EO-199, a specific antagonist of antiarrhythmic drugs: Assessment by binding experiments and in vivo studies

Edna Oppenheimer, Gideon Harel, Dafna Lipinsky, Yosef Sarne

Research output: Contribution to journalArticlepeer-review

Abstract

EO-199, a demethylated analog of the novel class I antiarrhythmic drug EO-122 was found to antagonize the antiarrhythmic activity of EO-122 and that of procainamide (Class IA). EO-199 did not block significantly the activity of a class IB antiarrhythmic agent, lidocaine. EO-199 also displaced the specific binding of [3H]EO-122 to rat heart membranes similarly to procainamide whereas lidocaine did not. The correlation between binding experiments and pharmacological effects points to a possible subclassification of these drugs; the two chemical analogs EO-199 and EO-122, as well as procainamide (IA) but not lidocaine (IB), compete at the same site or the same state of the sodium channel. The availability of a specific antagonist might be useful for studying the mechanism of action of antiarrhythmic drugs as well ad an antidote in cases of antiarrhythmics overdose intoxication.

Original languageEnglish
Pages (from-to)977-985
Number of pages9
JournalLife Sciences
Volume48
Issue number10
DOIs
StatePublished - 1991

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