Cationic Forms of Local Anaesthetics block Action Potentials from Inside the Nerve Membrane

Abstract

THERE is controversy as to whether the uncharged molecular form or the positively charged form of tertiary amine local anaesthetics is responsible for their nerve blocking action. Recent views favour the notion that the cationic form is active1,2. Little attention has, however, been paid to the site of action in the nerve fibre. The active form and the site of action of local anaesthetics can be determined by comparing the blocking potency of the anaesthetics as they are applied outside or inside the nerve membrane at different pH values. Such experiments have led us to conclude that the cationic forms of local anaesthetics block the excitability from inside the nerve membrane.

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NARAHASHI, T., YAMADA, M. & FRAZIER, D. Cationic Forms of Local Anaesthetics block Action Potentials from Inside the Nerve Membrane. Nature 223, 748–749 (1969). https://doi.org/10.1038/223748a0

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