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Neuroprotective Profile of Riluzole in In Vivo Models of Acute Neurodegenerative Diseases
J. M. Stutzmann,
F. Wahl,
J. Pratt,
V. Mary,
M. Reibaud,
E. Tecoult,
J. Rataud,
Corresponding Author
J. M. Stutzmann
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Address correspondence and reprint requests to Dr. J. M. Stutzmann, Rhône-Poulenc Rorer, CRVA, 13 quai Jules Ouesde, 94403 Vitry sur Seine Cedex, France. Fax: +33 (1) 55-71-3653.Search for more papers by this authorF. Wahl
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorJ. Pratt
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorV. Mary
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorM. Reibaud
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorE. Tecoult
Anesthesiology Department, Centre Hospitaller Universitaire de Limoges, Hopital Universitaire Dupuytren, 87042 Limoges Cedex, France.
Search for more papers by this authorJ. Rataud
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorJ. M. Stutzmann,
F. Wahl,
J. Pratt,
V. Mary,
M. Reibaud,
E. Tecoult,
J. Rataud,
Corresponding Author
J. M. Stutzmann
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Address correspondence and reprint requests to Dr. J. M. Stutzmann, Rhône-Poulenc Rorer, CRVA, 13 quai Jules Ouesde, 94403 Vitry sur Seine Cedex, France. Fax: +33 (1) 55-71-3653.Search for more papers by this authorF. Wahl
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorJ. Pratt
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorV. Mary
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorM. Reibaud
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this authorE. Tecoult
Anesthesiology Department, Centre Hospitaller Universitaire de Limoges, Hopital Universitaire Dupuytren, 87042 Limoges Cedex, France.
Search for more papers by this authorJ. Rataud
Neurodegenerative Diseases and Psychopharmacology Departments, Rhône-Poulenc Rorer, 94403 Vitry sur Seine Cedex, France.
Search for more papers by this author
References
- 1 Alaoui F, Pratt J, Trocherie S, Court L, Stutzmann JM. Acute effects of irradiation of the rat brain: Protection by glutamate blockade. Eur J Pharmacol 1995; 276: 55–60.
- 2 Aniksztejn L, Charriaut-Marlangue C, Roisin MP, Ben-Ari Y. Long-term potentiation in the rat hippocampus induced by the mast cell degranulating peptide: Analysis of the release of endogenous excitatory amino acids and proteins. Neuroscience 1990; 35: 63.
- 3 Bassant MH, Court L. Effects of whole body gamma irradiation on the activity of rabbit hippocampal neurons. Radial Res 1978; 75: 593–606.
- 4 Bath PMW. Treating acute ischemie stroke. Br Med J 1995; 311: 139–140.
- 5 Benavides J, Camelin JC, Mitrani N, et al. 2-Amino-6-trifluoromethoxy benzothiazole, a possible antagonist of excitatory amino acid neurotransmission. II. Biochemical properties. Neuropharmacology 1985; 24: 1085–1092.
- 6 Benoit E, Escande D. Riluzole specifically blocks inactivated Na+ channels in myelinated nerve fibre. Pflüger's Arch 1991; 419: 603–609.
- 7 Bensimon G, Lacomblez L, Meininger V, ALS/Riluzole Study Group. A controlled trial of riluzole in amyotrophic lateral sclerosis. N Engl J Med 1994; 330: 585–591.
- 8 Browne SE, McCulloch J. AMPA receptor antagonists and local cerebral glucose utilization in the rat. Brain Res 1994; 641: 10–20.
- 9 Cheramy A, Barbeito L, Godeheu G, Glowinski J. Riluzole inhibits the release of glutamate in the caudate nucleus of the cat in vivo. Neurosci Lett 1992; 147: 209–212.
- 10 Choi DW. Glutamate neurotoxicity and diseases of the central nervous system. Neuron 1988; 1: 623–634.
- 11 Collins GS. Some effects of excitatory amino acid receptor antagonists on synaptic transmission in the rat olfactory cortex slice. Brain Res 1982; 244: 311–318.
- 12 Davies SM, Albers GW, Diener ç-C, Lees KR, Norris J. Termination of acute stroke studies involving selfotel treatment. Lancet 1997; 349: 32.
- 13 Danysz W, Parsons CG, Bresink J, Quack G. Glutamate in CNS disorders. DN&P 1995; 8: 26l–277.
- 14 Debono MW, Le Guern J, Canton T, et al. Inhibition by riluzole of electrophysiological responses mediated by rat kainate and NMDA receptors expressed in Xenopus oocytes. Eur J Pharmacol 1993; 235: 283–289.
