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Mar. Drugs 2018, 16(2), 72; https://doi.org/10.3390/md16020072

Tetrodotoxin, a Candidate Drug for Nav1.1-Induced Mechanical Pain?

UMR CNRS 6015, INSERM U1083, Mitovasc Institute, Angers University, 49055 Angers, France
Received: 4 January 2018 / Revised: 9 February 2018 / Accepted: 20 February 2018 / Published: 22 February 2018
(This article belongs to the Special Issue Tetrodotoxin)
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Abstract

Tetrodotoxin (TTX), the mode of action of which has been known since the 1960s, is widely used in pharmacology as a specific inhibitor of voltage-gated sodium channels (Nav channels). This toxin has contributed to the characterization of the allosteric model of the Nav channel, and to discriminating TTX-sensitive and TTX-resistant subtypes. In addition to its role as a pharmacological tool, TTX is now considered a therapeutic molecule, and its development should lead to its use in certain pathologies involving Nav channels, particularly in the field of pain. Specifically, the blockade of Nav channels expressed in nociceptive fibres is one strategy for alleviating pain and its deleterious consequences on health. Recent work has identified, in addition to the Nav1.7, 1.8 and 1.9 channels, the Nav1.1 subtype on dorsal root ganglion (DRG) neurons as a crucial player in mechanical and non-thermal pain. The sensitivity of Nav1.1 to TTX could be exploited at the therapeutic level, especially in chronic pain conditions. View Full-Text
Keywords: tetrodotoxin; Nav channels; Nav1.1; mechanical pain; nociceptor tetrodotoxin; Nav channels; Nav1.1; mechanical pain; nociceptor
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Mattei, C. Tetrodotoxin, a Candidate Drug for Nav1.1-Induced Mechanical Pain? Mar. Drugs 2018, 16, 72.

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