Internationally recognized biomedical scientists describe recent technological breakthroughs and demonstrate their use in successful experimental designs. The diverse applications range from the study of allosteric regulation of ion channel activity using a classic mutagenesis approach, to the study of channel subunit stoichiometry using a novel biophysical approach based on fluorescence resonance energy transfer. Highlights include methods for heterologous expression of ion channels in cells, for determining channel structure-function, for studying channel regulation and physiological function, and for genetic screening and investigating channelopathies.