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
Current Topics in Medicinal Chemistry
Title: Kv7 Channels: Function, Pharmacology and Channel Modulators
Volume: 6 Issue: 10
Author(s): William Dalby-Brown, Henrik H. Hansen, Mads P.G. Korsgaard, Naheed Mirza and Soren-P Olesen
Affiliation:
Keywords: spike-frequency adaptation (SFA), BMS204352, Retigabine, atomic absorption assay, Epilepsy, Migraine, Pain
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.
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Dalby-Brown William, Hansen H. Henrik, Korsgaard P.G. Mads, Mirza Naheed and Olesen Soren-P, Kv7 Channels: Function, Pharmacology and Channel Modulators, Current Topics in Medicinal Chemistry 2006; 6 (10) . https://dx.doi.org/10.2174/156802606777323728
DOI https://dx.doi.org/10.2174/156802606777323728 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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