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Dronedarone

CAS No. : 141626-36-0

MCE 站：Dronedarone

产品活性：Dronedarone (SR 33589) 是胺碘酮 (HY-14187) 的衍生物，是一种用于研究心房颤动 (AF) 的 class III 抗心律失常的试剂 (antiarrhythmic agent)。Dronedarone 是多种离子电流 (ion currents) 的有效阻滞剂，包括钾电流，钠电流，和 L 型钙电流，并通过非竞争性结合到肾上腺素能受体显示出抗肾上腺素能的效果。Dronedarone 是 CYP3A4 的底物和中度抑制剂。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease  |  Autophagy

作用靶点：mAChR  |  Sodium Channel  |  Calcium Channel  |  Adrenergic Receptor  |  Cytochrome P450  |  Autophagy

In Vitro: In patch clamp experiments using human atrial myocytes, Dronedarone produces potent blockade of peak sodium current, resulting in a 97% block at 3 μM.
In guinea pig ventricular myocytes, Dronedarone inhibits the rapidly activating delayed-rectifier potassium current (IC₅₀<3 μM), the slowly activating delayed-rectifier potassium current (IC₅₀=10 μM), the inward rectifier potassium current (IC₅₀>30 μM), and L-type calcium current (IC₅₀=0.18 μM).
Dronedarone exhibits strong inhibitory effects on the acetylcholine-activated potassium current (I_K-Ach) in rabbit inoatrial nodal cells (IC₅₀=63 nM) and guinea pig atrial cells (IC₅₀=10 nM). Blockade of I_K-Ach by dronedarone is 100 times more potent than that of amiodarone.
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.
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.

In Vivo: Dronedarone (intraperitoneal injection; 25-100 mg/kg) exhibits anticonvulsant effects in a dose-dependent manner and increases the threshold for electroconvulsions in mice.

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