tetrodotoxin (ttx) as a therapeutic agent for pain河豚毒素(ttx)作为治疗疼痛.pdf

Mar. Drugs 2012, 10, 281-305; doi:10.3390/m OPEN ACCESS Marine Drugs ISSN 1660-3397 /journal/marinedrugs 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; E-Mails: ejcobos@ugr.es (E.J.C.); mtejada@ugr.es (M.Á.T); csanchezf@ugr.es (C.S.-F.); rgcano@ugr.es (R.G.-C.) * Authors to whom correspondence should be addressed; E-Mails: fnieto@ugr.es (F.R.N.); cmcendan@ugr.es (C.M.C.); Tel.: +34-958-243538 (F.R.N.); Fax: +34-958-243537 (F.R.N.). Received: 30 December 2011; in revised form: 19 January 2012 / Accepted: 19 January 2012 / Published: 31 January 2012 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 pa