Voltage-gated potassium Kv2.1 and Kv2.2 channels are highly expressed in pancreatic islets. Pancreatic β-cells from Kv2.1−/− mice display greater glucose-stimulated insulin secretion. Likewise, pharmacologic inhibition of Kv2.x channels enhances glucose stimulated insulin secretion from isolated wild-type mice and human islets but not in islets from Kv2.1−/− mice. These results suggest that inhibition of Kv2.1 may promote improved glucose tolerance. However, when Kv2.x inhibitors were administered in vivo, improved glucose tolerance was not observed, possibly because of the inhibition of Kv2.2. Therefore, the development of selective Kv2.1 inhibitors may provide new avenues to promote glucose-stimulated insulin secretion for the treatment of type 2 diabetes.
See article at J Pharmacol Exp Ther 2013, 344:407–416.
- Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics