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Tetrodotoxin (TTX) as a therapeutic agent for pain.

Abstract
Tetrodotoxin (TTX) is a potent neurotoxin that blocks voltage-gated sodium channels (VGSCs). VGSCs play a critical role in neuronal function under both physiological and pathological conditions. TTX has been extensively used to functionally characterize VGSCs, which can be classified as TTX-sensitive or TTX-resistant channels according to their sensitivity to this toxin. Alterations in the expression and/or function of some specific TTX-sensitive VGSCs have been implicated in a number of chronic pain conditions. The administration of TTX at doses below those that interfere with the generation and conduction of action potentials in normal (non-injured) nerves has been used in humans and experimental animals under different pain conditions. These data indicate a role for TTX as a potential therapeutic agent for pain. This review focuses on the preclinical and clinical evidence supporting a potential analgesic role for TTX. In addition, the contribution of specific TTX-sensitive VGSCs to pain is reviewed.
AuthorsFrancisco Rafael Nieto, Enrique José Cobos, Miguel Ángel Tejada, Cristina Sánchez-Fernández, Rafael González-Cano, Cruz Miguel Cendán
JournalMarine drugs (Mar Drugs) Vol. 10 Issue 2 Pg. 281-305 (Feb 2012) ISSN: 1660-3397 [Electronic] Switzerland
PMID22412801 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • Analgesics, Non-Narcotic
  • Nerve Tissue Proteins
  • Neurotoxins
  • Protein Isoforms
  • Sodium Channel Blockers
  • Sodium Channels
  • Tetrodotoxin
Topics
  • Acute Pain (drug therapy, immunology, metabolism)
  • Analgesics, Non-Narcotic (therapeutic use)
  • Animals
  • Humans
  • Nerve Tissue Proteins (antagonists & inhibitors, chemistry, genetics, metabolism)
  • Neuralgia (drug therapy, immunology, metabolism)
  • Neurons (drug effects, metabolism)
  • Neurotoxins (therapeutic use)
  • Protein Isoforms (antagonists & inhibitors, chemistry, genetics, metabolism)
  • Sodium Channel Blockers (therapeutic use)
  • Sodium Channels (chemistry, genetics, metabolism)
  • Tetrodotoxin (therapeutic use)

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