In vitro characterization of 5-carboxyl-2,4-di-benzamidobenzoic acid (NS3763), a noncompetitive antagonist of GLUK5 receptors

Journal of Pharmacology and Experimental Therapeutics

Volumn 309, Issue 3, 2004, Pages 1003-1010

  Christensen, Jeppe K ^a   Varming, Thomas ^a   Ahring, Philip K ^a   Jørgensen, Tino D ^a   Nielsen, Elsebet Ø ^a  

^a NEUROSEARCH A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

5 CARBOXYL 2,4 DIBENZAMIDOBENZOIC ACID; ALPHA AMINO 5 TERT BUTYL 3 HYDROXY 4 ISOXAZOLEPROPIONIC ACID; DOMOIC ACID; GLUTAMATE RECEPTOR ANTAGONIST; GLUTAMIC ACID; KAINIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID; NS 3763; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ARTICLE; BRAIN CELL; CALCIUM CELL LEVEL; CELL CULTURE; DRUG ACTIVITY; DRUG SCREENING; EPILEPSY; IN VITRO STUDY; KIDNEY CELL; MIGRAINE; PAIN; PRIORITY JOURNAL;

ANIMALS; BENZAMIDES; BENZOIC ACIDS; CALCIUM; CELLS, CULTURED; EXCITATORY AMINO ACID AGONISTS; HUMANS; MICE; RECEPTORS, AMPA; RECEPTORS, KAINIC ACID; RECEPTORS, N-METHYL-D-ASPARTATE;

EID: 2542439966     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.103.062794     Document Type: Article

References (40)

