NMDA receptor antagonists as analgesics: focus on the NR2B subtype

Ifenprodil and a group of related compounds are selective antagonists of NR2B-containing NMDA receptors. These compounds are antinociceptive in a variety of preclinical pain models and have a much lower side-effect profile compared with other NMDA receptor antagonists. It remains unclear whether the...

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Bibliographic Details
Published in:Trends in Pharmacological Sciences 2001-12, Vol.22 (12), p.636-642
Main Authors: Chizh, Boris A, Headley, P.Max, Tzschentke, Thomas M
Format: Article
Language:English
Subjects:
Analgesics - pharmacology
Animals
dependence
Excitatory Amino Acid Antagonists - pharmacology
Humans
Ifenprodil
neurotoxicity
NMDA receptors
nociception
NR2B subunit
psychotomimetic action
Receptors, N-Methyl-D-Aspartate - drug effects
side-effects
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Summary:Ifenprodil and a group of related compounds are selective antagonists of NR2B-containing NMDA receptors. These compounds are antinociceptive in a variety of preclinical pain models and have a much lower side-effect profile compared with other NMDA receptor antagonists. It remains unclear whether the improved safety of these compounds is due to their subtype selectivity or to a unique mode of inhibition of the receptor. Human trials have so far confirmed the good tolerability of these subtype-selective NMDA receptor antagonists; however, whether they are as effective as other NMDA receptor antagonists in pain patients remains to be demonstrated. Ifenprodil and related compounds are selective antagonists of NR2B-containing NMDA receptors and might have broader spectrum of pain indications and lower side-effect profile than non-subtype-selective compounds.
ISSN:0165-6147
1873-3735
DOI:10.1016/S0165-6147(00)01863-0