonist responses in rat cultured cortical neurones. Mol. Pharmacol. 39: 666-670.
14. Kemp J. A., Priestley T., Rowley M. and Leeson P. D. (1993) differences between the electrophysiological properties of 7-chorokynurenic acid and a new glycine site antagonist, L-695,902. J. Neurochem. 61: S281A.
15. Kemp J. A. and Leeson P. D. (1993) The glycine site of the NMDA receptor - five years on. Trends Pharmacol Sci. 14: 20-25.
16. Kleckner N. W. and Dingledine R. (1988) Requirement for glycine in activation of NMDA-receptors expressed in Xenopus oocytes. Science 241: 835-837.
17. Kulagowski J. J., Baker R., Curtis N. R., Leeson P. D., Mawer M., Moseley A. M., Ridgill M. P., Rowley M., Stansfield I., Foster A. C., Grimwood S., Hill R. G., Kemp J. A., Marshall G. R., Saywell K. L. and Tricklebank M. D. (1994) 3′-(Arylmethyl)-and 3′-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor. J. Med. Chem. 37: 1402-1405.
18. Leeson P. D., Baker R., Carling R. C., Kulagowski J. J., Mawer I. M., Ridgill M. P., Rowley M., Smith J. D., Stansfield I., Stevenson G. L. Foster A. C. and Kemp J. A. (1993) Amino acid bioisosteres: design of 2-quinone derivatives as glycine site N-methyl-D-aspartate receptor antagonists. BioMed. Chem. Lett. 3: 299-304.
19. Leeson P. D. and Iversen L. L. (1994) The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. J. Med. Chem. 37: 4053-4067.
20. Legendre P., Rosenmund C. and Westbrook G. L. (1993) Inactivation of NMDA channels in cultured hippocampal neurons by intracellular calcium. J. Neurosci. 13: 674-684.
21. Lester R. A. J., Tong G. and Jahr C. E. (1993) Interactions between the glutamate and glycine binding sites of the NMDA receptor. J. Neurosci. 13: 1088-1096.
22. Mayer M. L., Vyklicky L. and Clements J. (1989) Regulation of NMDA receptor desensitisation in mouse hippocampal neurons by glycine. Nature 338: 425-427.
23. McBain C. J. and Mayer M. L. (1994) N-methyl-D-aspartic acid receptor structure and function. Physiol Rev. 74: 723-753.
24. Muir K. W. and Lees K. R. (1995) Clinical experience with excitatory amino acid antagonist drugs. Stroke 26: 503-513.
25. Ornstein P. L., Monn J. A. and Schoepp D. D. (1994) Antagonists of the NMDA receptor complex. Drug News Persp. 7: 5-12.
26. Patneau D. K. and Mayer M. L. (1990) Structure activity relationships for amino acid transmitter candidates acting at N-methyl-D-aspartate and quisqualate receptors. J. Neurosci. 10: 2385-2399.
27. Priestley T., Danks P., Marshall G. R., Kemp J. A., Kulagowski J. J., Leeson P. D. and Hill R. G. (1994a) L-701,324: a high affinity antagonist at the glycine-recognition site of the NMDA receptor. Br. J. Pharmacol. 113: 31P.
28. Priestley T., Horne A. L., McKernan R. L. and Kemp J. A. (1990) The effect of NMDA receptor glycine site antagonists on hypoxia-induced neurodegeneration of rat cortical cell cultures. Brain Res. 531: 183-188.
29. Priestley T. and Kemp J. A. (1993) Agonist response kinetics of N-methyl-D-aspartate receptors in neurons cultured from rat cerebral cortex and cerebellum: evidence for receptor heterogeneity. Mol. Pharmacol. 44: 1252-1257.
30. Priestley T., Laughton P., Myers J., LeBourdelles B., Kerby J. and Whiting P. J. (1995) Pharmacological properties of recombinant human NMDA receptors comprising NR1a NR2A and NR1a NR2B subunit assemblies expressed in permanently transfected mouse fibroblast cells. Mol. Pharmacol. 48: 841-848.
31. Priestley T., Ochu E. O. and Kemp J. A. (1994b) Subtypes of NMDA receptor in neurones cultured from rat brain. NeuroReport 5: 1763-1765.
32. Rosenmund C. and Westbrook G. L. (1993) Calcium-induced actin depolymerization reduces NMDA channel activity. Neuron 10: 805-814.
33. Rowley M., Leeson P. D., Stevenson G. I., Moseley A. M., Stansfield I., Sanderson I., Robinson L., Baker R., Kemp J. A. and Marshall G. R. (1993) 3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex. J. Med. Chem. 36: 3386-3396.
34. Saywell K. L., Bristow L. J., Foster A. C., Grimwood S., Hill R. G., Hutson P. H., Kulagowski J. J., Leeson P. D. and Tricklebank M. D. (1995) The pharmacological profile of the glycine. NMDA receptor antagonist. L-701,324. Br. J. Pharmacol. 114: 320P.
35. Seeburg P. H., Burnashev N., Kohr G., Kuner T., Sprengel R. and Monyer H. (1995) The NMDA receptor: Molecular design of a coincidence detector. In: Recent Progress in Hormone Research, Vol. 50. pp. 19-34. Academic Press Inc., U.S.A..
36. Vyklicky L. M., Vlachova V. and Krusek J. (1990) The effect of external pH changes on responses to excitatory amino acids in mouse hippocampal neurons. J. Physiol. 430: 497-517.
37. Whiting P. J. and Priestley T. The molecular biology of NMDA type glutamate receptors. In: Amino Acid Neurotransmission, (Turner A. J. and Stephenson F. A., Eds). Portland Press Ltd., in press.