State-dependent NMDA receptor antagonism by Ro 8-4304, a novel NR2B selective, non-competitive, voltage-independent antagonist

British Journal of Pharmacology

Volumn 123, Issue 3, 1998, Pages 463-472

  Kew, James N C ^a   Trube, Gerhard ^a   Kemp, John A ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Glutamate receptors; Neuroprotection; NMDA receptor antagonists

Indexed keywords

4 [3 [4 (4 FLUOROPHENYL) 1,2,3,6 TETRAHYDRO 1 PYRIDINYL] 2 HYDROXYPROPOXY]BENZAMIDE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BRAIN NERVE CELL; EMBRYO; NEUROPROTECTION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

ANIMALS; BENZAMIDES; EVOKED POTENTIALS; EXCITATORY AMINO ACID ANTAGONISTS; GLUTAMIC ACID; ION CHANNEL GATING; KINETICS; PIPERIDINES; PROTEIN BINDING; PYRIDINES; RATS; RECEPTORS, N-METHYL-D-ASPARTATE; XENOPUS LAEVIS;

EID: 0031985248     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0701634     Document Type: Article

References (40)

1. BEHE, P., STERN, P., WYLLIE, D.J.A., NASSAR, M., SCHOEPFER, R. & COLQUHOUN, D. (1995). Determination of NMDA NR1 subunit copy number in recombinant NMDA receptors. Proc. R. Soc. Lond., 262, 205-213.
2. BENVENISTE, M., CLEMENTS, J., VYKLICKY, JR, L. & 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. BERTOCCI, B., MIGGIANO, V., DA PRADA, M., DEMBIC, Z., LAHM, H.W. & MALHERBE, P. (1991). Human catechol-O-methyltransferase: cloning and expression of the membrane-associated form. Proc. Natl. Acad. Sci. U.S.A., 88, 1416-1420.
4. BERTRAND, D., COOPER, E., VALERA, S., RUNGGER, D. & BALLIVET, M. (1991). Electrophysiology of neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes following nuclear injection of genes or cDNAs. In Electrophysiology and Microinjection (Methods in Neurosciences), Vol 4. ed. Conn, P.M. pp. 174-193. San Diego: Academic Press.
5. CARTER, C.J., LLOYD, K.G., ZIVKOVIC, B. & SCATTON, B. (1990). Ifenprodil and SL 82.0715 as cerebral antiischemic agents. III. Evidence for antagonistic effects at the polyamine modulatory site within the N-methyl-D-aspartate receptor complex. J. Pharmacol. Exp. Ther., 253, 475-482.
6. CHAZOT, P.L., COLEMAN, S.K., CIK, M. & STEPHENSON, F.A. (1994). Molecular characterization of N-methyl-D-aspartate receptors expressed in mammalian cells yields evidence for the coexistence of three subunit types within a discrete receptor molecule. J. Biol. Chem., 269, 24403-24409.
7. CLEMENTS, J.D. & 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.
8. FERRER-MONTIEL, A.V. & MONTAL, M. (1996). Pentameric subunit stoichiometry of a neuronal glutamate receptor. Proc. Natl. Acad. Sci. U.S.A., 93, 2741-2744.
9. GALLAGHER, M.J., HUANG, H., PRITCHETT, D.B. & LYNCH, D.R. (1996). Interactions between ifenprodil and the NR2B subunit of the N-methyl-D-aspartate receptor. J. Biol. Chem., 271, 9603-9611.
10. GOTTI, B., DUVERGER, D., BERTIN, J., CARTER, C., DUPONT, R., FROST, J., GAUDILLIERE, B., MACKENZIE, E.T., ROUSSEAU, J., SCATTON, B. & WICK, A. (1988). Ifenprodil and SL 82.0715 as cerebral anti-ischemic agents. I. Evidence for efficacy in models of focal cerebral ischemia. J. Pharmacol. Exp. Ther., 247, 1211-1221.
11. GRAHAM, D., DARLES, G. & LANGER, S.Z. (1992). The neuroprotective properties of ifenprodil, a novel NMDA receptor antagonist, in neuronal cell culture toxicity studies. Eur. J. Pharmacol., 226, 373-376.
12. ISHII, T., MORIYOSHI, K., SUGIHARA, H., SAKURADA, K., KADOTANI, H., YOKOI, M., AKAZAWA, C., SHIGEMOTO, R., MIZUNO, N., MASU, M. & NAKANISHI, S. (1993). Molecular characterization of the family of the N-methyl-D-aspartate receptor subunits. J. Biol. Chem., 268, 2836-2843.
13. JACKSON, A. & SANGER, D.J. (1988). Is the discriminative stimulus produced by phencyclidine due to an interaction with N-methyl-D-aspartate receptors? Psychopharmacology, 96, 87-92.
14. KASHIWAGI, K., FUKUCHI, J.-I., CHAO, J., IGARASHI, K. & WILLIAMS, K. (1996). An aspartate residue in the extracellular loop of the N-methyl-D-aspartate receptor controls sensitivity to spermine and protons. Mol. Pharmacol., 49, 1131-1141.
15. KEMP, J.A. & KEW, J.N.C. (1998). NMDA receptor antagonists. In Receptor Based Drug Design, ed. Leff, P. New York: Marcel Dekker (in press).
16. KEW, J.N.C., TRUBE, G. & KEMP, J.A (1996). A novel mechanism of activity-dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurones. J. Physiol., 497, 761-772.
