Advances in pain therapeutics.
Recent work in defining molecular targets for neuropathic pain has been plentiful and varied. Three novel targets have received much attention recently: N-methyl-D-aspartate receptor subtypes such as the glycine and NR2B sites, and the tetrodotoxin-resistant voltage-gated sodium channel (Na(v) 1.8; SNS/PN3). Preclinical data have been encouraging as a number of selective NR2B and glycine site antagonists have shown efficacy in animal models. Selective Na(v) 1.8 channel blockers have yet to emerge; however, strong genetic evidence and data from non-selective Na channel blockers indicate that this target too may hold much promise.
LoGrasso
Philip
P
Avera Pharmaceuticals, 12730 High Bluff Drive, Suite 160, San Diego, CA 92130, USA.
McKelvy
Jeffrey
J
D000779:Anesthetics, Local / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D005998:Glycine / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D062558:NAV1.9 Voltage-Gated Sodium Channel; D009479:Neuropeptides / Q000037:antagonists & inhibitors / Q000378:metabolism; D010146:Pain / Q000188:drug therapy*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D026941:Sodium Channel Blockers / Q000627:therapeutic use*; D015222:Sodium Channels / Q000378:metabolism; D013779:Tetrodotoxin / Q000494:pharmacology
D000779:Anesthetics, Local; D062558:NAV1.9 Voltage-Gated Sodium Channel; C121001:NR2B NMDA receptor; D009479:Neuropeptides; D016194:Receptors, N-Methyl-D-Aspartate; C491886:SCN11A protein, human; D026941:Sodium Channel Blockers; D015222:Sodium Channels; D013779:Tetrodotoxin; D005998:Glycine