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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Kv7 Channels: Function, Pharmacology and Channel Modulators

Author(s): William Dalby-Brown, Henrik H. Hansen, Mads P.G. Korsgaard, Naheed Mirza and Soren-P Olesen

Volume 6, Issue 10, 2006

Page: [999 - 1023] Pages: 25

DOI: 10.2174/156802606777323728

Price: $65

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


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