Comparison of effects of selected local anesthetics on sodium and potassium channels in mammalian neuron.
Effects of procaine, trimecaine, and a new carbanilate local anesthetic, carbizocaine, on early sodium inward current and fast and slow components of potassium outward current in the membrane of the rat dorsal root ganglion neuron were studied using the internal dialysis and potential clamp techniques. All the currents studied were depressed in the presence of the drugs tested. However, for inhibition of the inward current concentrations lower by approximately one to more than two orders were sufficient compared to those required for similar inhibition of the outward currents. Carbizocaine was the most effective, procaine the least effective drug. Almost identical ratios of the negative logarithms of mean effective concentrations for blocking the inward and the outward current respectively, were found for each of the drugs tested. None of the drugs could be characterized as a specific blocker of sodium or potassium channels. It is concluded that the mechanisms of action of these three local anesthetics in all the three types of ion channels studied in the neuronal membrane are very similar regardless of both the type of the chemical bond in the intermediary chain of the molecules (ester, anilide, carbanilate) and the structure of the aromatic moiety, or the absolute potency of the drug.
Stolc
S
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Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava.
D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D002219:Carbamates / Q000494:pharmacology; D004558:Electric Stimulation; D005727:Ganglia, Spinal / Q000187:drug effects / Q000502:physiology*; D007473:Ion Channels / Q000187:drug effects*; D008564:Membrane Potentials; D010477:Perfusion; D011343:Procaine / Q000494:pharmacology; D051381:Rats; D014288:Trimecaine / Q000494:pharmacology
D000779:Anesthetics, Local; D002219:Carbamates; D007473:Ion Channels; D011343:Procaine; C046030:carbizocaine; D014288:Trimecaine