N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics.
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.
Brown
Dean G
DG
AstraZeneca Pharmaceuticals, Lead Generation Department, 1800 Concord Pike, Wilmington, DE 19850, USA. dean.brown@astrazeneca.com
Krupp
Johannes J
JJ
D000700:Analgesics / Q000627:therapeutic use; D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000627:therapeutic use; D006146:Guanidines / Q000627:therapeutic use; D006801:Humans; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology
D000700:Analgesics; D018691:Excitatory Amino Acid Antagonists; D006146:Guanidines; D016194:Receptors, N-Methyl-D-Aspartate