State-dependent block of human cardiac hNav1.5 sodium channels by propafenone.

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Edrich T, Wang SY, Wang GK

State-dependent block of human cardiac hNav1.5 sodium channels by propafenone.

J Membr Biol. 2005 Sep;207(1):35-43. doi: 10.1007/s00232-005-0801-4.

PubMed ID

16463141 [ View in PubMed

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Abstract

State-dependent blockade of human cardiac hNav1.5 sodium channels by propafenone was studied using whole-cell patch clamp techniques. Both a direct investigation using cells with inactivation-deficient sodium channels and an algorithmic approach used on cells with wild-type channels revealed a rapid binding of propafenone to the open state. This occurs approximately 4000 and 700 times faster than the binding to the resting and inactivated state, respectively. An established mathematical "gating" model was modified to represent the experimental data.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Propafenone	Sodium channel protein type 5 subunit alpha	Protein	Humans	Yes	Inhibitor	Details