Abstract
Some effects of local anaesthetics (cocaine, procaine, amethocaine, and cinchocaine) have been investigated. In this study, the local anaesthetics inhibited citrate synthesis in intact cells of Escherichia coli, brain slices, and homogenates. The drugs also inhibited significantly the oxidation of α-oxoglutarate while having no appreciable effect upon the other isolated steps of the tricarboxylic acid cycle. The local anaesthetics also inhibited malate synthesis in intact cells of E. coli, acetoacetate synthesis, and sulfanilamide acetylation in tissue homogenates. In rats subjected to chronic cocaine treatment, there was no effect upon citrate synthesis in vivo nor were there any changes seen in serum and urine lactate levels and serum Ca 2+ levels. The drugs had no effect upon any of the metabolic reactions in cellular subfractions or on mitochondrial respiration. The drugs had no effect upon Mg 2+stimulated ATPase from rat nerve or on the Na +-sensitive ATPase from rat brain. The results support the probable implication of membrane structure as the site of action of local anaesthetics.
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