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  • Title: Pyrethroid modifications of the activation and inactivation kinetics of the sodium channels in squid giant axons.
    Author: de Weille JR, Brown LD, Narahashi T.
    Journal: Brain Res; 1990 Mar 26; 512(1):26-32. PubMed ID: 2159827.
    Abstract:
    The kinetics of sodium channel activation and inactivation were analyzed in the squid giant axons internally treated with various pyrethroids. Pyrethroids increased the steady-state sodium current in squid giant axons by removing the inactivation. The steady-state sodium conductances in control and pyrethroid-treated axons showed the same voltage dependence, indicating that the removal of inactivation by pyrethroids did not lead to an alteration of gating charge transfer. The pyrethroid-modified sodium channels were activated with a biphasic time course involving the movement of at least two gating particles, and both components were voltage-dependent. The slower component was abolished by treatment with either pronase or N-bromoacetamide. The net elementary charges transported in the electric membrane field were reduced in the course of slow activation of the pyrethroid-induced sodium current. It appears that the 'immobilization' of gating charge is related to the slow activation rather than the inactivation of the sodium channel.
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