Article
Quaternary ammonium block of mutant Na+ channels lacking inactivation: features of a transition-intermediate mechanism.
The Journal of physiology - 15 Nov 2000
Kimbrough J T, Gingrich K J
Abstract excerpt
1. The quaternary ammonium (QA) lidocaine derivative QX-314 (2-(triethylamino)-N-(2,6-dimethylphenyl)-acetamide) induces internal pore blockade of single cardiac Na+ channels enzymatically modified (papain) to eliminate fast inactivation. The mechanism involves dual, interacting blocking modes (rapid and discrete) with binding domains deep in the pore from the cytoplasmic mouth, and where the rapid blocked...
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