In vitro binding properties in rat brain of [3H] Ro 25-6981, a potent and selective antagonist of NMDA receptors containing NR2B subunits

Journal of Neurochemistry

Volumn 70, Issue 5, 1998, Pages 2147-2155

  Mutel, Vincent ^a   Buchy, Danièle ^a   Klingelschmidt, Agnès ^a   Messer, Jürg ^a   Bleuel, Zaiga ^a   Kemp, John A ^a   Richards, John Grayson ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Binding; NR2B subunit; Radioautography; 3H Ro 25 6981

Indexed keywords

N METHYL DEXTRO ASPARTIC ACID RECEPTOR;

ANIMAL TISSUE; ARTICLE; BINDING COMPETITION; BINDING SITE; BRAIN; BRAIN REGION; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG RECEPTOR BINDING; NEUROCHEMISTRY; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

ANIMALIA;

EID: 0031969962     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.1998.70052147.x     Document Type: Article

References (37)

1. Carter C., Benavides J., Legendre P., Vincent J. D., Noel F., Thuret F., Lloyd K. G., Arbilla S., Zivkovic B., MacKenzie E. T., Scatton B., and Langer S. Z. (1988) Ifenprodil and SL82.0715 as cerebral antiischemic agents. II. Evidence for N-methyl-D-aspartate receptor antagonist properties. J. Pharmacol. Exp. Ther. 247, 1222-1232.
2. Chenard B. L., Shalahy I. A., Koe B. K., Ronau R. T., Butler T. W., Prochniak M. A., Schmidt A. W., and Fox C. B. (1991) Separation of α 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds. J. Med. Chem. 34, 3085-3090.
3. 50) of an enzymatic reaction. Biochem. Pharmacol. 22, 3099-3108.
4. 3H](+)-3-PPP to σ1 binding sites in rat brain. Neurosci. Lett. 116, 190-193.
5. Fischer G., Mutel V., Trube G., Malherbe P., Kew J. N. C., Mohacsi E., Heitz M. P., and Kemp J. A. (1997) Ro 25-6981, a highly potent and selective blocker of NMDA receptors containing the NR2B subunit. Characterization in vitro. J. Pharmacol. Exp. Ther. 283, 1285-1292.
6. Gallagher M. J., Huang H., Pritchett D. B., and Lynch D. R. (1996) Interactions between ifenprodil and the NR2B subunit of the N-methyl-D-aspartate receptor. J. Biol. Chem. 271, 9603-9611.
7. Ganong A. H., Lazzaro J. T., Richter K. E. G., Tang L.-H., Aizenman E., Menniti F. S., and White W. F. (1995) CP-101,606, a potent and selective forebrain NMDA receptor antagonist: effects on NMDA receptor-mediated ion flux. Soc. Neurosci. Abstr. 21, 1114.
8. 3H] ifenprodil binding in rat brain. Eur. J. Pharmacol. Mol. Pharmacol. 266, 67-77.
9. Hollmann M. and Heinemann S. (1994) Cloned glutamate receptors. Annu. Rev. Neurosci. 17, 31-108.
10. Ilyin V. I., Whittmore E. R., Guastella J., Weber E., and Woodward R. M. (1996) Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol. Mol. Pharmacol. 50, 1541-1550.
11. Kashiwagi K., Fukuchi J.-I., Chao J., Igarashi K., and 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.
12. Kew J. N. C., Trube G., and 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. (Lond.) 497, 761-772.
13. Kuryatov A., Laube B., Betz H., and Kuhse J. (1994) Mutational analysis of the glycine-binding site of the NMDA receptor: structural similarity with bacterial amino acid-binding proteins. Neuron 12, 1291-1300.
14. Kutsuwada T., Kashiwabuchi N., Mori H., Sakimura K., Kushlya E., Araki K., Meguro H., Masaki H., Kumanishi T., Arakawa M., and Mishina M. (1992) Molecular diversity of the NMDA receptor channel. Nature 358, 36-41.
