R160 g012



Keywords: r160 g012
Description: K V channels are voltage-gated potassium channels that open in response to membrane depolarization thus serving as key elements after cell repolarization. K V channels regulate numerous

KV channels are voltage-gated potassium channels that open in response to membrane depolarization thus serving as key elements after cell repolarization. KV channels regulate numerous physiological processes. KV 2 channels are widely expressed in the CNS, pancreas and smooth muscle.

RY796 is a synthetic blocker of the KV 2.1 and KV 2.2 channels. It has an effective concentration of 0.1-10 µM and an IC50 of 0.09 µM and 0.25 µM for the KV 2.1 and KV 2.2 channels respectively. RY796 has greater selectivity for KV 2 channels over other KV channels out of 1894 compounds in a study conducted by Herrington, J. et al. In addition, RY796 does not affect other ion channels such as sodium and calcium.

RY796 blocks the KV channel in a use and dose dependent manner 1. In an experiment examining the role of KV channels in the regulation of insulin and somatostatin release from pancreatic islets, RY796 caused an increase of GSIS (glucose stimulated insulin secretion) in vitro however not producing the same effect in live mice. RY796 was also found to increase glucose stimulated somatostatin release from pancreatic δ-cells 2 .






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