Ion Channels as Drug Targets

Voltage-gated channels Potassium K+ Membrane potential 

The aim of this volume is to review, for the non-specialist, recent advances in the field of ion channel-related diseases. Six topics covering diseases such as cancer, cardiac arrhythmias, cystic fibrosis, and pain have been selected to reflect a number of different therapeutic areas, and each chapter is structured to cover the biological rational for the target, the current status in the development of novel agents to treat the disease, and the potential status of 

In order to fully appreciate the current advances in ion channel screening technologies, it is important to highlight some of the major discoveries that have directly or indirectly led to the current state in this field. The history of electrophysiology is rich and fascinating. It spans many different disciplines and fields (biology, physiology, biophysics, bioelectricity, etc.), extends over more than two centuries, and cannot be appropriately covered in this short review. Therefore, readers are referred to more comprehensive material on the subject matter [12-16]. 

However, the ionic currents measured using the voltage clamp technique were the result of fluxes through an ensemble of membrane channels. Until the 1970s, it had only been possible to study ion channels as macroscopic cur- 

Cell-attached patch, where the electrode remains sealed to the patch of membrane, allowing for the recording of currents through single ion channels in that patch of membrane 

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B. Progress in the pharmacological control of membrane transporters Voltage-Gated Ion Channels as Drug Targets... 

C. Potassium channels NON-SELECTIVE CATION CHANNELS AS DRUG TARGETS DIRECT LIGANDGATED ION CHANNELS (RECEPTORS WITH INTRINSIC ION CHANNEL)... 

Apart from very few exceptions, the entries in the main text do not contain drug names in their titles. Instead, drugs that are commonly used all over the world are listed in the Appendix. Also included in the Appendix are four-extensive sections that contain tables listing proteins such as receptors, transporters or ion channels, which are of particular interest as drug targets or modulators of drug action. 

Ion Channels As Targets For Drugs As major classes of pharmacological receptors ion channels are automatic loci for drug action. However, ion channels are particularly attractive targets for several additional reasons [ 4 ] ... 

With volumes on G-Protein-Coupled Receptors and Voltage-Gated Ion Channels we have started to edit volumes dedicated to important target classes. Here we introduce the third book following this concept. Eckhard Ottow and Hilmar Weinmann contribute a volume focusing on Nuclear Receptors as Drug Targets. 

A key concept is that ion channel-blocking drugs bind to specific sites on ion channel proteins to modify function (e.g., decrease current) and that the affinity of the ion channel protein for the drug on its target site varies as the ion channel protein shuttles among functional conformations (or ion... 

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