Abstract

Kv7 channels are unique among K+ channels, since four out of the five channel subtypes have well-documented roles in the development of human diseases. They have distinct physiological functions in the heart and in the nervous system, which can be ascribed to their voltage-gating properties. The Kv7 channels also lend themselves to pharmacological modulation, and synthetic openers as well as blockers of the channels, regulating neuronal excitability, have existed even before the Kv7 channels were identified by cloning. In the present review we give an account on the focused efforts to develop selective modulators, openers as well as blockers, of the Kv7 channel subtypes, which have been undertaken during recent years, along with a discussion of the Kv7 ion channel physiology and therapeutic indications for modulators of the neuronal Kv7 channels.

Keywords: spike-frequency adaptation (SFA), BMS204352, Retigabine, atomic absorption assay, Epilepsy, Migraine, Pain