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• Nieto, F
• Cobos, E
• Tejada, M
• Sánchez-Fernández, C
• González-Cano, R
• Cendán, C
• [+] on Google Scholar
• Nieto, F
• Cobos, E
• Tejada, M
• Sánchez-Fernández, C
• González-Cano, R
• Cendán, C
• [+] on PubMed
• Nieto, F
• Cobos, E
• Tejada, M
• Sánchez-Fernández, C
• González-Cano, R
• Cendán, C

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Mar. Drugs 2012, 10(2), 281-305; doi:10.3390/md10020281

Review

Tetrodotoxin (TTX) as a Therapeutic Agent for Pain

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 (Avenida de Madrid 11, 18012 Granada, Spain) and Biomedical Research Center, University of Granada, Parque Tecnológico de Ciencias de la Salud, 18100 Armilla, Granada, Spain

* Authors to whom correspondence should be addressed.

Received: 30 December 2011; in revised form: 19 January 2012 / Accepted: 19 January 2012 / Published: 31 January 2012

(This article belongs to the Special Issue Tetrodotoxin)

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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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