Lipid Bilayer–mediated Regulation of Ion Channel Function by Amphiphilic Drugs

• Published in: The Journal of general physiology Vol. 131; no. 5; pp. 421 - 429
• Main Author: Lundbaek, Jens A
• Format: Journal Article
• Language: English
• Published: United States Rockefeller University Press 01.05.2008; The Rockefeller University Press
• Subjects: Animals; Biomarkers, Pharmacological; Biomechanical Phenomena; Cell Membrane - chemistry; Cell Membrane - drug effects; Cellular biology; Dose-Response Relationship, Drug; Drug therapy; Energy Transfer - drug effects; Gramicidin - chemistry; Humans; Hydrophobic and Hydrophilic Interactions; Ion Channels - chemistry; Ion Channels - drug effects; Ions; Lipid Bilayers - chemistry; Lipids; Membranes; Pharmaceutical Preparations - chemistry; Pharmacology; Proteins; Surface-Active Agents - chemistry; Surface-Active Agents - pharmacology

Drugs that at pico- to nanomolar concentration regulate ion channel function by high-affinity binding to their cognate receptor often have a "secondary pharmacology," in which the same molecule at low micromolar concentrations regulates a diversity of membrane proteins in an apparently non...