Lidocaine block of cardiac sodium channels.
نویسندگان
چکیده
منابع مشابه
Lidocaine block of cardiac sodium channels
Lidocaine block of cardiac sodium channels was studied in voltage-clamped rabbit purkinje fibers at drug concentrations ranging from 1 mM down to effective antiarrhythmic doses (5-20 muM). Dose-response curves indicated that lidocaine blocks the channel by binding one-to-one, with a voltage-dependent K(d). The half-blocking concentration varied from more than 300 muM, at a negative holding pote...
متن کاملLidocaine Block of Cardiac Sodium Channels
I N T R O D U C T I O N Lidocaine is effective as an an t i a r rhy thmic agent in the heart over a concent ra t ion range of 5-20 ~ M (Gianelly et al., 1967; Jewi t t et al., 1968; Bellet et al., 1971). Unlike its local anesthet ic effect on nerve, which clearly involves block of Na channels at m u c h higher (>100 /~M) drug concentrat ions (Schmid tmayer and Ulbricht , 1980; Cour tney , 1981;...
متن کاملKinetic Effects of Quarternary Lidocaine Block of Cardiac Sodium Channels" A Gating Current Study
The interaction of antiarrhythmic drugs with ion channels is often described within the context of the modulated receptor hypothesis, which explains the action of drugs by proposing that the binding site has a variable affinity for drugs, depending upon whether the channel is closed, open, or inactivated. Lack of direct evidence for altered gating of cardiac Na channels allowed for the suggesti...
متن کاملKinetic effects of quaternary lidocaine block of cardiac sodium channels: a gating current study
The interaction of antiarrhythmic drugs with ion channels is often described within the context of the modulated receptor hypothesis, which explains the action of drugs by proposing that the binding site has a variable affinity for drugs, depending upon whether the channel is closed, open, or inactivated. Lack of direct evidence for altered gating of cardiac Na channels allowed for the suggesti...
متن کاملBlockade of cardiac sodium channels by lidocaine. Single-channel analysis.
The mechanism of interaction of lidocaine with cardiac sodium channels during use-dependent block is not well defined. We examined the blockade of single cardiac sodium channels by lidocaine and its hydrophobic derivative RAD-242 in rabbit ventricular myocytes. Experiments were performed in cell-attached and inside-out patches. Use-dependent block was assessed with trains of ten 200-msec pulses...
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ژورنال
عنوان ژورنال: Journal of General Physiology
سال: 1983
ISSN: 0022-1295,1540-7748
DOI: 10.1085/jgp.81.5.613