This book reviews the science of voltage-gated ion channel modulation as it pertains to the discovery of novel drugs. The book is divided into three general sections; these are 1.) Neuronal Voltage-Gated Ion Channel Functions, 2.) Modulatory Mechanisms and Influences on Voltage-Gated Ion Channel Activity and 3.) Drug Discovery Targets and Technology. The book features descriptions of the function assessments of neuronal voltage-gated ion channels, with an eye towards their applicability in drug discovery. Chapters explore the utility of ion channel targets for therapeutics in traditional and emerging drug targets, such as for pain and cardiovascular targets. Following chapters discussing biochemical and molecular mechanisims and pathways, other chapters cover advances in screening technologies, splicing techniques, and methods for regulating these ion channels.