ABSTRACT
Ion channels represent the second largest class among 435 proven eect-mediating drug targets after G-protein-coupled receptors (GPCRs) (Rask-Andersen et al., 2011). ey are primary targets for therapeutic areas of neuropsychiatric disorders (such as pain, epilepsy, stroke, Alzheimer’s disease, anxiety, schizophrenia, etc.), cardiovascular and metabolic diseases (such as hypertension, arrhythmias, and diabetes), immunodiseases (such as asthma), nephrology (such as urinary retention and incontinence), irritable bowel syndrome, and pulmonary/respiratory diseases (such as chronic obstructive pulmonary airway disease). From 1939 to 2012, US Food and Drug Administration (FDA) approved a total of 2265 small molecule drugs (including the same molecular entity in dierent formulation) for all therapeutic areas. Among these approved drugs, there are about 730 drugs (more than one-third of the total) that have been classied as ion channeltargeting drugs although the exact mechanisms for most of them are not dened or unknown, in particular for drugs that were approved before the year of 2000. is chapter summarizes some
of the representative drugs whose mechanisms of action are better studied or known. e description is organized based on target subclasses.
