Review of NMDA antagonist-induced neurotoxicity and implications for clinical development

International Journal of Clinical Pharmacology and Therapeutics

Volumn 42, Issue 1, 2004, Pages 1-14

  Low, S J ^a   Roland, C L ^a  

^a Cognetix Inc ^*  (United States)

Author keywords

CGX 1007; MK 801; Neurodegeneration; Neurotoxicity; NMDA antagonist; Vacuolization

Indexed keywords

6 NITRO 7 SULFAMOYLBENZO[F]QUINOXALINE 2,3 DIONE; ATROPINE; BARBITURIC ACID DERIVATIVE; BENZATROPINE; BIPERIDEN; CLONIDINE; CLOZAPINE; DIAZEPAM; DIPHENHYDRAMINE; DIZOCILPINE; FLUOXETINE; FLUPERLAPINE; GUANABENZ; HALOTHANE; HEAT SHOCK PROTEIN; HEAT SHOCK PROTEIN 70; ISOFLURANE; KETAMINE; LISURIDE; LOXAPINE; LYSERGIDE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; OLANZAPINE; PHENCYCLIDINE; PROPOFOL; SCOPOLAMINE; TILETAMINE; TRIHEXYPHENIDYL; UNINDEXED DRUG; XYLAZINE;

AGE; ATAXIA; BEHAVIOR DISORDER; BRAIN CELL; BRAIN INJURY; BRAIN REGION; CELL DEATH; CELL VACUOLE; DOSE RESPONSE; DRUG EXPOSURE; DRUG INDUCED DISEASE; DRUG RESEARCH; EPILEPSY; FEMALE; GABAERGIC SYSTEM; GUINEA PIG; HISTOCHEMISTRY; HUMAN; IMMOBILIZATION; INHIBITION KINETICS; MALE; MEDICAL ASSESSMENT; METHODOLOGY; MOUSE; NERVE CELL; NERVE CELL DEGENERATION; NERVE FIBER DEGENERATION; NEUROLOGIC DISEASE; NEWBORN; NONHUMAN; PAIN; PARKINSON DISEASE; PRACTICE GUIDELINE; PROTEIN INDUCTION; RAT; REVIEW; RHESUS MONKEY; SAMPLING; SEIZURE; SENSITIVITY ANALYSIS; SEX DIFFERENCE; SPECIES DIFFERENCE; STROKE; TIME;

EID: 0346505342     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/CPP42001     Document Type: Review

References (77)

