The Novel Class III Antiarrhythmic Agent MS-551 Blocks the Cardiac Inward Rectifier With Greater Potency Than Sotalol or E-4031: Possible Relevance to Reverse Use Dependence.

Abstract:

:BACKGROUND: The tendency for the electrophysiologic effect of class III antiarrhythmic agents (action potential prolongation) to be diminished at faster heart rates represents a major drawback of this class of drug and is usually referred to as "reverse use dependence." A novel class III agent, MS-551, has recently been reported to exhibit less reverse use dependence than E-4031. We set out to investigate whether this observation may be due to differential blockade of the inward rectifier current (i(K1)) by these drugs. METHODS AND RESULTS: We recorded i(K1) using single channel methods and cell attached patch configurations, with standard patch clamp technology. Neither E-4031 nor racemic sotalol in concentrations up to 100 µM had any significant effect on the open probability or kinetics of i(K1) without altering the single-channel conductance. Openings to subconductance levels were abolished in three of six patches in which they had been frequently present in the absence of drug. MS-551 had no effect on mean channel open time but increased the slower component of the closed time. CONCLUSIONS: MS-551, unlike E-4031 and sotalol, appears to produce significant blockade of the inwardly rectifying potassium channel at clinically relevant concentrations. We propose that this might provide a partial explanation for the observed differences in their response to rate changes.

authors

Nakaya Y,Martin DK,Campbell TJ

doi

10.1177/107424849700200105

keywords:

subject

Has Abstract

pub_date

1997-01-01 00:00:00

pages

39-46

issue

1

eissn

1074-2484

issn

1940-4034

pii

S1074248497000035

journal_volume

2

pub_type

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