1. Bleakman D, Ballyk BA, Schoepp DD, Palmer AJ, Bath CP, Sharpe EF, Woolley ML, Bufton HR, Kamboj RK, Tarnawa I, and Lodge D (1996) Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology 35:1689-1702.
2. Bleakman D, Gates MR, Ogden AM, and Mackowiak M (2002) Kainate receptor agonists, antagonists and allosteric modulators. Curr Pharm Des 8:873-885.
3. Bortolotto ZA, Clarke VR, Delany CM, Parry MC, Smolders I, Vignes M, Ho KH, Miu P, Brinton BT, Fantaske R, et al. (1999) Kainate receptors are involved in synaptic plasticity. Nature (Lond) 402:297-301.
4. Clarke VR, Ballyk BA, Hoo KH, Mandelzys A, Pallizzari A, Bath CP, Thomas J, Sharpe EF, Davies CH, Ornstein PL, et al. (1997) A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmission. Nature (Lond) 389:599-603.
5. Collingridge GL and Lester RA (1989) Excitatory amino acid receptors in the vertebrate central nervous system. Pharmacol Rev 41:143-210.
6. Davies J, Francis AA, Jones AW, and Watkins JC (1981) 2-Amino-5-phosphonovalerate (2APV), a potent and selective antagonist of amino acid-induced and synaptic excitation. Neurosci Lett 21:77-81.
7. Donevan SD and Rogawski MA (1993) GYKI 52466, a 2,3-benzodiazepine, is highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron 10:51-59.
8. 3H]GABA from cultured mouse cerebral cortex interneurons. J Neurosci 7:2910-2916.
9. Filla SA, Winter MA, Johnson KW, Bleakman D, Bell MG, Bleisch TJ, Castaño AM, Clemens-Smith A, del Prado M, Dieckman DK, et al. (2002) Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycarbonylimidazol-1-ylmethyl) decahydroisoquinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. J Med Chem 45:4383-4386.
10. Fletcher EJ, Martin D, Aram JA, Lodge D, and Honoré T (1988) Quinoxalinediones selectively block quisqualate and kainate receptors and synaptic events in rat neocortex and hippocampus and frog spinal cord in vitro. Br J Pharmacol 95:585-597.
11. Hamill OP, Marty A, Neher E, Sakmann B, and Sigworth FJ (1981) Improved patch-clamp techniques for high-resolution current recordings from cells and cell-free membrane patches. Pflueg Arch 391:85-100.
12. Honoré T, Davies SN, Drejer J, Fletcher EJ, Jacobsen P, Lodge D, and Nielsen FE (1988) Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists. Science (Wash DC) 241:701-703.
13. Huettner JE (1990) Glutamate receptor channels in rat DRG neurons: activation by kainate and quisqualate and blockade of desensitization by Con A. Neuron 5:255-266.
14. 3H]kainate binding. Eur J Pharmacol 246:195-204.
15. Korczak B, Nutt SL, Fletcher EJ, Hoo KH, Elliott CE, Rampersad V, McWhinnie EA, and Kamboj RK (1995) cDNA cloning and functional properties of human glutamate receptor EAA3 (GluR5) in homomeric and heteromeric configuration. Receptors Channels 3:41-49.
16. Lauridsen J, Honoré T, and Krogsgaard-Larsen P (1985) Ibotenic acid analogues. Synthesis, molecular flexibility and in vitro activity of agonists and antagonists at central glutamic acid receptors. J Med Chem 28:668-672.
17. Lerma J, Paternain AV, Naranjo JR, and Mellström B (1993) Functional kainate-selective glutamate receptors in cultured hippocampal neurons. Proc Natl Acad Sci USA 90:11688-11692.
18. Lerma J, Patemain AV, Rodriquez-Moreno A, and Lopez-Garcia JC (2001) Molecular physiology of kainate receptors. Physiol Rev 81:971-998.
19. Li P, Wilding TJ, Kim SJ, Calejesan AA, Huettner JE, and Zhuo M (1999) Kainate-receptor-mediated sensory synaptic transmission in mammalian spinal cord. Nature (Lond) 397:161-164.
20. Lodge D, Jones MG, and Palmer AJ (1991) Excitatory amino acids: new tools for old stories or pharmacological subtypes of glutamate receptors: electrophysiological studies. Can J Physiol Pharmacol 69:1123-1128.
21. Madden DR (2002) The structure and function of glutamate receptor ion channels. Nat Rev Neurosci 3:91-101.
22. Mulle C, Sailer A, Swanson GT, Brana C, O'Gorman S, Bettler B, and Heinemann SF (2000) Subunit composition of kainate receptors in hippocampal interneurons. Neuron 28:475-484.
23. Nielsen EØ, Varming T, Mathiesen C, Jensen LH, Møller A, Gouliaev AH, Wätjen F, and Drejer J (1999) SPD 502: a water-soluble and in vivo long-lasting AMPA antagonist with neuroprotective activity. J Pharmacol Exp Ther 289:1492-1501.
24. Partin KM, Patneau DK, Winters CA, Mayer ML, and Buonanno A (1993) Selective modulation of desensitization at AMPA versus kainate receptors by cyclothiazide and concanavalin A. Neuron 11:1069-1082.
25. Paternain AV, Herrera MT, Nieto MA, and Lerma J (2000) GluR5 and GluR6 kainate receptor subunits coexist in hippocampal neurons and coassemble to form functional receptors. J Neurosci 20:196-205.
26. Paternain AV, Morales M, and Lerma J (1995) Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 14:185-189.
27. Paternain AV, Vicente MA, Nielsen EØ and Lerma J (1996) Comparative antagonism of kainate-activated AMPA and kainate receptors in hippocampal neurons. Eur J Neurosci 8:2129-2136.
28. Procter MJ, Houghton AK, Faber ES, Chizh BA, Ornstein PL, Lodge D, and Headley PM (1998) Actions of kainate and AMPA selective glutamate receptor ligands on nociceptive processing in the spinal cord. Neuropharmacology 37:1287-1297.
29. Rammes G, Swandulla D, Spielmanns P, and Parsons CG (1998) Interactions of GYKI 52466 and NBQX with cyclothiazide at AMPA receptors: experiments with outside-out patches and EPSCs in hippocampal neurones. Neuropharmacology 37:1299-1320.
30. Ruscheweyh R and Sandkühler J (2002) Role of kainate receptors in nociception. Brain Res Rev 40:215-222.
31. Schoepp DD, Jane DE, and Monn JA (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38:1431-1476.
32. Sheardown MJ, Nielsen EØ, Hansen AJ, Jacobsen P and Honoré T (1990) 2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline: a neuroprotectant for cerebral ischemia. Science (Wash DC) 247:571-574.
33. Simmons RM, Li DL, Hoo KH, Deverill M, Ornstein PL, and Iyengar S (1998) Kainate GluR5 receptor subtype mediates the nociceptive response to formalin in the rat. Neuropharmacology 37:25-36.
34. K5-containing kainate receptors prevent pilocarpine-induced limbic seizures. Nat Neurosei 5:796-804.
35. Sommer B, Burnashev N, Verdoorn TA, Keinanen K, Sakmann B, and Seeburg PH (1992) A glutamate receptor channel with high affinity for domoate and kainate. EMBO J 11:1651-1656.
36. Varming T, Ahring PK, Sager TN, Mathiesen C, Johansen TH, Wätjen F, and Drejer J (2001) Optimization of isatine oximes as neuroprotective AMPA receptor antagonists: in vitro and in vivo evaluation of SPD 502, in Excitatory Amino Acids: 10 Years Later (Turski L, Schoepp DD, and Cavalheiro EA eds) pp 193-205, IOS Press, Amsterdam.
37. Verdoorn TA, Johansen TH, Drejer J and Nielsen EO (1994) Selective block of recombinant glur6 receptors by NS-102, a novel non-NMDA receptor antagonist. Eur J Pharmacol 269:43-49.
38. Wilding TJ and Huettner JE (1996) Antagonist pharmacology of kainate and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors. Mol Pharmacol 49:540-546.
39. Wilding TJ and Huettner JE (2001) Functional diversity and developmental changes in rat neuronal kainate receptors. J Physiol (Lond) 532:411-421.
40. Wong EH, Kemp JA, Priestly T, Knight AR, Woodruff GN, and Iversen LL (1986) The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci USA 83:7104-7108.