Over the past 25 years, there have been significant contributions to the understanding of GIRK channel pharmacology and the modulation of channel properties by various drugs. Until recently, however, a majority of the drugs which were found to modulate GIRK channels were developed for other targets, and were therefore difficult to study in vivo. The recent studies, detailed here, employed both structure-based and structure-activity based screening methods for identifying GIRK channel-specific drugs and represent a significant advance.
