| Glutamatergic mechanisms in different disease states: overview and therapeutical implications -- an introduction. | |
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MedLine Citation:
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PMID: 12373529 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Glutamate is the most widely distributed excitatory transmitter in the central nervous system (CNS). It is acting via large - and still growing - families of receptors: NMDA-, AMPA-, kainate-, and metabotropic receptors. Glutamate has been implicated in a large number of CNS disorders, and it is hoped that novel glutamate receptor ligands offer new therapeutic possibilities in disease states such as chronic pain, stroke, epilepsy, depression, drug addiction and dependence or Parkinson's disease. While an extensive preclinical literature exists showing potential beneficial effects of NMDA-, AMPA-, kainate- and metabotropic receptor ligands, only NMDA receptor antagonists have been characterized clinically to any appreciable degree. In these trials it has been shown that while several compounds are therapeutically active, they also produce serious side effects at therapeutic doses. Current interest largely centers on the development of receptor subtype-selective compounds, namely compounds selective for receptors containing the NR2B subunit. Preclinical findings and the first clinical results are encouraging, and it may be that such subunit-selective compounds may have a sufficiently wide therapeutic window to be safe for human use. |
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Authors:
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T M Tzschentke |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Amino acids Volume: 23 ISSN: 0939-4451 ISO Abbreviation: Amino Acids Publication Date: 2002 |
Date Detail:
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Created Date: 2002-10-09 Completed Date: 2004-02-26 Revised Date: 2005-11-16 |
Medline Journal Info:
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Nlm Unique ID: 9200312 Medline TA: Amino Acids Country: Austria |
Other Details:
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Languages: eng Pagination: 147-52 Citation Subset: IM |
Affiliation:
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Grünenthal GmbH, Research and Development, Department of Pharmacology, Aachen, Germany. thomas.tzschentke@gruenthal.de |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Excitatory Amino Acid Antagonists / metabolism, therapeutic use* Glutamic Acid / metabolism* Humans Ligands Nervous System Diseases / drug therapy* Receptors, Glutamate / metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Excitatory Amino Acid Antagonists; 0/Ligands; 0/Receptors, Glutamate; 56-86-0/Glutamic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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