Recent advances in electrophysiology-based screening technology and the impact upon ion channel discovery research.

Ion channels are recognised as an increasingly tractable class of targets for the discovery and development of new drugs, with a diverse range of ion channel proteins now implicated across a wide variety of disease states and potential therapeutic applications. Whilst the field now ranks as one of the most dynamic fields for drug discovery research, it has historically been regarded by many researchers as a class of proteins associated with numerous technical challenges. Recent advances in our understanding of molecular biology and the increasing acceptance of electrophysiology-based screening methodology mean that ion channels are rapidly progressing towards universal acceptance as worthy and approachable targets for drug discovery. This chapter will outline the commercially available electrophysiology-based screening technologies and give an overview of the range of options for progressing pharmaceutical research and development against this important target class.

Strategies to identify ion channel modulators: current and novel approaches to target neuropathic pain.

Modulation of ion channel function has been a successful area for drug development, with ion channel modulating drugs being used in the therapeutic treatment of epilepsy, hypertension, diabetes and chronic pain. Most of the ion channel-modulating drugs that are currently on the market were developed without extensive knowledge of the molecular structure of ion channels, or an understanding of the full complexity of ion channel subtypes or knowledge of how ion channel expression is regulated during pathology. As new information on the roles that different ion channel subtypes play in pathophysiological processes becomes available, drugs will be designed to target specific ion channel subtypes via mechanisms that involve either direct channel block or modulation of ion channel functional expression. Using neuropathic pain as an example, this article reviews current knowledge of the structure and function of ion channels and current technology and future opportunities for the identification of novel drugs that are capable of modulating ion channel function.