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.