Abstract
NMDA receptors are known to be involved in nociceptive transmission and pain processing. Many structurally diverse NMDA antagonists have been reported to have activity in both animal models and clinical models of neuropathic pain. Untoward side effects such as ataxia and sedation have severely limited the clinical uses of this class of potential therapeutics. However, antagonists at the glycine-site, NR2B sites and weak-binding channel blockers have demonstrated an improved side effect profile in animal models of pain. These types of compounds may hold potential promise for future pain therapies. This review covers reported pain data surrounding representative examples of NMDA antagonists and provides a current assessment of potential clinical utility.
Keywords: Sensitization, Chronic neuropathic pain, nociceptive events, Non-Competitive NMDA Receptor Antagonists, glutamate-competitive antagonists, spermidine
Current Topics in Medicinal Chemistry
Title: N-Methyl-D-Aspartate Receptor (NMDA) Antagonists as Potential Pain Therapeutics
Volume: 6 Issue: 8
Author(s): Dean G. Brown and Johannes J. Krupp
Affiliation:
Keywords: Sensitization, Chronic neuropathic pain, nociceptive events, Non-Competitive NMDA Receptor Antagonists, glutamate-competitive antagonists, spermidine
Abstract: NMDA receptors are known to be involved in nociceptive transmission and pain processing. Many structurally diverse NMDA antagonists have been reported to have activity in both animal models and clinical models of neuropathic pain. Untoward side effects such as ataxia and sedation have severely limited the clinical uses of this class of potential therapeutics. However, antagonists at the glycine-site, NR2B sites and weak-binding channel blockers have demonstrated an improved side effect profile in animal models of pain. These types of compounds may hold potential promise for future pain therapies. This review covers reported pain data surrounding representative examples of NMDA antagonists and provides a current assessment of potential clinical utility.
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Cite this article as:
Brown G. Dean and Krupp J. Johannes, N-Methyl-D-Aspartate Receptor (NMDA) Antagonists as Potential Pain Therapeutics, Current Topics in Medicinal Chemistry 2006; 6 (8) . https://dx.doi.org/10.2174/156802606777057571
DOI https://dx.doi.org/10.2174/156802606777057571 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |

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