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.
Keywords: tetrodotoxin; TTX; TTX-sensitive voltage-gated sodium channels; pain; neuropathic pain
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Nieto, F.R.; Cobos, E.J.; Tejada, M.Á.; Sánchez-Fernández, C.; González-Cano, R.; Cendán, C.M. Tetrodotoxin (TTX) as a Therapeutic Agent for Pain. Mar. Drugs 2012, 10, 281-305.
Nieto FR, Cobos EJ, Tejada MÁ, Sánchez-Fernández C, González-Cano R, Cendán CM. Tetrodotoxin (TTX) as a Therapeutic Agent for Pain. Marine Drugs. 2012; 10(2):281-305.
Nieto, Francisco Rafael; Cobos, Enrique José; Tejada, Miguel Ángel; Sánchez-Fernández, Cristina; González-Cano, Rafael; Cendán, Cruz Miguel. 2012. "Tetrodotoxin (TTX) as a Therapeutic Agent for Pain." Mar. Drugs 10, no. 2: 281-305.