The G-protein activated, inward-rectifying potassium (K+) channels, "GIRKs", are a family of ion channels that has been the focus of intense research interest for nearly two decades. GIRK has been shown to play important roles in the pathophysiology of diseases such as anxiety, epilepsy, Down's syndrome, pain perception and drug addiction. Here scientists at Vanderbilt developed the first truly potent, effective, and selective GIRK activator, ML297 (VU0456810) and demonstrated that ML297 is active in animal models of epilepsy. While the group is using ML297 to continue to explore the therapeutic benefits of GIRK modulation, they are continuing to develop more selective and druggable GIRK inhibitors from different scaffolds.
