Ion channel modulators: new targets and new indications for old targets.
Over recent years, our ever-increasing knowledge of the physiological roles of specific ion channel subtypes has led to drug discovery efforts aimed at ion channels of unknown pharmacology. Two of these are the transient receptor potential (TRP) channel TRPV1 and the acid-sensing ion channel (ASIC) family. Drug discovery efforts focused on both of these targets have led to interesting outcomes related to species differences in the mechanism of action of TRPV1 blockers and tissue differences in the physiological roles of the different ASIC subtypes. In addition to the pursuit of novel targets, recent evidence suggests that there are new indications for known channel subtypes and modulators, including pain management for sodium and T-type calcium channel blockers and urinary incontinence for K(ATP) openers.
Priest
Birgit
B
Department of Ion Channels, Merck Research Laboratories, Mail Code 80N-C31, PO Box 2000, Rahway, NJ 07065, USA.
Kaczorowski
Gregory J
GJ
Garcia
Maria L
ML
D062565:Acid Sensing Ion Channels; D000818:Animals; D016503:Drug Delivery Systems; D006801:Humans; D007473:Ion Channels / Q000187:drug effects*; D008565:Membrane Proteins / Q000187:drug effects / Q000502:physiology; D009419:Nerve Tissue Proteins / Q000187:drug effects / Q000502:physiology; D026941:Sodium Channel Blockers / Q000494:pharmacology; D015222:Sodium Channels / Q000187:drug effects / Q000502:physiology; D050052:TRPC Cation Channels / Q000187:drug effects / Q000502:physiology; D050916:TRPV Cation Channels / Q000187:drug effects / Q000502:physiology
D062565:Acid Sensing Ion Channels; D007473:Ion Channels; D008565:Membrane Proteins; D009419:Nerve Tissue Proteins; D026941:Sodium Channel Blockers; D015222:Sodium Channels; D050052:TRPC Cation Channels; D050916:TRPV Cation Channels; C494482:TRPV1 protein, human