Effects of lidocaine on transport properties of renal brush-border membranes.
The effect of lidocaine was examined in membrane vesicles from rabbit renal brush borders. Changes in the ionic permeability and the kinetics of Na+-dependent metabolite transport were observed at different concentrations of anesthetic. Lidocaine was found to alter the membrane permeability of all inorganic cations examined (Li+, Rb+, K+, and Na+). At low lidocaine concentrations, there was a saturable decrease in permeability, whereas at higher concentrations (greater than 0.2 mM) there was a non-saturable general increase in cation permeability. Lidocaine (1.0 mM) inhibited Na+-coupled transport of all ten substrates examined (sugars, amino acids and Krebs cycle intermediates). The affinity for the substrate decreased in the presence of the anesthetic.
D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002463:Cell Membrane Permeability / Q000187:drug effects; D007687:Kidney Tubules, Proximal / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D008012:Lidocaine / Q000494:pharmacology*; D008871:Microvilli / Q000187:drug effects* / Q000378:metabolism; D011817:Rabbits; D012964:Sodium / Q000378:metabolism
D008012:Lidocaine; D012964:Sodium