Key result
Five quinolizidine derivatives exhibited higher antiarrhythmic activity than reference drugs like amiodarone and lidocaine, with only moderate QT interval prolongation in guinea pig heart tissues.
Why the study?
Do novel quinolizidine derivatives exhibit antiarrhythmic activity with favorable QT profiles compared to standard antiarrhythmic drugs in isolated guinea pig heart tissues?
Do novel quinolizidine derivatives exhibit antiarrhythmic activity with favorable QT profiles compared to standard antiarrhythmic drugs in isolated guinea pig heart tissues?
Novel quinolizidine derivatives demonstrate potent antiarrhythmic activity with favorable QT profiles compared to standard antiarrhythmic drugs in preclinical models.
Quinolizidine derivatives merit further preclinical testing; leaves open translation to in vivo efficacy and human safety.
Fifteen quinolizidine derivatives have been tested for antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig (gp) heart tissues and to assess calcium antagonist activity. All compounds exhibited from moderate to high antiarrhythmic activity, and five of them (3, 4, 6, 13, and 15) were more active and potent than the reference drugs (amiodarone, lidocaine, procainamide, and quinidine). These compounds were studied on spontaneously beating Langendorff-perfuse gp heart; even at concentration 17-67 times higher than the corresponding EC(50) for antiarrhythmic activity, they prolonged the QT intervals only moderately, comparing favorably with amiodarone and quinidine. Compounds 3 and 15 deserve further investigation due to their interesting cardiovascular profiles.
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Tasso et al. (2010) studied Arrhythmia. Quinolizidine derivatives vs. Reference drugs (amiodarone, lidocaine, procainamide, and quinidine) was evaluated on Antiarrhythmic, inotropic, and chronotropic effects, and calcium antagonist activity. Five quinolizidine derivatives exhibited higher antiarrhythmic activity than reference drugs like amiodarone and lidocaine, with only moderate QT interval prolongation in guinea pig heart tissues.
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