4.7 Review

One man's side effect is another man's therapeutic opportunity: targeting Kv7 channels in smooth muscle disorders

Journal

BRITISH JOURNAL OF PHARMACOLOGY
Volume 168, Issue 1, Pages 19-27

Publisher

WILEY
DOI: 10.1111/j.1476-5381.2012.02133.x

Keywords

retigabine; KCNQ; Kv7 channels; smooth muscle; ion channels; voltage-gated potassium channels; hypertension

Funding

  1. Biotechnology and Biological Sciences Research Council [BB/G016321/1]
  2. British Heart Foundation [PG/09/104/28136] Funding Source: researchfish

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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.

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