15. Laurie D. J. and Seeburg P. H. (1994a) Ligand affinities at recombinant N-methyl-D-aspartate receptors depend on subunit composition. Eur. J. Pharmacol. Mol. Pharmacol. 268, 335-345.
16. Laurie D. J. and Seeburg P. H. (1994b) Regional and developmental heterogeneity in splicing of the rat brain NMDARI mRNA. J. Neurosci. 14, 3180-3194.
17. Legendre P. and Westbrook G. L. (1991) Ifenprodil blocks N-methyl-D-aspartate receptors by a two-component mechanism. Mol. Pharmacol. 40, 289-298.
18. Luque J. M., Malherbe P., and Richards J. G. (1995) Localization of NMDA receptor subunit mRNAs in the rat locus coeruleus. Mol. Brain Res. 29, 224-232.
19. 125I-labelled CGP 55802A. Proc. Natl. Acad. Sci. USA 90, 8434-8438.
20. 125I-Ifenprodil: synthesis and characterization of binding to a polyamine-sensitive site in cerebral cortical membranes. J. Neurochem. 61, 120-126.
21. Monyer H., Sprengel R. I., Schoepfer R., Herb A., Higuchi M., Lomeli H., Burnashev N., Sakmann B., and Seeburg P. H. (1992) Heteromeric NMDA receptors: molecular and functional distinction of subtypes. Science 256, 1217-1221.
22. Monyer H., Bumashev N., Laurie D. J., Sakmann B., and Seeburg P. H. (1994) Developmental and regional expression in the rat brain and functional properties of four NMDA receptors. Neuron 12, 529-540.
23. Mori H. and Mishina M. (1995) Structure and function of the NMDA receptor channel. Neuropharmacology 34, 1219-1237.
24. 2+-block site of the NMDA receptor channel. Nature 358, 673-675.
25. 3H]-CGP 39653 in rat brain. Br. J. Pharmacol. 119, 819-828.
26. Reynolds I. J. and Miller R. J. (1989) Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with polyamines. Mol. Pharmacol. 36, 758-765.
27. 3H]Ro 25-6981 in rat brain (Abstr.). Br. J. Pharmacol. 120 (Suppl.), 39P.
28. 3H]MK-801 binding in rat brain. J. Neurochem. 60, 1344-1353.
29. 3H]-ifenprodil, a novel NMDA antagonist, to a polyamine-sensitive site in the rat cerebral cortex. Eur. J. Pharmacol. 176, 249-250.
30. Sullivan J. M., Traynelis S. F., Chen H.-S. V., Escobar W., Heinemann S. F., and Lipton S. A. (1994) Identification of two cysteine residues that are required for redox modulation of the NMDA subtype of glutamate receptor. Neuron 13, 929-936.
31. Traynelis S. F., Hartley M., and Heinemann S. F. (1995) Control of proton sensitivity of the NMDA receptor by RNA splicing and polyamines. Science 268, 873-876.
32. Weiland G. A. and Molinoff P. B. (1981) Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties. Life Sci. 29, 313-330.
33. Wenzel A., Scheurer L., Kunzi R., Fritschy J. M., Mohler H., and Benke D. (1995) Distribution of NMDA receptor subunit proteins NR2A, 2B, 2C and 2D in rat brain. Neuroreport 7, 45-48.
34. 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.
35. Williams K. (1995) Pharmacological properties of recombinant N-methyl-D-aspartate (NMDA) receptors containing the ∈4 (NR2D) subunit. Neurosci. Lett. 184, 181-184.
36. Williams K., Russell S. L., Shen Y. M., and Molinoff P. B. (1993) Developmental switch in the expression of NMDA receptors occurs in vivo and in vitro. Neuron 10, 267-278.
37. 2+ potentiation of recombinant NMDA receptors. Neuron 12, 811-818.