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J Med Chem. 2015 Sep 24;58(18):7093-118. doi: 10.1021/jm501981g. Epub 2015 May 14.

Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.

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Merck Research Laboratories , 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States.


The tremendous therapeutic potential of voltage-gated sodium channels (Na(v)s) has been the subject of many studies in the past and is of intense interest today. Na(v)1.7 channels in particular have received much attention recently because of strong genetic validation of their involvement in nociception. Here we summarize the current status of research in the Na(v) field and present the most relevant recent developments with respect to the molecular structure, general physiology, and pharmacology of distinct Na(v) channel subtypes. We discuss Na(v) channel ligands such as small molecules, toxins isolated from animal venoms, and the recently identified Na(v)1.7-selective antibody. Furthermore, we review eight characterized ligand binding sites on the Na(v) channel α subunit. Finally, we examine possible therapeutic applications of Na(v) ligands and provide an update on current clinical studies.

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