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Molecular Pharmacology, Vol 9, 360-371, Copyright © 1973 by the American Society for Pharmacology and Experimental Therapeutics

On the Molecular Action of Local Anesthetics

I. The Mitochondrion as a Model Membrane System for Studying Local Anesthetic Action

CARL L. JOHNSON 1, MARGARET A. GOLDSTEIN 1, and ARNOD SCHWARTZ 1

1 Department of Cell Biophysics, Division of Myocardial Biology, Baylor College of Medicine, and Fondren-Brown Cardiovascular Research and Training Center, Methodist Hospital, Houston, Texas 77025

Local anesthetics inhibit valinomycin-induced potassium uptake and basic protein-induced swelling of liver mitochondria. The present results suggest that a common feature of these effects of the local anesthetics on mitochondria is a stabilization of membrane structure. In view of the proposed role of protein conformational changes in nerve impulse conduction, the results suggest that the molecular mechanism of local anesthesia may involve an inhibition of membrane conformational changes rather than a direct inhibition of transport of monovalent or divalent cations, as generally believed. A correlation exists between the activity of these drugs on mitochondria and their activity on nerve conduction blockade. The mitochondrion may therefore serve as a useful model system to study local anesthetic action at the molecular level. Structure-activity studies indicate that the major determinant of potency of these anesthetics on mitochondria is the lipid solubility of the drug.

Note:
ACKNOWLEDGMENT We extend our appreciation to Dr. Jeanie M. Wood for carrying out several experiments and critically reviewing the manuscript.

Submitted on December 19, 1972




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