development of the nmda ion-channel blocker, aptiganel hydrochloride, as a neuroprotective agent for acute cns injury

International Review of Neurobiology

Volumn , Issue 40, 1996, Pages 173-195

  McBurney, Robert N ^a  

^a CeNeS Pharmaceuticals plc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

APTIGANEL; GUANIDINE DERIVATIVE; N METHYLASPARTIC ACID; NEUROPROTECTIVE AGENT; NEW DRUG;

ACUTE DISEASE; BRAIN INJURY; CEREBROVASCULAR DISEASE; CHEMISTRY; CLINICAL TRIAL; DRUG ANTAGONISM; GLASGOW COMA SCALE; HUMAN; METABOLISM; PATHOPHYSIOLOGY; REFERENCE VALUE; REVIEW; SPINAL CORD INJURY;

ACUTE DISEASE; BRAIN INJURIES; CEREBROVASCULAR DISORDERS; CLINICAL TRIALS; DRUGS, INVESTIGATIONAL; GLASGOW COMA SCALE; GUANIDINES; HUMANS; N-METHYLASPARTATE; NEUROPROTECTIVE AGENTS; REFERENCE VALUES; SPINAL CORD INJURIES;

EID: 0030635685     PISSN: 00747742     EISSN: None     Source Type: Book Series    
DOI: 10.1016/s0074-7742(08)60720-5     Document Type: Article

References (28)

