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

2008/04/14 by Jens A. Lundbæk · 18 citations
Biochemistry, Genetics and Molecular Biology · Neuroscience · #Lipid Membrane Structure and Behavior #Ion channel regulation and function #Neuroscience and Neuropharmacology Research

paper · pdf · doi:10.1085/jgp.200709948

Abstract

d a d l n e t . d k Drugs that at pico-to nanomolar concentration regulate ion channel function by high-affi nity 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 nonspecifi c manner. It has long been suspected that this promiscuous regulation of membrane protein function could be due to changes in the physical properties of the host lipid bilayer, but the underlying mechanisms have been poorly understood.

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