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- Volume 8, Issue 10, 2002
Current Pharmaceutical Design - Volume 8, Issue 10, 2002
Volume 8, Issue 10, 2002
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Amino-Alkyl-Cyclohexanes as a Novel Class of Uncompetitive NMDA Receptor Antagonists
Authors: W. Danysz, C.G. Parsons, A. Jirgensons, V. Kauss and J. TillnerBecause of its widespread involvement in the physiology and pathology of the CNS, the glutamatergic system has gained considerable attention as a potential target for development of new agents for a number of therapeutic indications. In this respect, the glutamate receptor subtype of the NMDA type has been most intensively studied. The present review describes the rational for developing amino-alkyl-cyclohexanes, as ne Read More
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NR2B Selective NMDA Receptor Antagonists
Authors: S.S. Nikam and L.T. MeltzerNR2B antagonists have received considerable attention in recent years. In this class of excitatory amino acid receptor antagonists NR2B antagonists have shown efficacy in neuroprotection, anti-hyperalgesic and anti-Parkinson animal models. Several groups are involved in developing these compounds as therapeutic agents and evaluating newer therapeutic targets for these agents. Until recently benzylpiperidine and Read More
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The AMPA Receptor Binding Site: Focus on Agonists and Competitive Antagonists
Authors: T. Stensbol, U. Madsen and P. Krogsgaard-LarsenIt is generally agreed that (S)-glutamic acid (Glu) receptors are involved in the development of a number of diseases in the central nervous system (CNS), and ligands that interact with these receptors are of significant interest. Selective ligands are indispensable as tools for the elucidation of the physiological role of AMPA receptors and as leads for the development of therapeutic agents. Over the last decade a wide variety of suc Read More
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Kainate Receptor Agonists, Antagonists and Allosteric Modulators
Authors: D. Bleakman, M.R. Gates, A.M. Ogden and M. MackowiakInterest in kainate receptors has increased over the past few years. Our understanding of their physiology and pharmacology has improved markedly since their original cloning and expression in the early 1990s. For example, agonist profiles at recombinant kainate receptors have been used to identify and distinguish kainate receptors in neurons. Furthermore, the development of selective antagonists for kainate recepto Read More
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The Role of Ionotropic Glutamate Receptors in Nociception with Special Regard to the AMPA Binding Sites
Authors: J.I. Szekely, K. Torok and G. MateThe recent literature on the antinociceptive action of ionotropic glutamate receptor antagonists is reviewed with special emphasis on their clinical potential. Actually the glutamatergic pathways descending from the brain stem into the spinal cord may generate analgesia. However, physiologically more important is that glutamate and aspartate are apparently the main neurotransmitters along the ascending nocicept Read More
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Non-competitive AMPA Antagonists of 2,3-Benzodiazepine Type
Authors: S. Solyom and I. TarnawaThe discovery of the selective AMPA antagonist character of 2,3-benzodiazepine derivative GYKI 52466 (5) in the late eighties and the recognition of the non-competitive nature of its mode of action some years later set off the world-wide search for novel class of drugs. Notably the quest to develop new antiepileptic and neuroprotective medicines, which allosterically inhibit the AMPA sensitive glutamate operated channels. T Read More
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AMPA Receptor Antagonists with Additional Mechanisms of Action: New Opportunities for Neuroprotective Drugs?
By T. WeiserIschaemic stroke of the brain accounts for about one third of all deaths in industrialized countries. Many of the patients who survive are severily impaired. Thus, there is an enormous need for pharmacotherapy for the treatment of ischaemic stroke.Why is such a treatment not available yet? Are the pathophysiological sequelae of brain ischaemia not well understood? Have there been no attempts for clinical development of n Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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