- 15 Demeyer I, Luther RR, Verhoeven FJS. SNX-111 in severe head injury: Preliminary results. Abstracts of the 6th International Symposium on Pharmacology of Cerebral Ischemia 1996; 94.
- 16 Diener HC, Hacke W, Hennerici M, et al. Lubeluzole in the acute treatment of ischemie stroke: Results of phase-2 trial. J Cereb Blood Flow Metab (Suppl) 1995; 15: S128.
- 17 Diener HC, Hacke W, Hennerici M, et al. Lubeluzole in acute ischemie stroke. A double-blind, placebo-controlled phase 11 trial. Stroke 1996; 27: 76–81.
- 18 Doble A, Hubert JP, Blanchard JC. Pertussis toxin pretreatment abolishes the inhibitory effect of riluzole and carbachol on D-[3H]aspartate release from cultured cerebellar granule cells. Neurosci Lett 1992; 140: 251–254.
- 19 Doble A, Perrier ML. Pharmacology of excitatory amino acid receptors coupled to inositol phosphate metabolism in neonatal rat striatum. Neurochem Int 1989; 15: 1–8.
- 20 Estevez A, Stutzmann JM, Barbeito L. Protective effect of riluzole on excitatory amino acid-mediated neurotoxicity in motoneuron-enriched cultures. Eur J Pharmacol 1995; 280: 47–53.
- 21 Fix AS, Long GG, Wozniak DF, Olney JW. Pathomorphologic effects of N-methyl-D-aspartate antagonists in the rat posterior cingulate/retrosplenial cerebral cortex: A review. Drug Dev Res 1994; 32: 147–152.
- 22 Gamzu ER. Update on cerestat clinical development. In: IBC, ed. Recent Advances in the Understanding, Therapy and Diagnosis of Ischemie Stroke. Southborough : IBC Inc, 1996.
- 23 Gill R, Lodge D. The neuroprotective effects of the decahydroisoquinoline, LY 215490; a novel AMPA antagonist in focal ischemia. Neuropharmacology 1994; 33: 1529–1536.
- 24 Girdlestone D, Dupuy A, Coston A, et al. D. Riluzole antagonizes excitatory amino acid-evoked firing in rat facial motoneurons in vivo. Br J Pharmacol (Suppl 583P) 1989; 97.
- 25 Greifenstein FE, DeVault M, Yoshitake J, Gajewski JE. A study of 1-aryl cyclohexylamine for anesthesia. Anesth Analg 1959; 31: 433–439.
- 26 Gueneau G, Privat A, Drouet J, Court L. Subgranular zone of the dentate gyrus of young rabbits as a secondary matrix. Develop Neurosci 1982; 5: 345–358.
- 27 Hacke W, Niedermaier N, Wildemann B. Thrombolytic therapy in acute ischemie stroke — an update. In: J Krieglstein, ed. Pharmacology of Cerebral Ischemia. Boca Raton : CRC Press, 1994; 617–623.
- 28 Hall E, Althaus J, Von Voigtlander P. Lazaroids: Neuroprotective antioxidant mechanisms. Can J Physiol Pharmacol (Suppl 1) 1994; 72: S26.3.
- 29 Hall ED. High glucose treatment improves neurological recovery in head-injury mice. J Neurosurg 1995; 62: 882–887.
- 30 Heros RC. Stroke: Early pathophysiology and treatment. Stroke 1994; 25: 1877–1881.
- 31 Hommel M, Bogousslavsky J. Thrombolytics in acute cerebral ischemia. Exp Opin Invest Drugs 1994; 3: 1011–1020.
- 32 Johnstone M, Evans V, Baigel S. Sernyl (CI-395) in clinical anesthesia. Br J Anaesth 1959; 96: 2S–135.
- 33 Kligerman MM, Turrisi AT, Urtasun RC, et al. Final report on phase 1 trial of WR-2721 before protracted fractionated radiation therapy. Int J Radiat Oncol Biol Phys 1988; 14: 1119–1122.
- 34 Kraus JF. Overview in epidemiology of traumatic brain injury. Abstracts 1st World Congress on Brain Injury 1995; 5.
- 35 Lacomblez L, Bensimon G, Nigel Leigh P, et al. Dose-ranging study of riluzole in amyotrophic lateral sclerosis. Lancet 1996; 347: 1425–1431.
