pH-dependent effects of local anaesthetics in perturbing lipid membranes

Gen Physiol Biophys. 1987 Jun;6(3):271-7.

Abstract

The effects of local anaesthetics lidocaine, benzocaine, carbisocaine and carbisocaine derivatives, KaQ-7 and Ka-O, in perturbing bovine brain lipid membranes or egg lecithin membranes were compared at pH 6.0; 7.0; and 8.0. The electron spin resonance method with stearic acid labeled at carbon position 16 as the spin probe was employed. The perturbation effects of lidocaine and Ka-O were found to increase with increasing pH of the sample, whereas the effect of carbisocaine decreased with increasing pH. The perturbation effects of benzocaine and KaQ-7 were independent of pH. The pH-dependent perturbation effects of the local anaesthetics tested on lipid membrane fairly corresponded with their pH-dependent potency to block nerve action potentials.

MeSH terms

  • Anesthetics, Local / pharmacology*
  • Animals
  • Benzocaine / pharmacology
  • Brain / metabolism
  • Carbamates / pharmacology
  • Cattle
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Lidocaine / pharmacology
  • Membrane Lipids / metabolism*
  • Phosphatidylcholines / metabolism

Substances

  • Anesthetics, Local
  • Carbamates
  • Membrane Lipids
  • Phosphatidylcholines
  • carbizocaine
  • Lidocaine
  • Benzocaine