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Mar. Drugs 2015, 13(2), 984-995;

Selective Blocking Effects of 4,9-Anhydrotetrodotoxin, Purified from a Crude Mixture of Tetrodotoxin Analogues, on NaV1.6 Channels and Its Chemical Aspects

Department of Pharmacology, Faculty of Medicine, Saga University, Saga 849-8501, Japan
Laboratory of Biomedical Engineering, Graduate School of Biomedical Engineering, Tohoku University, Sendai 980-8575, Japan
Laboratory of Bioorganic Chemistry of Natural Products, Graduate School of Agricultural Science, Tohoku University, Sendai 981-8555, Japan
Author to whom correspondence should be addressed.
Academic Editor: Vítor Vasconcelos
Received: 24 December 2014 / Revised: 30 January 2015 / Accepted: 3 February 2015 / Published: 12 February 2015
(This article belongs to the Special Issue Emerging Marine Toxins)
PDF [518 KB, uploaded 24 February 2015]


Tetrodotoxin (TTX) is a potent neurotoxin found in a number of marine creatures including the pufferfish, where it is synthesized by bacteria and accumulated through the food chain. It is a potent and selective blocker of some types of voltage-gated Na+ channel (NaV channel). 4,9-Anhydrotetrodotoxin (4,9-anhydroTTX) was purified from a crude mixture of TTX analogues (such as TTX, 4-epiTTX, 6-epiTTX, 11-oxoTTX and 11-deoxyTTX) by the use of liquid chromatography-fluorescence detection (LC-FLD) techniques. Recently, it has been reported that 4,9-anhydroTTX selectively blocks the activity of NaV1.6 channels with a blocking efficacy 40–160 times higher than that for other TTX-sensitive NaV1.x channel isoforms. However, little attention has been paid to the molecular properties of the α-subunit in NaV1.6 channels and the characteristics of binding of 4,9-anhydroTTX. From a functional point of view, it is important to determine the relative expression of NaV1.6 channels in a wide variety of tissues. The aim of this review is to discuss briefly current knowledge about the pharmacology of 4,9-anhydroTTX, and provide an analysis of the molecular structure of native NaV1.6 channels. In addition, chemical aspects of 4,9-anhydroTTX are briefly covered. View Full-Text
Keywords: 4,9-anhydrotetrodotoxin; LC-FLD techniques; NaV1.6 channels; tetrodotoxin 4,9-anhydrotetrodotoxin; LC-FLD techniques; NaV1.6 channels; tetrodotoxin

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Teramoto, N.; Yotsu-Yamashita, M. Selective Blocking Effects of 4,9-Anhydrotetrodotoxin, Purified from a Crude Mixture of Tetrodotoxin Analogues, on NaV1.6 Channels and Its Chemical Aspects. Mar. Drugs 2015, 13, 984-995.

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