| Bioactivity | Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents. |
| Invitro | Dronedarone (SR-33589) is a multichannel blocker for atrial fibrillation . It is a potent inhibitor of the acetylcholine-activated K+ current from atrial and sinoatrial nodal tissue, and inhibits the rapid delayed rectifier more potently than slow and inward rectifier K+ currents and inhibits L-type calcium current. Under whole-cell patch clamp, it blocks IKr (IC50=3 μM) and ICa-L (IC50=0.18 μM). The effects on ICa-L are use- and frequency-dependent. Dronedarone inhibits current carried by human ether-a-go-go gene (HERG)-expressing oocytes (analagous to IKr) with an IC50 of 9 μM[1]. In guinea pig ventricular myocytes, dronedarone exhibits a state dependent inhibition of the fast Na+ channel current with an IC50 of 0.7±0.1 μM, when the holding potential is −80 mV[2]. |
| In Vivo | Dronedarone (Hydrochloride) reduces significantly the incidence of ventricular fibrillation (VF) from 80 to 30% (p in vivo. Thrombin- and collagen-induced platelet aggregation is impaired indronedarone-treated mice (P\0.05), and expression ofplasminogen activator inhibitor-1 (PAI1), an inhibitor of the fibrinolytic system, is reduced in the arterial wall[4]. |
| Name | Dronedarone Hydrochloride |
| CAS | 141625-93-6 |
| Formula | C31H45ClN2O5S |
| Molar Mass | 593.22 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Bogdan R, et al. Effect of?dronedarone?on Na+, Ca2+ and HCN channels. Naunyn Schmiedebergs Arch Pharmacol.?2011 Apr;383(4):347-56.? [2]. Doggrell SA, et al. Dronedarone: an amiodarone analogue. Expert Opin Investig Drugs. 2004 Apr;13(4):415-26. [3]. Manning AS, et al. SR 33589, a new amiodarone-like agent: effect on ischemia- and reperfusion-induced arrhythmias in anesthetized rats. J Cardiovasc Pharmacol. 1995 Sep;26(3):453-61. [4]. Breitenstein A, et al. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol. 2012 Nov;107(6):302. |
Dronedarone Hydrochloride
CAS: 141625-93-6 F: C31H45ClN2O5S W: 593.22
Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
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