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Dronedarone Hydrochloride

CAS No. : 141625-93-6

MCE 国际站：Dronedarone Hydrochloride

产品活性：Dronedarone Hydrochloride 是一种非碘化胺碘酮衍生物, 可抑制Na⁺, K⁺ and Ca²⁺的电流。

研究领域：Membrane Transporter/Ion Channel  |  Autophagy

作用靶点：Potassium Channel  |  Autophagy

In Vitro: 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 I_Kr (IC₅₀=3 μM) and I_Ca-L (IC₅₀=0.18 μM). The effects on I_Ca-L are use- and frequency-dependent. Dronedarone inhibits current carried by human ether-a-go-go gene (HERG)-expressing oocytes (analagous to I_Kr) with an IC₅₀ of 9 μM. 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.

In Vivo: Dronedarone (Hydrochloride) reduces significantly the incidence of ventricular fibrillation (VF) from 80 to 30% (p < 0.05) at 3 mg/kg i.v. and eliminated VF and mortality at 10 mg/kg i.v. . Dronedarone inhibited carotid artery thrombus formation 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.

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