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Toxins 2012, 4(11), 1236-1260; doi:10.3390/toxins4111236

Conotoxins Targeting Neuronal Voltage-Gated Sodium Channel Subtypes: Potential Analgesics?

Health Innovations Research Institute, RMIT University, Melbourne, Victoria 3083, Australia
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Received: 10 October 2012 / Revised: 5 November 2012 / Accepted: 5 November 2012 / Published: 8 November 2012
(This article belongs to the Special Issue Animal Toxins Targeting Ion Channels Involved in Pain)
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Abstract

Voltage-gated sodium channels (VGSC) are the primary mediators of electrical signal amplification and propagation in excitable cells. VGSC subtypes are diverse, with different biophysical and pharmacological properties, and varied tissue distribution. Altered VGSC expression and/or increased VGSC activity in sensory neurons is characteristic of inflammatory and neuropathic pain states. Therefore, VGSC modulators could be used in prospective analgesic compounds. VGSCs have specific binding sites for four conotoxin families: μ-, μO-, δ- and ί-conotoxins. Various studies have identified that the binding site of these peptide toxins is restricted to well-defined areas or domains. To date, only the μ- and μO-family exhibit analgesic properties in animal pain models. This review will focus on conotoxins from the μ- and μO-families that act on neuronal VGSCs. Examples of how these conotoxins target various pharmacologically important neuronal ion channels, as well as potential problems with the development of drugs from conotoxins, will be discussed.
Keywords: voltage-gated sodium channel; Nav1.3; Nav1.7; Nav1.8; Nav1.9; m-conotoxin; mO-conotoxin; nociception; analgesic; pain voltage-gated sodium channel; Nav1.3; Nav1.7; Nav1.8; Nav1.9; m-conotoxin; mO-conotoxin; nociception; analgesic; pain
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Knapp, O.; McArthur, J.R.; Adams, D.J. Conotoxins Targeting Neuronal Voltage-Gated Sodium Channel Subtypes: Potential Analgesics? Toxins 2012, 4, 1236-1260.

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