Background:

Dronedarone HCL is an amiodarone analogue which has been shown an effective and promising treatment for Atrial fibrillation (AF) [1].

In vitro, dronedarone has been demonstrated to inhibit muscarinic acetylcholine receptor-operated K+ current IK(ACh) induced by carbachol or GTP-gamma-S with IC50 values of 10nm and<100nm, respectively, in cells isolated from guinea pig atria. Notably, dronedarone was 100-fold potent and selective over amiodarone in inhibiting IK(ACh) [1].

In vivo, dronedarone has shown to block arterial thrombus formation, decrease platelet aggregation and reduce plasminogen activator inhibitor-1 (PAI1) expression in C57Bl/6 mice [2].

参考文献:
[1] Guillemare E1,?Marion A,?Nisato D,?Gautier P. Inhibitory effects of?dronedarone?on muscarinic K+ current in guinea pig atrial cells. J Cardiovasc Pharmacol.?2000 Dec;36(6):802-5.
[2] Breitenstein A1,?Sluka SH,?Akhmedov A,?Stivala S,?Steffel J,?Camici GG,?Riem HH,?Beer HJ,?Studt JD,?Duru F,?Luscher TF,?Tanner FC. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol.?2012 Nov;107(6):302.