The Journal of General Physiology
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The Journal of General Physiology, Vol 77, 137-153, Copyright © 1981 by The Rockefeller University Press

ARTICLES

Local anesthetics QX 572 and benzocaine act at separate sites on the batrachotoxin-activated sodium channel

LM Huang and G Ehrenstein

We have studied the effect of local anesthetics QX 572, which is permanently charged, and benzocaine, which is neutral, on batrachotoxin- activated sodium channels in mouse neuroblastoma N18 cells. The dose- response curves for each drug suggest that QX 752 and benzocaine each act on a single class of binding sites. The dissociation constants are 3.15 X 10(-5) M for QX 572 and 2.65 X 10(-4) M for benzocaine. Equilibrium and kinetic experiments indicate that both drugs are competitive inhibitors of batrachotoxin. When benzocaine and QX 572 are present with batrachotoxin, they are much more effective at inhibiting Na+ flux than would be predicted by a one-site model. Our results indicate that QX 572 and benzocaine bind to separate sites, each of which interacts competitively with batrachotoxin.
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G Ehrenstein and L. Huang
Side-effect reduction by use of drugs that bind to separate but equivalent binding sites
Science, December 18, 1981; 214(4527): 1365 - 1366.
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