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Distinct mechanisms of inhibition of Kv2 potassium channels by tetraethylammonium and RY785.


ABSTRACT: Voltage-gated K+ channels play central roles in human physiology, both in health and disease. A repertoire of inhibitors that are both potent and specific would therefore be of great value, not only as pharmacological agents but also as research tools. The small molecule RY785 has been described as particularly promising in this regard, as it selectively inhibits channels in the Kv2 subfamily with high potency. Kv2 channels are expressed in multiple cell types in humans, and are of particular importance for neuronal function. The mechanism of action of RY785 has not yet been determined at the molecular level, but functional studies indicate it differs from that of less specific inhibitors, such as quaternary-ammonium compounds or aminopyridines; RY785 is distinct also in that it

SUBMITTER: Zhang S 

PROVIDER: S-EPMC11451595 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature