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Dronedarone

CAS No. : 141626-36-0

MCE 國際站：Dronedarone

產(chǎn)品活性：Dronedarone (SR 33589) 是胺碘酮 (HY-14187) 的衍生物，是一種用于研究心房顫動 (AF) 的 class III 抗心律失常的試劑 (antiarrhythmic agent)。Dronedarone 是多種離子電流 (ion currents) 的有效阻滯劑，包括鉀電流，鈉電流，和 L 型鈣電流，并通過非競爭性結(jié)合到腎上腺素能受體顯示出抗腎上腺素能的效果。Dronedarone 是 CYP3A4 的底物和中度抑制劑。

研究領(lǐng)域：GPCR/G Protein  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease  |  Autophagy

作用靶點：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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