Analysis of the inhibitory effect of eugenol on voltage-gated Na+ channels of sensory neurons. / Análise do efeito inibitório do eugenol sobre canais para Na+ ativados por voltagem em neurônios sensitivos.

AUTOR(ES)
DATA DE PUBLICAÇÃO

2010

RESUMO

The previously described inhibitory effects of eugenol (EUG) on voltage-activated Na+ channels (Nav) are not compatible with our results. We have studied the effects of EUG on macroscopic Na+ currents and compared them to the effects of lidocaine, a local anesthetic. EUG blocked both mixed (TTX-S and TTX-R) and TTX-R Na+ currents in a fast and reversible manner. The values of IC50 for the inhibition of mixed and TTX-R currents were 2.28 and 2.27 mmol/L respectively. The blockade depends on frequency of depolarizing pulses. In mixed currents EUG displaced the activation curve to the right, the inactivation curve to the left, does not alter the inactivation kinetics and retards the recovery from inactivation, fast and slow, of the Na+ channels. In TTX-R currents, EUG effects were similar, except on the activation curve, which was not shifted. In conclusion, EUG blocks Nav by binding to the resting and inactivated conformational states of channels, fast and slow. EUG effects resembles lidocaine ones, but are not identical.

ASSUNTO(S)

sodium currents eletrofisiologia eugenol patch champ sodium channels correntes de sódio canais iônicos eugenol ion channels patch champ electrophysiology canais de sódio

ACESSO AO ARTIGO

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