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Ion channels are located within the plasma membrane of nearly all cells and many intracellular organelles. These enigmatic proteins play a critical role in numerous fundamental physiological functions including generating and shaping action potentials, regulating cell volume and controlling epithelial secretion to name but a few. Ion channel modulators have historically proven their major therapeutic utility in numerous clinical paradigms including reduction of blood pressure, analgesia and local anaesthesia—however their potential as targets for novel and efficacious therapeutics is yet to be fully realized. The recent focus on the human genome has attributed an increasing number of diseases to genetic ion channel dysfunction (channelopathies). This emphasizes not only the important physiological and pathophysiological roles these proteins play but directs the drug discoverer to not only new targets but a clear understanding of potentially how they should be modulated.

Advances in our understanding of ion channel function combined with enabling technologies, such as automated electrophysiology, has fuelled interest and investment in ion channel modulation in both industrial and academic settings. The coming years promise to be exciting times as these new therapeutic opportunities are identified and realized.

This book builds on the platform created by the highly successful series of Royal Society of Chemistry ‘Ion Channels as Therapeutic Targets’ meetings in the last decade. These meetings, supported by both academic and industrial scientists, have covered themes including advances in screening technology, ion channel structure and modeling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels.

Our goal was to provide a reference text of interest to a wide range of readers by eliciting contributions from highly respected academic and industrial researchers covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as an introduction to the new ‘ion channel drug discoverer’. We thank the many contributors to this book and hope you enjoy reading it as much as we did editing it.

Brian Cox and Martin Gosling

Horsham, UK

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