1. Albers, G.W., Atkinson, R.P., Kelley, R.E. & Rosenbaum, D.M. on behalf of the Dextrorphan Study Group (1995) Safety, tolerability, and pharmacokinetics of the N-methyl-D-aspartate antagonist dextrorphan in patients with acute stroke. Stroke 26, 254-258.
2. Barnes, D.M. (1988) NMDA receptors trigger excitement. Science 239, 254-256.
3. Block, G.A. for the 1102-003 Study Group (1995) Final results from a dose-escalating safety and tolerance study of the non-competitive NMDA antagonist CNS 1102 in patients with acute cerebral ischaemia. Stroke 26, 185.
4. Choi, S.C., Barnes, M.S., Bullock, R., Germanson, T.A., Marmarou, A. & Young, H. (1994) Temporal profile ofoutcomes in severe head injuryj. Neurosurg, 81, 169-173.
5. Cotman, C.W. & Iversen, L.L. (1987) Excitatory amino acids in the brain - focus on NMDA receptors. Trends Xeurosci. 10, 263-265.
6. del Zoppo, GJ. (1995) Acute stroke. On the threshold of a therapy? New Engl. J. Med. 333, 1632-1633.
7. Dingledine, R. (1986) NMDA receptors: \vhat do they do? Trends Murosci. 9, 47-49.
8. Fayad, P.B., Edwards, K., Hormes, J. & Lees, K.R. (1996) The safety and tolerability of non weight-adjusted doses of aptiganel HC1 (CERESTAT®) in acute ischaemic stroke patients. A. H.A. February 1996.
9. Gamzu, E.R. for the CNS 1102-002 Study Group (1994) CERESTAT™ (CNS 1102) an NMDA antagonist in severe traumatic brain injury. A. JVC A. October 1994.
10. Ginsberg, M. (1995a) Neuroprotection in brain ischaemia: an update Part I. Neurosci. 1,95-103.
11. Ginsberg, M. (1995b) Neuroprotection in brain ischaemia: an update Part II. Neurosci. 1, 164-175.
12. Ginsberg, M.D., Sternau, L.L., Globus, M.Y.-T, Dietrich, W.D. & Busto, R. (1992) Therapeutic modulation of brain temperature: relevance to ischaemic brain injury. Cerebrorasc. Brain Aletab. Rev. 4, 189-225.
13. Grotta, J., Clark, W, Coull, B., Pettigrew, L.C., Mackay, B., Goldstein, L.B., Meissner, I., Murphy, D. & LaRue, L. (1995) Safety and tolerability of the glutamate antagonist CGS 19 755 (selfotel) in patients with acute ischaemic stroke. Stroke 26, 602-605.
14. Kemp, J.A., Foster, A.C. & Wong, E.H.F. (1987) Non-competitive antagonists of excitatory amino acid receptors. Trends j\eurosci. 10, 294-298.
15. Kirk, C.J., Reddy, N.L., Fischer, J.B., Wolcott, T.C., Knapp, A.G. & McBurney, R.N. (1994) In titra neuroprotection by substituted guanidines with varying affinities for the N-methyl-D-aspartate receptor ionophore and for sigma sites:,)'. Pharmaeol. Exp. Ther. 271, 1080-85.
16. McBurney, R.N. (1994) Therapeutic potential of NMDA antagonists in neurodegenerative diseases. Murobiol. Aging. 15,271-273.
17. McCullochJ., Bullock, R. & Teasdale, G.M. (1992) Excitatory Amino Acid Antagonists: Opportunities for the Treatment of Ischaemic Brain Damage in Alan (ed. Meldrum, B.), pp. 287-326. Blackwell Scientific, Oxford.
18. Meadows, M.-E., Fisher, M. & Minematsu, K. (1994) Delayed treatment with a noncompetitive NMDA antagonist, CNS-1102, reduces infarct size in rats. Cerebrofasc, Dis. 4, 26-31.
19. Minematsu, K., Fisher, M., Li, L., Davis, M.A., Knapp, A.G., Cotter, R.E., McBurney, R.N. & Sotak, C.H. (1993a) Effects of a novel NMDA antagonist on experimental stroke rapidly and quantitatively assessed by diffusion-weighted MRI. Neural. 43, 397-403.
20. Minematsu, K., Fisher, M., Li, L. & Sotak, C. (1993b) Diffusion and perfusion MRI studies to evaluate a non-competitive NMDA antagonist and reperfusion in experimental stroke in rats. Stroke 24, 2074-2081.
21. Muir, K.W., Grossct, D.G., Gamzu, E. & Lees, K.R. (1994) Pharmacological effects of the noncompetitive NMDA antagonist CNS 1102 in normal volunteers. Br. J. Clin. Pharmaeol. 38, 33-38.
22. Muir, K.W. & Lees, K.R. (1995) Clinical experience with excitatory amino acid antagonist drugs. Stroke 26, 503-513.
23. NINDS rt-PA Stroke Study Group (1995) Tissue plasminogen activator for acute ischaemic stroke. JtewEngl.J. Med. 333, 1581-1587.
24. Olney,J.W., Labruyere, J. & Price, M.T. (1989) Pathological changes induced in cerebrocortical neurones by phencyclidine and related drugs. Science 244, 1360-1362.
25. Park, C.K., McBurney, R.N., Holt, W.F., Cotter, R.E., McCullochJ., KangJ.K. & Choi, G.G. (1993) The dose-dependency of the antischaemic efficacy and of the side effects of a novel NMDA antagonist, CNS 1102. J. Cereb. Blood Flow Metab. 13, 641.
26. Reddy, N.L., Hu, L.-Y., Cotter, R.E., Fischer, J.B., Wong, WJ., McBurney, R.N., Weber, E., Holmes, D.L., Wong, S.T., Prasad, R. & KeanaJ.F.W. (1994) Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(l-Naphythyl)-N'-(3-ethyIphenyl)-N'methylguanidine: A new, selective non-competitive NMDA receptor antagonist. J. Med. Chem. 37, 260-267.
27. Wang, S., Zhou, D., Fischer, J.B., Knapp, A.G. & Holt, W.F. (1995) CNS 1102 protects against brain damage due to hypoxic ischaemia (HI) in the neonatal rat. Soc. Neurosci. Abstr. 21, 995.
28. Wong, E.H.R. & KempJ.A. (1991) Sites for antagonism on the JV-methyl-D-aspartate receptor channel complex. Ann. Rev. Pharmaeol. Toxicol. 31, 401-425.