1. Allen HL 1990 Phencyclidine, dizocilpine and cerebrocortical neurons. Science 247: 221
2. Andine P, Axelsson R et al 1995 The effect of anosmia on MK-801-induced behaviour in mice. Neurosci Lett 190: 113-116
3. Auer RN 1994 Assessing structural changes in the brain to evaluate neurotoxicological effects of NMDA receptor antagonists. Psychopharmacol Bull 30: 585-591
4. Auer RN 1996 Effect of age and sex on N-methyl-D-aspartate antagonist-induced neuronal necrosis in rats. Stroke 27: 743-746
5. Auer RN, Coulter KC 1994 The nature and time course of neuronal vacuolation induced by the N-methyl-D-aspartate antagonist MK-801. Acta Neuropathol 87: 1-7
6. Auer RN, Coupland SG et al 1996 Postischemic therapy with MK-801 (dizocilpine) in a primate model of transient focal brain ischemia. Mol Chem Neuropathol 29: 193-210
7. Beltramino CA, de Olmos JS et al 1993 Silver staining as a tool for neurotoxic assessment NIDA. Res Monogr 136: 101-126
8. Berger P, Farrel K et al 1994 Drugs acting at the strychnine-insensitive glycine receptor do not induce HSP70 protein in the cingulate cortex. Neurosci Lett 168: 147-150
9. Bloom FE 1996 Neurotransmission and the central nervous system. In: Joel LEL, Hardman G, Molinoff PB, Ruddon RW (eds) Goodman and Gilman's The Pharmacological Basis of Therapeutics (9th ed). McGraw-Hill, New York
10. Chenard BL, Menniti FS 1999 Antagonists selective for NMDA receptors containing the NR2B subunit. Curr Pharm Des 5: 381-404
11. Colbourne F, Rakic D et al 1999 The effects of temperature and scopolamine on N-methyl-D-aspartate antagonist-induced neuronal necrosis in the rat. Neuroscience 90: 87-94
12. Cory-Slechta DA 1994 The impact of NMDA receptor antagonists on learning and memory functions. Psychopharmacol Bull 30: 601-612
13. Cull-Candy S, Brickley S et al 2001 NMDA receptor subunits: diversity, development and disease. Curr Opin Neurobiol 11: 327-335
14. Dingledine R, Borges K et al 1999 The glutamate receptor ion channels. Pharmacol Rev 51: 7-61
15. Doble A 1995 Excitatory amino acid receptors and neurodegeneration. Therapy 50: 319-337
16. Ellison G 1994 Competitive and noncompetitive NMDA antagonists induce similar limbic degeneration. Neuro-report 5: 2688-2692
17. 2-adrenergic agonists prevent MK-801 neurotoxicity. Neuropsychopharmacology 12: 347-349
18. Farber NB, Faster J et al 1996 Olanzapine and fluperlapine mimic clozapine in preventing MK-801 neurotoxicity. Schizophr Res 21: 33-37
19. Farber NB, Hanslick J et al 1998 Serotonergic agents that activate 5HT2A receptors prevent NMDA antagonist neurotoxicity. Neuropsychopharmacology 18: 57-62
20. Farber NB, Jiang XP et al 2002 Antiepileptic drugs and agents that inhibit voltage-gated sodium channels prevent NMDA antagonist neurotoxicity. Mol Psychiatry 7: 726-733
21. Farber NB, Kim SH et al 2002 Receptor mechanisms and circuitry underlying NMDA antagonist neurotoxicity. Mol Psychiatry 7: 32-43
22. Farber NB, Wozniak DF et al 1995 Age-specific neurotoxicity in the rat associated with NMDA receptor blockade: potential relevance to schizophrenia? Biol Psychiatry 38: 788-796
23. Fix AS, Horn JW et al 1993 Neuronal vacuolization and necrosis induced by the noncompetitive N-methyl-D-aspartate (NMDA) antagonist MK(+)801 (dizocilpine maleate): a light and electron microscopic evaluation of the rat retrosplenial cortex. Exp Neurol 123: 204-215
24. Fix AS, Wozniak DF et al 1995 Quantitative analysis of factors influencing neuronal necrosis induced by MK-801 in the rat posterior cingulate/retrosplenial cortex. Brain Res 696: 194-204
25. Fujimura M, Hashimoto K et al 2000 Effects of anti-psychotic drugs on neurotoxicity, expression of fos-like protein and c-fos mRNA in the retrosplenial cortex after administration of dizocilpine. Eur J Pharmacol 398: 1-10
26. Grotta J 1994 Safety and tolerability of the glutamate antagonist CGS19755 in acute stroke patients. Stroke 25: 255
27. Haggerty GC, Brown G 1996 Neurobehavioral profile of subcutaneously administered MK-801 in the rat. Neurotoxicology 17: 913-921
28. Hargreaves EL, Cain DP 1992 Hyperactivity, hyper-reactivity and sensorimotor deficits induced by low doses of the N-methyl-D-aspartate noncompetitive channel blocker MK-801. Behav Brain Res 47: 23-33
