학술논문

Effects of calcium on the local anesthetic suppression of ionic conductances in squid axon membranes.
Document Type
Article
Source
The Journal of Pharmacology and Experimental Therapeutics; May 1976, Vol. 197 Issue: 2 p426-438, 13p
Subject
Language
ISSN
00223565; 15210103
Abstract
The effects of varying the external calcium concentration on the suppression of membrane ionic conductances by procaine and benzocaine have been examined under voltage-clamped conditions. The suppression of peak conductance and steady-state conductance by procaine or benzocaine applied externally or internally was not affected by changing the external calcium concentration between 10 and 100 mM. When the calcium concentration was lowered below 10 mM (5 or 2 mM), the procaine effect was slightly potentiated. This augmentation could not be ascribed to an acceleration in the rate of penetration of procaine into the axon in low calcium solutions. The resting membrane conductance was slightly decreased by procaine in a manner independent of the external calcium concentration. The maximum effect of procaine on resting conductances was obtained at a concentration much lower than that required for maximum suppression of peak and steady-state conductances. The present results are not compatible with the hypothesis that calcium competes with local anesthetics for a negatively charged site on the membrane. It is suggested that hydrophobic interactions of local anesthetic molecules with the membrane affect the resting membrane conductance whereas coulombic interactions are responsible for the conductance changes observed during nerve activity.