| CAS |
141626-36-0 |
| Chinese Name |
决奈达隆 |
| English Name |
Dronedarone |
| Synonyms |
决奈达隆;Dronedarone;Multaq;UNII-JQZ1L091Y2; |
| Molecular Formula |
C31H44N2O5S |
| Molecular Weight |
556.76 |
| Solubility |
Soluble in DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00910331 |
| SMILES |
CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC |
| InChIKey |
ZQTNQVWKHCQYLQ-UHFFFAOYSA-N |
| InChI |
InChI=1S/C31H44N2O5S/c1-5-8-12-29-30(27-23-25(32-39(4，35)36)15-18-28(27)38-29)31(34)24-13-16-26(17-14-24)37-22-11-21-33(19-9-6-2)20-10-7-3/h13-18，23，32H，5-12，19-22H2，1-4H3 |
| PubChem CID |
208898 |
| Target Point |
Sodium Channel; Calcium Channel; Adrenergic Receptor |
| Passage |
Membrane Transporter&Ion Channel;Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling |
| Background |
It is an effective blocker of a variety of ion currents, including potassium currents, sodium currents, and L-shaped calcium currents, and exhibits an anti-adrenergic effect by noncompetitively binding to the adrenergic receptor. |
| Biological Activity |
Dronedarone (SR 33589)是胺碘酮(HY-14187)的衍生物，是III类抗心律失常药物，用于房颤(AF)和心房扑动的研究。Dronedarone是多种离子电流的有效阻滞剂，包括钾电流、钠电流和l型钙电流，并通过与β-肾上腺素能受体的非竞争性结合表现出抗肾上腺素能作用。Dronedarone是CYP3A4的底物和中度抑制剂。[1] |
| In Vitro |
在使用人心房肌细胞的膜片钳实验中，Dronedarone对峰值钠电流产生有效阻断，在3 μM处阻断97%。在豚鼠心室肌细胞中，Dronedarone抑制快速激活的延迟整流钾电流(IC50<3 μM)、缓慢激活的延迟整流钾电流(IC50=10 μM)、内向整流钾电流(IC50>30 μM)和l型钙电流(IC50=0.18 μM)。对家兔心房结细胞(IC50=63 nM)和豚鼠心房细胞(IC50=10 nM)乙酰胆碱激活钾电流(IK-Ach)有较强的抑制作用。Dronedarone对IK-Ach的阻断作用是胺碘酮的100倍。Dronedarone通过非竞争性结合β-肾上腺素能受体(IC50=1.8 μM)和抑制激动剂诱导的腺苷酸环化酶活性增加来发挥其抗肾上腺素能作用。Dronedarone(0.01-1 μM)可诱导离体豚鼠心脏冠脉灌注压浓度依赖性降低，其作用不依赖于一氧化氮合酶途径，可能与其钙电流阻断有关。[1] |
| In Vivo |
Dronedarone(腹腔注射;25-100 mg/kg)表现出剂量依赖性的抗惊厥作用，并增加小鼠电惊厥阈值。[2] |
| Data Literature Source |
[1]. Patel C，et al. Circulation. 2009 Aug 18;120(7): 636-44. doi: 10.1161/CIRCULATIONAHA.109.858027.
[2]. Sawicka KM，et al. Influence of dronedarone (a class III antiarrhythmic drug) on the anticonvulsant potency of four classical antiepileptic drugs in the tonic-clonic seizure model in mice. J Neural Transm (Vienna). 2019 Feb;126(2): 115-122. |
| Unit |
Bottle |
| Specification |
10mg |
English
中文
Manual Download
