Open-channel blockers of the NMDA receptor complex

Benedict C. Albensi, Erin Ilkanich, Mark Mattson, Jennifer Liang

Research output: Contribution to journalArticle

Abstract

A variety of compounds have been shown to limit or prevent excitotoxicity by blocking N-methyl-D-aspartate (NMDA) receptor-mediated neurotransmission. However, many first-generation NMDA antagonists did not live up to clinical expectations in trials of acute brain injury because of the manifestation of multiple side effects. In spite of this, development of NMDA antagonists continues, where some of the newer agents block excitotoxicity through alternative mechanisms. For example, blockers selective to the NR2B subunit or agents that block metabotropic glutamate receptors or α-amino-3-hydroxy-5- methyl-4-isoxazolepropionic acid receptors are currently under investigation. Several years ago, the arylalkylamine spider toxins were demonstrated to function as open-channel blockers similar to memantine, which was very recently approved by the U.S. FDA for use in patients with Alzheimer's dementia. With this said, programs focusing on NMDA antagonism via alternative mechanisms may still hold promise for treating acute injury and even chronic forms of dementia.

Original languageEnglish (US)
Pages (from-to)557-562
Number of pages6
JournalDrug News and Perspectives
Volume17
Issue number9
DOIs
StatePublished - Nov 2004
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology

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    Albensi, B. C., Ilkanich, E., Mattson, M., & Liang, J. (2004). Open-channel blockers of the NMDA receptor complex. Drug News and Perspectives, 17(9), 557-562. https://doi.org/10.1358/dnp.2004.17.9.872569