Beta-Adrenolytic- and local anesthetic-induced potentials in artificial lipid membranes.

Abstract

Local anesthetics and β-adrenoceptor blocking agents have been tested on artificial membranes of different lipid composition. These drugs, upon interaction with such membranes, produce significant potentials, the side to which the drug was added being negative. By changing the membrane lipid composition and concentration, the electrolyte concentration of the membrane bathing solution and its pH the following results for propranolol could be obtained: Dose response curves show clear differences in the intensity of action for the various β-adrenoceptor blocking agents and local anesthetics. The following sequence, related to bupranolol = 1 has been determined: bupranolol 1, alprenolol 0.96, propranolol 0.91, inpea 0.42, sotalol 0.35, practolol 0.29 and cinchocaine 0.91, tetracaine 0.87, lidocaine 0.50, procaine 0.37. This sequence corresponds to that found in biological tissues, i.e. β-blocking activity in atria and local anesthetic potency in axons.