Abstract
Retigabine is a first in class anticonvulsant that has recently undergone clinical trials to test its efficacy in epileptic patients. Retigabine's novel mechanism of action - activating Kv7 channels - suppresses neuronal activity to prevent seizure generation by hyperpolarizing the membrane potential and suppressing depolarizing surges. However, Kv7 channels are not expressed exclusively in neurones and data generated over the last decade have shown that Kv7 channels play a key role in various smooth muscle systems of the body. This review discusses the potential of targeting Kv7 channels in the smooth muscle to treat diseases such as hypertension, bladder instability, constipation and preterm labour.
© 2012 The Authors. British Journal of Pharmacology © 2012 The British Pharmacological Society.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Anticonvulsants / pharmacology
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Carbamates / pharmacology*
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Constipation / drug therapy
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Female
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Humans
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Hypertension / drug therapy
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KCNQ1 Potassium Channel / drug effects*
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KCNQ1 Potassium Channel / metabolism*
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Membrane Potentials / drug effects
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Membrane Transport Modulators / pharmacology
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Muscle Tonus / drug effects
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Muscle, Smooth / drug effects*
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Muscle, Smooth / metabolism
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Muscle, Smooth, Vascular / drug effects
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Muscle, Smooth, Vascular / metabolism
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Muscular Diseases / drug therapy*
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Muscular Diseases / metabolism
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Neurons / drug effects
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Obstetric Labor, Premature / drug therapy
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Phenylenediamines / pharmacology*
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Potassium Channels, Voltage-Gated / drug effects*
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Potassium Channels, Voltage-Gated / metabolism*
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Pregnancy
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Urinary Bladder Diseases / drug therapy
Substances
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Anticonvulsants
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Carbamates
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KCNQ1 Potassium Channel
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KCNQ1 protein, human
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Membrane Transport Modulators
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Phenylenediamines
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Potassium Channels, Voltage-Gated
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ezogabine