Abstract

AbstractThe isolation and characterization of cloned Na channels have given new insights into structure‐function relationships. In particular, recent mutational analyses of the tetrodotoxin binding site and the inactivation gate have begun to clarify the structural basis for the phenomena of drug block at the extracellular mouth of the ion‐conducting pore, and regulation of ion conductance by gating at the intracellular mouth. However, much more work remains to be done, particularly in regard to the receptors for the inactivation gate and for the local anesthetic class of drugs. This paper reviews the background, and some of the recent advances and future direction in Na channel structure‐function studies. © 1994 Wiley‐Liss, Inc.

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