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

Journal Article · Tue Jan 01 00:00:00 EST 1991 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(91)90363-G· OSTI ID:5947390

Oppenheimer, E; Harel, G; Lipinsky, D; Sarne, Y ^[1]

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1. Tel-Aviv Univ. (Israel)

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 I{sub A}). EO-199 did not block significantly the activity of a class I{sub B} antiarrhythmic agent, lidocaine. EO-199 also displaced the specific binding of ({sup 3}H)EO-122 to rate 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 (I{sub A}) but not lidocaine (I{sub B}), 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 as an antidote in cases of antiarrhythmics overdose intoxication.

• OSTI ID: 5947390
• Journal Information: Life Sciences; (USA), Vol. 48:10; ISSN 0024-3205
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
CARDIOVASCULAR AGENTS
BIOCHEMICAL REACTION KINETICS
CELL MEMBRANES
HEART
IN VIVO
RATS
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
BODY
CARDIOVASCULAR SYSTEM
CELL CONSTITUENTS
DRUGS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
ORGANS
PROTEINS
REACTION KINETICS
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques