Article
Outward stabilization of the S4 segments in domains III and IV enhances lidocaine block of sodium channels.
The Journal of physiology - 1 Jul 2007
Sheets Michael F, Hanck Dorothy A
Abstract excerpt
The anti-arrhythmic drug lidocaine has been shown to have a lower affinity for block of voltage-gated sodium channels at hyperpolarized potentials compared to depolarized potentials. Concomitantly, lidocaine reduces maximum gating charge (Qmax) by 40% resulting from the complete stabilization of the S4 in domain III in an outward, depolarized position and partial stabilization of the S4 in domain IV in wild-type...
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