Dronedarone 是一种胺碘酮类似物，对治疗心房颤动可能有效。它是CYP3A4的底物和中度抑制剂。它是多种离子电流的有效阻滞剂，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 is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Dronedarone reduces the incidence of early and delayed after depolarizations evoked by 1 mM Dofetilide and 0.2 mM Strophantidine in Purkinje fibres. Dronedarone (10 mM) markedly reduces the L-type calcium current (76.5%) and the rapid component of the delayed rectifier potassium current (97%) in ventricular myocytes [1]. Dronedarone inhibits the activity of I(K(ACh)) channels recorded from cell-attached patches by reducing the channel open probability (from 0.56 to 0.11) without modification of the single-channel conductance in single cells isolated from sinoatrial node (SAN) tissue of rabbit hearts [2]. Dronedarone exhibits a state-dependent inhibition of the fast Na(+) channel current with an IC50 of 0.7 μM in guinea pig ventricular myocytes, when the holding potential (V (hold)) is -80 mV. Dronedarone blocks Ca(2+) currents elicited by rectangular pulses at V (hold)?=?-40 mV with IC50 value of 0.4 μM, whereas at V (hold)?=?-80 mV, Dronedarone (10 μM) blocks only 20?% of the current [3].

Dronedarone increases action potential duration in normal hearts of rats. Dronedarone reduces the late sustained K(+) current, I(K) (or Isus) by 69%. Dronedarone induces only a tonic block of I(K). Dronedarone induces a weak increase in the fast transient outward current, I(to), in rats after myocardial infarction [4].

141626-36-0

C31H44N2O5S

556.76

SR 33589;决奈达隆

DMSO:27.8 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years