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Local Anesthetics Inhibit the Ca 2+ ,Mg 2+ ‐ATPase Activity of Rat Brain Synaptosomes
Author(s) -
GarciaMartin Elena,
GutiérrezMerino Carlos
Publication year - 1986
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1986.tb00663.x
Subject(s) - dibucaine , tetracaine , procaine , chemistry , anesthetic , atpase , vesicle , biophysics , potency , general anesthetics , pharmacology , synaptosome , biochemistry , lidocaine , in vitro , anesthesia , membrane , enzyme , biology , medicine
Many biochemical effects of local anesthetics are expressed in Ca 2+ ‐dependent processes [Volpi M., Sha'afi R. I., Epstein P. M., Andrenyak P. M., and Feinstein M. B. (1981) Proc. Natl. Acad. Sci. USA 78, 795–799]. In this communication we report that local anesthetics (dibucaine, tetracaine, lidocaine, and procaine and the analogue quinacrine) inhibit the Ca 2+ ‐dependent and the Mg 2+ ‐dependent ATPase activity of rat brain synaptosomes and of membrane vesicles derived from them by osmotic shock. This inhibition is induced by concentrations of these drugs close to their pharmacological doses, and a good correlation between K 0.5 of inhibition and their relative anesthetic potency is found. The Ca 2+ ‐dependent ATPase is more selectively inhibited at lower drug concentrations. The physiological relevance of these findings is discussed briefly.