17. KUTSUWADA, T., KASHIWABUCHI, N., MORI, H., SAKIMURA, K., KUSHIYA, E., ARAKI, K , MEGURO, H., MASKAI, H., KUMANISHI, T., ARAKAWA, M. & MISHINA, M. (1992). Molecular diversity of the NMDA receptor channel. Nature, 358, 36-41.
18. LAURIE, D.G. & SEEBURG, P.H. (1994). Regional and developmental heterogeneity in splicing of the rat brain NMDAR1 mRNA. J. Neurosci., 14, 3180-3194.
19. LAURIE, D.J., PUTZKE, J., ZIEGLGÄNSBERGER, W., SEEBURG, P.H. & TOLLE, T.R. (1995). The distribution of splice variants of the NMDAR1 subunit mRNA in the adult rat brain. Mol. Brain Res., 32, 94-108.
20. LEGENDRE, P. & WESTBROOK, G.L. (1991). Ifenprodil blocks N-methyl-D-aspartate receptors by a two-component mechanism. Mol. Pharmacol., 40, 289-298.
21. LESTER, R.A.J. & JAHR, C.E. (1992). NMDA channel behaviour depends on agonist affinity. J. Neurosci., 12, 635-643.
22. LESTER, R.A.J., TONG. G. & JAHR, C.E. (1993). Interactions between the glycine and glutamate binding sites of the NMDA receptor. J. Neurosci., 13, 1088-1096.
23. LUO, J., WANG, Y., YASUDA, R.P., DUNAH. A.W. & WOLFE, B.B. (1997). The majority of N-methyl-D-aspartate receptor complexes in adult rat cerebral cortex contain at least three different subunits (NR1/NR2A/NR2B). Mol. Pharmacol., 51, 79-86.
24. MCBAIN, C.J. & MAYER, M.L. (1994). N-methyl-D-aspartic acid receptor structure and function. Physiol. Rev., 74, 723-760.
25. MEGURO, H., MORI, H., ARAKI, K., KUSHIYA, E., KUTSUWADA, T., YAMAZAKI, M., KUMANISHI, T., ARAKAWA, M., SAKIMURA, K. & MISHINA, M. (1992). Functional characterization of a heteromeric NMDA receptor channel expressed from cloned cDNAs. Nature, 357, 70-74.
26. 28k. Brain Res., 648, 109-120.
27. MONYER, H., BURNASHEV, N., LAURIE, D.J., SAKMANN, B. & SEEBURG, P.H. (1994). Developmental and regional expression in the rat brain and functional properties of four NMDA receptors. Neuron, 12, 529-540.
28. MONYER, H., SPRENGEL, R., SCHOEPFER, R., HERB, A., HIGUCHI, M., LOMELI, H., BURNASHEV, N., SAKMANN, B. & SEEBURG, P.H. (1992). Heteromeric NMDA receptors: molecular and functional distinction of subtypes. Science, 256, 1217-1221.
29. PERRAULT, G., MOREL, E., SANGER, D.G. & ZIVKOVIC, B. (1989). Comparison of the pharmacological profiles of four NMDA antagonists, ifenprodil. SL 82.0715, MK-801 and CPP, in mice. Br. J. Pharmacol., 97, 580P.
30. PRIESTLEY, T., OCHU, E. & KEMP, J.A. (1994). Subtypes of NMDA receptor in neurones cultured from rat brain. NeuroReport, 5, 1763-1765.
31. RANSOM, R.W. (1991). Polyamine and ifenprodil interactions with the NMDA receptor's glycine site. Eur. J. Pharmacol., 208, 67-71.
32. REYNOLDS, L.J. & MILLER, R.J. (1989). Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with polyamines. Mol. Pharmacol., 36, 758-765.
33. SHENG, M., CUMMINGS, J., ROLDAN, L.A., JAN, Y.N. & JAN, L.Y. (1994). Changing subunit composition of heteromeric NMDA receptors during development of rat cortex. Nature, 368, 144-147.
34. SIGEL, E., BAUR, R. & MALHERBE, P. (1994). Protein kinase C transiently activated heteromeric N-methyl-D-aspartate receptor channels independent of the phosphorylatable C-terminal splice domain and of consensus phosphorylation sites. J. Biol. Chem., 269, 8204-8208.
35. TRUBE, G., EHRHARD, P., MALHERBE, P. & HUBER, G. (1996). The selectivity of RO 25-6981 for NMDA receptor subtypes expressed in Xenopus oocytes. Soc. Neurosci. Abstr., 693.4.
36. WAFFARD, K.A., BAIN, C.J., LE BOURDELLES, B., WHITING, P.J. & KEMP, J.A. (1993). Preferential co-assembly of recombinant NMDA receptors composed of three different subunits. NeuroReport, 4, 1347-1349.
37. WILLIAMS, K. (1993). Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors. Mol. Pharmacol., 44, 851-859.
38. WILLIAMS, K., KASHIWAGI, K., FUKUCHI, J.-I. & IGARASHI, K. (1995). An acidic amino acid in the N-methyl-D-aspartate receptor that is important for spermine stimulation. Mol. Pharmacol., 48, 1087-1098.
39. WILLIAMS, K., RUSSELL, S.L., SHEN, Y.M. & MOLINOFF, P.B. (1993). Developmental switch in the expression of NMDA receptors occurs in vivo and in vitro. Neuron, 10, 267-278.
40. ZUKIN, R.S. & BENNETT, M.V.L. (1995). Alternatively spliced isoforms of the NMDARI receptor subunit. Trends Neurosci., 18, 306-313.