Classification of drugs based on properties of sodium channel inhibition: a comparative automated patch-clamp study.

ABSTRACT:

Background

There is only one established drug binding site on sodium channels. However, drug binding of sodium channels shows extreme promiscuity: ∼25% of investigated drugs have been found to potently inhibit sodium channels. The structural diversity of these molecules suggests that they may not share the binding site, and/or the mode of action. Our goal was to attempt classification of sodium channel inhibitors by measuring multiple properties of inhibition in electrophysiology experiments. We also aimed to investigate if different properties of inhibition correlate with specific chemical properties of the compounds.

Methodology/principal findings

A comparative electrophysiological study of 35 compounds, including classic sodium channel inhibitors (anticonvulsants, antiarr

SUBMITTER: Lenkey N 

PROVIDER: S-EPMC3004914 | biostudies-literature | 2010 Dec

REPOSITORIES: biostudies-literature