Molecular mechanism of allosteric modification of voltage-dependent sodium channels by local anesthetics
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چکیده
منابع مشابه
Molecular mechanism of allosteric modification of voltage-dependent sodium channels by local anesthetics
The hallmark of many intracellular pore blockers such as tetra-alkylammonium compounds and local anesthetics is their ability to allosterically modify the movement of the voltage sensors in voltage-dependent ion channels. For instance, the voltage sensor of domain III is specifically stabilized in the activated state when sodium currents are blocked by local anesthetics. The molecular mechanism...
متن کاملThe role of inactivation in the cumulative blockage of voltage-dependent sodium channels by local anesthetics and antiarrythmics.
Previously published results (Khodorov 1973; Khodorov et al. 1974, 1976; Zaborovskaya 1976) showed that along with a decrease in the maximum sodium permeability ('tonic block') the tertiary amine local anesthetics (LA), procaine and trimecain cause a drastic slowing of Na channel reactivation after membrane depolarization. This effect ("drug-induced slow Na inactivation") underlies a use-depend...
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BACKGROUND The general anesthetic ketamine is known to be an N-methyl-D-aspartate receptor blocker. Although ketamine also blocks voltage-gated sodium channels in a local anesthetic-like fashion, little information exists on the molecular pharmacology of this interaction. We measured the effects of ketamine on sodium channels. METHODS Wild-type and mutant (F1579A) recombinant rat skeletal mus...
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ژورنال
عنوان ژورنال: Journal of General Physiology
سال: 2010
ISSN: 1540-7748,0022-1295
DOI: 10.1085/jgp.201010438