29. Hargreaves RJ, Hill RG et al 1994 Neuroprotective NMDA antagonists: the controversy over their potential for adverse effects on cortical neuronal morphology. Acta Neurochir Suppl 60: 15-19
30. Hargreaves RJ, Rigby M et al 1993 Competitive as well as uncompetitive N-methyl-D-aspartate receptor antagonists affect cortical neuronal morphology and cerebral glucose metabolism. Neurochem Res 18: 1263-1269
31. Hashimoto K, Minabe Y et al 1997 Expression of cyclo-oxygenase-2 mRNA in rat retrosplenial cortex following administration of phencyclidine. Brain Res 762: 259-263
32. Hawkinson JE, Huber KR et al 1997 The N-methyl-D-aspartate (NMDA) receptor glycine site antagonist ACEA 1021 does not produce pathological changes in rat brain. Brain Res 744: 227-234
33. Herrling PL 1994 D-CPPene (DSZ EAA 494), a competitive NMDA antagonist: results from animal models and first results in humans. Neuropsychopharmacology 10: 591S
34. Hetman M, Danysz W et al 1997 Increased expression of cathepsin D in retrosplenial cortex of MK-801-treated rats. Exp Neurol 147: 229-237
35. Hof PR, Vissavajjhala P et al 1996 Distribution of glutamate receptor subunit proteins GluR2(4), GluR5/6/7 and NMDAR1 in the canine and primate cerebral cortex: a comparative immunohistochemical analysis. Brain Res 723: 77-89
36. Horvath ZC, Czopf J et al 1997 MK-801-induced neuronal damage in rats. Brain Res 753: 181-195
37. Ishimaru M, Fukamauchi F et al 1995 Halothane prevents MK-801 neurotoxicity in the rat cingulate cortex. Neurosci Lett 193: 1-4
38. Jevtovic-Todorovic V, Kirby CO et al 1997 Isoflurane and propofol block neurotoxicity caused by MK-801 in the rat posterior cingulate/retrosplenial cortex. J Cereb Blood Flow Metab 17: 168-174
39. Jevtovic-Todorovic V, Wozniak DF et al 1998 Clonidine potentiates the neuropathic pain-relieving action of MK-801 while preventing its neurotoxic and hyperactivity side effects. Brain Res 781: 202-211
40. Jevtovic-Todorovic V, Wozniak DF et al 2001 Propofol and sodium thiopental protect against MK-801-induced neuronal necrosis in the posterior cingulate/retrosplenial cortex. Brain Res 913: 185-189
41. Johnson KM, Phillips M et al 1998 Chronic phencyclidine induces behavioral sensitization and apoptotic cell death in the olfactory and piriform cortex. J Neurosci Res 52: 709-722
42. Katsuta K, Nakanishi H et al 1995 The neuroprotective effect of the novel noncompetitive NMDA antagonist, FR115427 in focal cerebral ischemia in rats. J Cereb Blood Flow Metab 15: 345-348
43. Kilander K, Williams H 1992 Yohimbine reduces neuropathology induced by ketamine/xylazine anesthesia. Physiol Behav 51: 657-659
44. Koek W, Woods JH et al 1988 MK-801, a proposed noncompetitive antagonist of excitatory amino acid neurotransmission, produces phencyclidine-like behavioral effects in pigeons, rats and rhesus monkeys. J Pharmacol Exp Ther 245: 969-974
45. Konopka D, Szklarczyk AW et al 1998 Plasticity- and neurodegeneration-linked cyclic-AMP responsive element modulator/inducible cyclic-AMP early repressor messenger RNA expression in the rat brain. Neuroscience 86: 499-510
46. Kristensen JD, Svensson B et al 1992 The NMDA-receptor antagonist CPP abolishes neurogenic "wind-up pain" after intrathecal administration in humans. Pain 51: 249-253
47. Lan JQ, Chen J et al 1997 Induction of heat-shock protein (HSP72) in the cingulate and retrosplenial cortex by drugs that antagonize the effects of excitatory amino acids. Brain Res Mol Brain Res 46: 297-302
48. Leber, P 1994 Psychotherapeutic Medications Development Program (PMDP) Workshop on NMDA Receptor Antagonists: neurotoxicity evaluation. Introduction. Psychopharmacol Bull 30: 527-532
49. Li Q, Clark S et al 2002 NMDA receptor antagonists disinhibit rat posterior cingulate and retrosplenial cortices: a potential mechanism of neurotoxicity. J Neurosci 22: 3070-3080
50. Lynch DR, Guttmann RP 2001 NMDA receptor pharmacology: perspectives from molecular biology. Curr Drug Targets 2: 215-231
51. Lynch DR, Guttmann RP 2002 Excitotoxicity: perspectives based on N-methyl-D-aspartate receptor subtypes. J Pharmacol Exp Ther 300: 717-723