- 36 Lea TJ, Ashley CC. Harmaline distribution in single muscle libres and the inhibition of sodium efflux. Biochim Biophys Acta 1981; 664: 74–81.
- 37 Leach MJ, Swan JH, Eisenthal D, et al. BW6I9C89, a glutamate release inhibitor, protects against focal cerebral ischemie damage. Stroke 1993; 24: 1063–1067.
- 38 Lees KR. Therapeutic interventions in acute stroke. Br J Clin Pharmacol 1992; 34: 486–493.
- 39 MacCown TJ, Givens BS, Breese GR. Amino acid influences on seizures elicited within the inferior colliculus. J Pharmacol Exp Ther 1987; 243: 603–608.
- 40 MacCulloch J. Excitatory amino acid antagonists and their potential for the treatment of ischemie brain damage in man. Br J Clin Pharmacol 1992; 34: 106–114.
- 41 Mackay KB, Kusumoto K, Graham Dl, MacCulloch J. Effect of the kappa-1 opioid agonist CI-977 on ischemie brain damage and cerebral blood flow after middle cerebral artery occlusion in the rat. Brain Res 1993; 629: 10–18.
- 42 Malgouris C, Bardot F, Daniel M, et al. Riluzole, a novel anti-glutamate, prevents memory loss and hip-pocampal neuronal damage in ischemie gerbils. J Neurosci 1989; 9: 3720–3727.
- 43 Martin D, Thompson MA, Nadler JV. The neuroprotective agent riluzole inhibits release of L-glutamate and L-aspartate from slices of hippocampal area CAI. Br J Pharmacol (Suppl) 1991; 104: 240P.
- 44 Mclntosh TK, Voddi M, Smith D, Stutzmann JM. Riluzole, a compound which interferes with glutamate neurotransmission, improves cognitive deficit following experimental brain injury in rats. J Neurotrauma 1995; 12: 379.
- 45 Mclntosh TK, Smith DH, Voddi M, Perri BR, Stutzmann JM. Riluzole, a novel neuroprotective agent, attenuates both neurological motor and cognitive dysfunction following traumatic brain injury in the rat. J Neurotrauma 1996; 13: 767–780.
- 46 Meldrum BS, Chapman AG. Excitatory amino acids and anticonvulsant drug action. In: L Hertz, E Kvamme, E McGeer, A Schousboe, eds. Glutamine, Glutamate and GABA in the Central Nervous System. New York : Alan R. Liss, 1983; 625–642.
- 47 Meldrum BS. Possible therapeutic applications of antagonists of excitatory amino acid neurotransmitters. Clin Sci 1985; 68: 113–122.
- 48 Meldrum BS, Garthwaite J. Excitatory amino acid neurotoxicity and neurodegenerative disease. Trends Pharmacol Sci 1990; 11: 379–387.
- 49 Meldrum BS. Amino acids as dietary excitotoxins: A contribution to understanding neurodegenerative disorders. Brain Res Rev 1993; 18: 293–314.
- 50 Millan MH, Chapman AG, Meldrum BS. Dual inhibitory action of enadoline (CI 977) on release of amino acids in the rat hippocampus. Etir J Pharmacol 1995; 279: 75–81.
- 51 Mizoule J, Meldrum B, Mazadier M, et al. 2-Amino-6-trifluoromethoxy benzothiazole, a possible antagonist of excitatory amino acid neurotransmission. I. Anticonvulsant properties. Neuropharmacology 1985; 24: 767–773.
- 52 Mottet I, Demeure R, Lucas M, et al. Neuroprotective effect of intravenous administration of Riluzole in focal cerebral ischemia in rats: Follow-up of the lesion development by magnetic resonance imaging 1997 (submitted).
- 53 Muir KW, Lees KR. Clinical experience with excitatory amino acid antagonist drugs. Stroke 1995; 26: 503–513.
- 54 Olney JW, Labruyere J, Wang G, et al. NMDA antagonist neurotoxicity mechanism and prevention. Scienee 1991; 254: 1515–1518.
- 55 Osikowska-Evers BA, Wihelm D, Nebel U, et al. The effects of the novel neuroprotective compound lubeluzole on sodium current and veratridine induced sodium load in rat brain neurons and synaptosomes. J Cereb Blood Flow Melab (Suppl) 1995; 15: S380.
- 56 Pratt J, Rataud J, Bardot F, et al. Neuroprotective action of riluzole in rodent models of global and focal cerebral ischemia. Neurosci Lett 1992; 140: 251–254.
