The pharmacology of voltage-gated sodium channel activators

Deuis, Jennifer R., Mueller, Alexander, Israel, Mathilde R. and Vetter, Irina (2017) The pharmacology of voltage-gated sodium channel activators. Neuropharmacology, 127 87-108. doi:10.1016/j.neuropharm.2017.04.014

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Author Deuis, Jennifer R.
Mueller, Alexander
Israel, Mathilde R.
Vetter, Irina
Title The pharmacology of voltage-gated sodium channel activators
Journal name Neuropharmacology   Check publisher's open access policy
ISSN 1873-7064
0028-3908
Publication date 2017-04-14
Sub-type Article (original research)
DOI 10.1016/j.neuropharm.2017.04.014
Open Access Status File (Author Post-print)
Volume 127
Start page 87
End page 108
Total pages 22
Place of publication Kidlington, Oxford, United Kingdom
Publisher Pergamon Press
Language eng
Subject 3004 Pharmacology
2804 Cellular and Molecular Neuroscience
Abstract Toxins and venom components that target voltage-gated sodium (Na) channels have evolved numerous times due to the importance of this class of ion channels in the normal physiological function of peripheral and central neurons as well as cardiac and skeletal muscle. Na channel activators in particular have been isolated from the venom of spiders, wasps, snakes, scorpions, cone snails and sea anemone and are also produced by plants, bacteria and algae. These compounds have provided key insight into the molecular structure, function and pathophysiological roles of Na channels and are important tools due to their at times exquisite subtype-selectivity. We review the pharmacology of Na channel activators with particular emphasis on mammalian isoforms and discuss putative applications for these compounds. This article is part of the Special Issue entitled ‘Venom-derived Peptides as Pharmacological Tools.’
Formatted abstract
Toxins and venom components that target voltage-gated sodium (NaV) channels have evolved numerous times due to the importance of this class of ion channels in the normal physiological function of peripheral and central neurons as well as cardiac and skeletal muscle. NaV channel activators in particular have been isolated from the venom of spiders, wasps, snakes, scorpions, cone snails and sea anemone and are also produced by plants, bacteria and algae. These compounds have provided key insight into the molecular structure, function and pathophysiological roles of NaV channels and are important tools due to their at times exquisite subtype-selectivity. We review the pharmacology of NaV channel activators with particular emphasis on mammalian isoforms and discuss putative applications for these compounds.
Keyword Activator
Pharmacology
Toxin
Voltage sensor
Voltage-gated sodium channel
Q-Index Code C1
Q-Index Status Provisional Code
Grant ID FT130101215
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: HERDC Pre-Audit
School of Pharmacy Publications
Institute for Molecular Bioscience - Publications
 
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