• Francisco Rafael Nieto, Enrique José Cobos, Miguel Ángel Tejada, Cristina Sánchez-Fernández, Rafael González-Cano, and Cruz Miguel Cendán.
• Department of Pharmacology and Institute of Neuroscience, Faculty of Medicine, University of Granada, Granada, Spain. fnieto@ugr.es
• Mar Drugs. 2012 Feb 1;10(2):281-305.

AbstractTetrodotoxin (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.

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