Potent antihyperalgesic activity without tolerance produced by glycine site antagonist of N-methyl-D-aspartate receptor GV196771A

Journal of Pharmacology and Experimental Therapeutics

Volumn 290, Issue 1, 1999, Pages 158-169

  Quartaroli, M ^a   Carignani, C ^a   Dal Forno, G ^a   Mugnaini, M ^a   Ugolini, A ^a   Arban, R ^a   Bettelini, L ^a   Maraia, G ^a   Belardetti, F ^a   Reggiani, A ^a   Trist, D G ^a   Ratti, E ^a   Di Fabio, R ^a   Corsi, M ^a  

^a GSK   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCINE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; SODIUM 4,6 DICHLORO 3 (2 OXO 1 PHENYLPYRROLIDIN 3 YLIDENEMETHYL) 1H INDOLE 2 CARBOXYLATE; UNCLASSIFIED DRUG;

ANALGESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; DRUG BINDING SITE; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG TOLERANCE; HYPERALGESIA; MALE; NERVE INJURY; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT;

ANALGESICS, NON-NARCOTIC; ANIMALS; BEHAVIOR, ANIMAL; BINDING, COMPETITIVE; CEREBRAL CORTEX; DRUG TOLERANCE; ELECTROPHYSIOLOGY; EMBRYO; EXCITATORY AMINO ACID ANTAGONISTS; HYPERALGESIA; INDOLES; MALE; MICE; PAIN MEASUREMENT; PATCH-CLAMP TECHNIQUES; PYRROLES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GLYCINE; RECEPTORS, N-METHYL-D-ASPARTATE; SPINAL CORD;

