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Mar. Drugs 2015, 13(2), 984-995; doi:10.3390/md13020984

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

1
Department of Pharmacology, Faculty of Medicine, Saga University, Saga 849-8501, Japan
2
Laboratory of Biomedical Engineering, Graduate School of Biomedical Engineering, Tohoku University, Sendai 980-8575, Japan
3
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)
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Abstract

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
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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MDPI and ACS Style

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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