Quantitative structure-activity relationships of antiarrhythmic drugs.

A Comprehensive review of quantitative structure-activity relationship (QSAR) studies on antiarrhythmic agents is presented. From the discussion point of view, the antiarrhythmic agents have been put into two broad classes: specific and nonspecific. While the main members of the former class can be beta-adrenergic blocking agents (beta-blockers), any chemical that can act directly on the myocardial cell membrane, producing a cardiodepressant effect via changes in basic electrophysiological properties of the membrane, such as automaticity, excitability, conductivity, and refractoriness, has been put in the latter class. QSARs exhibit that the biological actions of a variety of drugs belonging to any class depend primarily on the lipophilic haracter of the molecule or substituents. Thus, the hydrophobic interaction is found to play a dominant role in the action of antiarrhythmic agents. In certain cases, the QSARs also exhibit the role of electronic parameters, suggesting that certain receptors may have electronic site also, permitting the drugs to involve in some electronic interactions, too.