- 57 Rataud J, Malgouris C, Bardot F, et al. Neuronal protection by riluzole against ischemie brain damage in gerbils. In: J Krieglstein, ed. Pharmacology of Cerebral Ischemia. Boca Raton : CRC Press, 1988; 261–264.
- 58 R & D focus. 1995;4: 8.
- 59 R & D focus. 1996;5: 6.
- 60 Rotlunan SM, Olney JW. Glutamate and the pathophysiology of hypoxic-ischemic brain damage. Ann Neuroi 1986; 19: 105–111.
- 61 Sandercock P, Willems H. Medical treatment of acute ischemie stroke. Lancet 1992; 339: 537–539.
- 62
Scatton B,
Benavides J,
Carter C, et al.
The NMDA macromolecular complex as a target for the development of anti-ischemic drugs.
Clin Neuropharmacol
1992; 15: S133–437.
10.1097/00002826-199201001-00357 Google Scholar
- 63 Scheller D, Kolb J, Szathmary S, Zacharias E, et al. Extracellular changes of glutamate in the periinfarct zone. Effect of lubeluzole. J Cereb Blood Flow Melab (Suppl) 1995; 15: S379.
- 64 Sila CA. Prophylaxis and treatment of stroke. Drugs 1993; 45: 329–337.
- 65 Smith SE, Lekieffre D, Sowinski P, Meldrum BS. Cerebroprotective effect of BW619C89 after focal or global cerebral ischemia in the rat. Neuroreport 1993; 4: 1339–1342.
- 66 Stoehr SJ, Campbell GW, Rock DM. The NMDA receptor antagonists Ifenprodil and Eliprodil blocked voltage-gated Na+ channels. Abstr Am Soc Neurosci 1996; 22: 33–32.
- 67 Strategies in stroke treatment and prophylaxis. Pharma Projects. Executive Briefing. February 1995; 25–29.
- 68 Stutzmann JM, Böhme GA, Gandolfo G, et al. Riluzole prevents hyperexcitability produced by the mast cell degranulating peptide and dentrotoxin I in the rat. Eur J Pharmacol 1991; 193–223.
- 69 Stutzmann JM, Pratt J, Boraud T, Gross C. Riluzole's Effect on post-traumatic spinal cord injury in the rat. Neuroreport 1996; 7(2): 387–392.
- 70 Stutzmann JM, Doble A. Blockade of glutaminergic transmission and neuroprotection: The strange case of riluzole. In: G Jolles, JM Stutzmann, eds. Neurodegenerative Disease. New York : Academic Press, 1994; 205–214.
- 71 Sun FY, Faden AI. Neuroprotective effects of 619C89, a use-dependent sodium channel blocker, in rat traumatic brain injury. Brain Res 1995; 673: 133–140.
- 72 Tannira A, Graham Dl, MacCulloch J, Teasdale GM. Focal cerebral ischemia in the rat: I. Description of technique and early neuropathological consequences following middle cerebral artery occlusion. J Cereb Blood Flow Metab 1981; 1: 53–60.
- 73 Taylor C, Tsai C, Lehmann J. Sodium fluxes modulating neuronal glutamate uptake: Differential effects of local anesthetic and anticonvulsant drugs. J Pharmacol Exp Ther 1988; 244: 666–673.
- 74 Taylor CP, Vartanian MG. Probenecid pretreatment enhances anticonvulsant action of NBQX in mice. Eur J Pharmacol 1992; 213: 151–153.
- 75 The American Nimodipine Study Group. Clinical trial of nimodipine in acute ischemie stroke. Stroke 1992; 23: 3–8.
- 76 Turkei CC. Is stroke penumbra the victim of lactate neurotoxicity. In: IBC, ed. Recent Advances in the Understanding, Therapy and Diagnosis of Ischemia Stroke. Southborough : IBC Inc, 1996.
- 77 Wahl F, Allix M, Plotkine M, Boulu RG. Effects of riluzole on focal cerebral ischemia in rats. Eur J Pharmacol 1993; 230: 209–214.
- 78 Wauquier A, Ashton D, Clincke G, Niemegeers CJE. Anti-hypoxic effects of etomidate, thiopental and methohexital. Arch Int Pharmacodyn Ther 1981; 249: 330–334.
- 79 Yum SW, Saden AI. Comparison of the neuroprotective effects of N-methyl-D-aspartate antagonist MK-801 and the opiate-receptor antagonist nalmefene in experimental spinal cord ischemia. Arch Neural 1990; 47: 277–281.
