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 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.
Chizh
B A
BA
Dept of Pharmacology, Grünenthal GmbH Research & Development, Zieglerstr. 6, 52078, Aachen, Germany. Boris_A_Chizh@gsk.com
Headley
P M
PM
Tzschentke
T M
TM
D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D006801:Humans; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects*
D000700:Analgesics; D018691:Excitatory Amino Acid Antagonists; C121001:NR2B NMDA receptor; D016194:Receptors, N-Methyl-D-Aspartate