EID: 0032966913     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. Arunlakshana O and Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol 14:48-58.
2. Bennett GJ and Xie YK (1988) A peripheral mononeuropathy in the rat that produces disorders of pain sensation like those seen in man. Pain 33:87-107.
3. Boxall SJ, Thompson SWN, Dray A, Dickenson AM and Urban L (1996) Metabotropic glutamate receptor activation contributes to nociceptive reflex activity in the rat spinal cord in-vitro. Neuroscience 74:13-20.
4. Choi DW (1994) Glutamate receptors and the induction of excitotoxic neuronal death. Prog Brain Res 100:47-51.
5. Coderre TJ, Vaccarino AL and Melzack R (1990) Central nervous system plasticity in the tonic pain response to subcutaneous formalin injection. Brain Res 535:155-158.
6. Collingridge GL and Bliss TV (1995) Memories of NMDA receptors and LTP. Trends Neurosci 18:54-56.
7. Corsi M, Fina P and Trist DG (1996) Co-agonism in drug-receptor activation: Illustrated by the NMDA receptor. Trends Pharmacol Sci 17:220-222.
8. Davar G, Hama A, Deykin A, Vos B and Maciewicz R (1991) MK-801 blocks the development of thermal hyperalgesia in a rat model of experimental painful neuropathy. Brain Res 553:327-330.
9. De Lean A, Munson PJ and Rodbard D (1978) Simultaneous analysis of families of sigmoidal curves: Application to bioassay, radioligand assay, and physiological dose-response curves. Am J Physiol 235:E97-E102.
10. Dickenson AH and Aydar E (1991) Antagonism at the glycine site on the NMDA receptor reduces spinal nociception in the rat. Neurosci Lett 121:263-266.
11. Dickenson AH and Sullivan A (1987) Subcutaneous formalin-induced activity of dorsal horn neurones in the rat: Differential response to an intrathecal opiate administered pre or post formalin. Pain 30:349-360.
12. Dougherty PM and Willis WD (1991) Modification of the responses of primate spinothalamic neurons to mechanical stimulation by excitatory amino acids and an N-methyl-D-aspartate antagonist. Brain Res 542(Suppl 1):15-22.
13. Dunnett CW and Tamhane AC (1991) Step-down multiple test for comparing treatments with control in unbalanced one-way layouts. Stat Med 10:939-947.
14. Fitzgerald SC (1989) Dissociated spinal cord and dorsal root ganglion cultures upon plastic tissue culture dishes, glass coverslips and wells, in A Dissection and Tissue Culture Manual of the Nervous System (Shahar A, De Vellis J, Vernadakis A and Haber B, eds) pp. 219-222, Alan Liss, New York.
15. Foster AC and Wong EMF (1987) The novel anticonvulsant MK-801 binds to the activated state of the N-methyl-D-aspartate receptor in rat brain. Br J Pharmacol 91:403-409.
16. Giacobbe SA, Baraldi D and Di Fabio R (1998) Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction. Bioorg Med Chem Lett 8(Suppl 13):1689-1692.
17. 3H]-alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA) to rat cortex membranes reveals two sites or affinity states. J Recept Res 11:727-741.
18. Goslin K and Banker G (1991) Rat hippocampal neurons in low-density culture, in Culturing Nerve Cells (Banker G and Goslin K eds) pp 251-281, MIT Press, Cambridge, MA.
19. Haley JE, Sullivan AF and Dickenson AH (1990) Evidence for spinal N-methyl-D-aspartate receptor involvement in prolonged chemical nociception in the rat. Brain Res 518:218-226.
20. Harris JA, Corsi M, Quartaroli M, Arban R and Bentivoglio M (1996) Upregulation of spinal glutamate receptors in chronic pain. Neuroscience 74:7-12.
21. Heapy CG, Jamieson A and Russel NJW (1987) Afferent C-fibre and A-delta activity in models of inflammation. Br J Pharmacol 90:164P.
22. Herron CE, Lester RA, Coan EJ and Collingridge GL (1986) Frequency-dependent involvement of NMDA receptors in the hippocampus: A novel synaptic mechanism. Nature (Lond) 322:265-268.
23. Hollmann M and Heinemann S (1994) Cloned glutamate receptors. Annu Rev Neurosci 17:31-108.
24. Leff P and Dougall IG (1993) Further concerns over Cheng-Prusoff analysis. Trends Pharmacol Sci 14:110-112.
25. Ma QP and Woolf CJ (1995) Noxious stimuli induce an N-methyl-D-aspartate receptor-dependent hypersensitivity of the flexion withdrawal reflex to touch: Implications for the treatment of mechanical allodynia Pain 61(Suppl 3):383-390.
26. Malmberg AB and Yaksh TL (1995) Cyclooxygenase inhibition and the spinal release of prostaglandin E2 and amino acids evoked by paw formalin injection: A microdialysis study in unanesthetized rats. J Neurosci 15(Suppl 4):2768-2776.
27. Mao J, Price DD and Mayer DJ (1994) Thermal hyperalgeaia in association with the development of morphine tolerance in rats: Role of excitatory amino acid receptors and protein kinase C. J Neurosci 14:2301-2312.
28. 2+ of NMDA responses in spinal cord neurones. Nature (Lond) 309:261-263.
29. Millian MJ and Seguin L (1994) Chemically-diverse ligands at the glycine B site coupled to N-methyl-D-aspartate (NMDA) receptors selectively block the late phase of formalin-induced pain in mice. Neurosci Lett 178:139-143.
30. 3H]5,7-Dichlorokynurenic acid recognises two binding sites in rat cerebral cortex membranes. J Recept Signal Transduct Res 18(Suppl 2 & 3):91-112.
31. Munson PJ and Rodbard D (1980) LIGAND: A versatile computerized approach for characterization of ligand-binding data. Anal Biochen 107:220-239.
32. Murphy DE, Hutchinson AJ, Hurt SD, Williams M and Sills MA (1988) Characterization of the binding of [3H]-CGS 19755: A novel N-methyl-D-aspartate antagonist with nanomolar affinity in rat brain. Br J Pharmacol 95(Suppl 3):932-938.
33. Neumann S, Doubell TP, Leslie T and Woolf CJ (1996) Inflammatory pain hypersensitivity mediated by phenotypic switch in myelinated primary sensory neurons. Nature (Lond) 384:360-364.
34. Ren K, Hylden JLK, Williams G, Ruda MA and Dubner R (1992) The intrathecal administration of excitatory amino acid receptor antagonists selectively attenu-ated carrageenan-induced behavioural hyperalgesia in rats. Eur J Pharmacol 219:235-243.
35. Sivilotti LG, Thompson SWN and Woolf CJ (1993) Rate of rise of the cumulative depolarization evoked by repetitive stimulation of small caliber afferents is a predictor action potential wind-up in rat spinal neurons in-vitro. J Neurophysiol 69:1621-1632.
36. Sluka KA and Westlund KN (1992) An experimental arthritis in rate: Dorsal horn aspartate and glutamate increases. Neurosci Lett 145(Suppl 2):141-144.
37. Smart D and Lambert DG (1996) The stimulatory effects of opioids and their possible role in the development of tolerance. Trends Pharmacol Sci 17:264-269.
38. Tang L and Aizenman E (1993) The modulation of N-methyl-D-aspartate receptors by redox and alkylating reagents in rat cortical neurones in vitro. J Physiol 465:303-323.
39. Thompson SWN, Gerber G, Sivilotti LG and Woolf CJ (1992) Long duration ventral root potentials in the neonatal rat spinal cord in vitro; the effects of ionotropic and metabotropic excitatory amino acids receptors antagonists. Brain Res 595:87-97.
40. Thompson SWN, Woolf CJ and Sivilotti LG (1993) Small-caliber afferent inputs produce a heterosynaptic facilitation of the synaptic responses evoked by primary afferents A-fibers in the neonatal rat spinal cord in-vitro. J Neurophysiol 69:2116-2128.
41. Woolf CJ and Thompson SWN (1991) The induction and maintenance of central sensitisation is dependent on NMDA receptor activation: Implications for the treatment of post-injury pain hypersensitivity states. Pain 44:293-299.