TY - JOUR
T1 - EO-199, a specific antagonist of antiarrhythmic drugs
T2 - Assessment by binding experiments and in vivo studies
AU - Oppenheimer, Edna
AU - Harel, Gideon
AU - Lipinsky, Dafna
AU - Sarne, Yosef
N1 - Funding Information:
This work was supported by grants Health and the Slezak Foundation.
PY - 1991
Y1 - 1991
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0026035106&partnerID=8YFLogxK
U2 - 10.1016/0024-3205(91)90363-G
DO - 10.1016/0024-3205(91)90363-G
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AN - SCOPUS:0026035106
SN - 0024-3205
VL - 48
SP - 977
EP - 985
JO - Life Sciences
JF - Life Sciences
IS - 10
ER -