Naunyn-Schmiedeberg's archives of pharmacology
-
Naunyn Schmiedebergs Arch. Pharmacol. · May 1982
Hydrophobic membrane interaction of etidocaine, bupivacaine and 2-chloroprocaine. A spin and fluorescent probe study.
It has been suggested that local anesthetics may block sodium conductance through nervous membranes also by hydrophobic interaction, e.g., by expanding the membrane. Decreased anisotropy (fluidization) and depressed phase transition temperatures have been shown by relatively high local anesthetic concentrations. We studied the dose dependence of the effect of three clinically used local anesthetics, with different lipid solubility, on lipid fluidity parameters of four different model membranes. ⋯ The effect was most marked with bupivacaine (1-10 mM) when cis-parinaric acid was used. While isolated mammalian nerves are blocked by local anesthetic concentrations below 100 muM, this study shows that the clinically used local anesthetics increase fluidity and depress phase transition temperature only at 10-100 times higher concentrations at physiological pH. This kind of hydrophobic membrane interaction may not be important for the nerve blocking effect.