Structure, function and pharmacology of voltage-gated sodium channels

Citation
H. Denac et al., Structure, function and pharmacology of voltage-gated sodium channels, N-S ARCH PH, 362(6), 2000, pp. 453-479
Citations number
288
Categorie Soggetti
Pharmacology & Toxicology
Journal title
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
ISSN journal
00281298 → ACNP
Volume
362
Issue
6
Year of publication
2000
Pages
453 - 479
Database
ISI
SICI code
0028-1298(200012)362:6<453:SFAPOV>2.0.ZU;2-9
Abstract
Voltage-gated sodium channels (VGSCs) are responsible for the initial inwar ds current during the depolarisation phase of action potential in excitable cells. Therefore, VGSCs are crucial for cardiac and nerve function, since the action potential of nerves and muscle cannot occur without them. Their importance in generation and transmission of signals has been known for mor e than 40 years but the more recent introduction of new electrophysiologica l methods and application of molecular biology techniques has led to an exp losion of research on many different ion channels, including VGSCs. Their e xtraordinary biological importance makes them logical and obvious targets f or toxins produced by animals and plants for attack or defence. The action of these and similar substances modulating the function of the VGSCs is int eresting with respect to their possible use in medicine or use as tools in the study of these molecules. This review summarises recent progress in thi s research field and, in particular, considers what is known about the rela tionship of the structure to function, including a current understanding of the pharmacological modulation of VGSCs.