52. Matsuki H, Shirayama Y et al 2001 Effects of age and gender on the expression of brain-derived neurotrophic factor mRNA in rat retrosplenial cortex following administration of dizocilpine. Neuropsychopharmacology 25: 258-266
53. Mattson MP, Rychlik B et al 1992 Degenerative and axon outgrowth-altering effects of phencyclidine in human fetal cerebral cortical cells. Neuropharmacology 31: 279-291
54. Morimoto T, Hashimoto K et al 2002 Neuropharmacological profile of a novel potential atypical antipsychotic drug Y-931 (8-fluoro-12-(4-methylpiperazin-1-yl)-6H-[1]benzothieno[2,3-b][1,5] benzodiazepine maleate). Neuropsychopharmacology 26: 456-467
55. Nikam SS, Meltzer LT 2002 NR2B-selective NMDA receptor antagonists. Curr Pharm Res 8: 845-855
56. O'Callaghan JP 1994 Biochemical analysis of glial fibrillary acidic protein as a quantitative approach to neurotoxicity assessment: advantages, disadvantages and application to the assessment of NMDA receptor antagonist-induced neurotoxicity. Psychopharmacol Bull 30: 549-554
57. Olney JW 1994 Neurotoxicity of NMDA receptor antagonists: an overview. Psychopharmacol Bull 30: 533-540
58. Olney JW, Farber NB 1994 Efficacy of clozapine compared with other antipsychotics in preventing NMDA antagonist neurotoxicity. J Clin Psychiatry 55 (Suppl B): 43-46
59. Olney JW, Labruyere J et al 1989 Pathological changes induced in cerebrocortical neurons by phencyclidine and related drugs. Science 244: 1360-1362
60. Olney JW, Labruyere J et al 1991 NMDA antagonist neurotoxicity: mechanism and prevention. Science 254: 1515-1518
61. Parsons CG, Danysz W et al 1999 Memantine is a clinically well-tolerated N-methyl-D-aspartate (NMDA) receptor antagonist - a review of preclinical data. Neuropharmacology 38: 735-767
62. Paule MG 1994 Acute behavioral toxicity of MK-801 and phencyclidine: effects on rhesus monkey performance in an operant test battery. Psychopharmacol Bull 30: 613-621
63. Pearlstein RD, Beirne JP et al 1998 Neuroprotective effects of NMDA receptor glycine recognition site antagonism: dependence on glycine concentration. J Neurochem 70: 2012-2019
64. Raboisson P, Flood K et al 1997 MK-801 neurotoxicity in the guinea pig cerebral cortex: susceptibility and regional differences compared with the rat. J Neurosci Res 49: 364-371
65. Sahai S 1990 Glutamate in the mammalian CNS. Eur Arch Psychiatry Clin Neurosci 240: 121-133
66. Schmued LC, Hopkins KJ 2000 Fluoro-Jade B: a high affinity fluorescent marker for the localization of neuronal degeneration. Brain Res 874: 123-130
67. Sharp FR, Butman M et al 1994 Neuronal injury produced by NMDA antagonists can be detected using heat shock proteins and can be blocked with antipsychotics. Psychopharmacol Bull 30: 555-560
68. Sharp FR, Butman M et al 1992 Haloperidol prevents induction of the HSP70 heat shock gene in neurons injured by phencyclidine (PCP), MK-801 and ketamine. J Neurosci Res 33: 605-616
69. Sonders MS, Keana JF et al 1988 Phencyclidine and psychotomimetic sigma opiates: recent insights into their biochemical and physiological sites of action. Trends Neurosci 11: 37-40
70. Switzer RC 2002 A higher standard for assessing neurotoxicity. http://www.neuroscienceassociates.com/htmls/higherstandard.html
71. Switzer RC 3rd 1991 Strategies for assessing neurotoxicity. Neurosci Biobehav Rev 15: 89-93
72. Tomitaka M, Tomitaka S et al 2000 Fluoxetine prevents PCP- and MK-801-induced HSP70 expression in injured limbic cortical neurons of rats. Biol Psychiatry 47: 836-841
73. Tomitaka SI, Hashimoto K et al 1997 Regionally different effects of scopolamine on NMDA antagonist-induced heat shock protein HSP70. Brain Res 763: 255-258
74. Willetts J, Balster RL et al 1990 The behavioral pharmacology of NMDA receptor antagonists. Trends Pharmacol Sci 11: 423-428
75. Wozniak DF, Brosnan-Watters G et al 1996 MK-801 neurotoxicity in male mice: histologic effects and chronic impairment in spatial learning. Brain Res 707: 165-179
76. Wozniak DF, Olney JW et al 1990 Behavioral effects of MK-801 in the rat. Psychopharmacology 101: 47-56
77. Ye X, Carp RI et al 2001 Fluoro-Jade and silver methods: application to the neuropathology of scrapie, a transmissible spongiform encephalopathy. Brain Res Brain Res Protoc 8: 104-112