DronedaroneDronedarone
MedChemExpress (MCE)
HY-A0016
141626-36-0
SR 33589
99.93%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
In patch clamp experiments using human atrial myocytes, Dronedarone produces potent blockade of peak sodium current, resulting in a 97% block at 3 μM[1].In guinea pig ventricular myocytes, Dronedarone inhibits the rapidly activating delayed-rectifier potassium current (IC5050=10 μM), the inward rectifier potassium current (IC50>30 μM), and L-type calcium current (IC50=0.18 μM)[1].Dronedarone exhibits strong inhibitory effects on the acetylcholine-activated potassium current (IK-Ach) in rabbit inoatrial nodal cells (IC50=63 nM) and guinea pig atrial cells (IC50=10 nM). Blockade of IK-Ach by dronedarone is 100 times more potent than that of amiodarone[1].Dronedarone exerts its antiadrenergic effects by noncompetitive binding to β-adrenergic receptors (IC50=1.8 μM) and inhibition of agonist-induced increases in adenylate cyclase activity[1]. Dronedarone (0.01-1 μM) induces a concentration-dependent reduction of coronary perfusion pressure in isolated guinea pig hearts, effects that are independent of the nitric oxide synthase pathway and possibly related to its calcium current blockade[1].
Dronedarone (intraperitoneal injection
25-100 mg/kg) exhibits anticonvulsant effects in a dose-dependent manner and increases the threshold for electroconvulsions in mice[2].
L-type calcium channel CYP3
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[1]. Chinmay Patel, et al. Dronedarone. Circulation. 2009 Aug 18
120(7):636-44. [Content Brief]
[2]. Katarzyna M Sawicka, et al. Influence of dronedarone (a class III antiarrhythmic drug) on the anticonvulsant potency of four classical antiepileptic drugs in the tonic-clonic seizure model in mice. J Neural Transm (Vienna). 2019 Feb
126(2):115-122. [Content Brief]