| CAS |
141625-93-6 |
| Chinese Name |
决奈达隆盐酸盐 |
| English Name |
Dronedarone Hydrochloride |
| Synonyms |
盐酸决奈达隆;TolfenpyradStandard; |
| Molecular Formula |
C31H45ClN2O5S |
| Molecular Weight |
593.22 |
| Solubility |
Soluble in DMSO ≥3mg/mL |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00914940 |
| SMILES |
CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC.Cl |
| InChIKey |
DWKVCQXJYURSIQ-UHFFFAOYSA-N |
| InChI |
InChI=1S/C31H44N2O5S.ClH/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;1H |
| PubChem CID |
219025 |
| Target Point |
Potassium Channel;Sodium Channel;Calcium Channel |
| Passage |
Membrane Transporter&Ion Channel |
| Background |
It is an effective blocker of ion currents, inhibiting Na+, K+ and Ca2+ currents. |
| Biological Activity |
Dronedarone Hydrochloride是一种非碘化胺酮衍生物，可抑制 Na+、K+ 和 Ca2+ 电流。用于治疗阵发性和持续性房颤或房扑的患者。[1-4] |
| In Vitro |
应用膜片钳技术研究了离体豚鼠心室肌细胞快速Na(+)和Ca(2+)电流以及中国仓鼠卵巢(CHO)细胞表达的人HCN4通道。在豚鼠心室肌细胞中，当保持电位(V(hold))为-80 mV时，dronedarone 对快速Na(+)通道电流表现出状态依赖性抑制，IC(50)为0.7±0.1 μM。在CHO细胞中表达的人HCN4通道被dronedarone阻断，其IC(50)为1.0±0.1 μM。dronedarone对快速Na(+)和Ca(2+)通道的抑制取决于细胞的静息膜电位(状态依赖性阻滞)，有利于心房选择性作用模式。除了快速的Na(+)和Ca(2+)通道外，dronedarone也抑制HCN4电流。[1] 在豚鼠心室肌细胞中，当保持电位为- 80 mV时，dronedarone对快速Na+通道电流表现出状态依赖性抑制，IC50为0.7±0.1 μM。[2] |
| In Vivo |
Dronedarone Hydrochloride在 3 毫克/千克静脉注射时可将心室颤动(VF)的发生率从 80% 显著降至 30%(p < 0.05)，在 10 毫克/千克静脉注射时可消除 VF 并降低死亡率。[3] Dronedarone Hydrochloride可抑制体内颈动脉血栓形成。经屈奈达隆处理的小鼠凝血酶和胶原诱导的血小板聚集功能受损(P/0.05)，动脉壁中纤维蛋白溶解系统的抑制剂--胰蛋白酶原激活物抑制剂-1(PAI1)的表达减少。[4] |
| Data Literature Source |
[1]. Bogdan R，Goegelein H，Ruetten H. Effect of dronedarone on Na+，Ca2+ and HCN channels. Naunyn Schmiedebergs Arch Pharmacol. 2011 Apr;383(4): 347-56. doi: 10.1007/s00210-011-0599-9. Epub 2011 Jan 29.
[2]. Doggrell SA，Hancox JC. Dronedarone: an amiodarone analogue. Expert Opin Investig Drugs. 2004 Apr;13(4): 415-26. doi: 10.1517/13543784.13.4.415.
[3]. Manning AS，et al. SR 33589，a new amiodarone-like agent: effect on ischemia- and reperfusion-induced arrhythmias in anesthetized rats. J Cardiovasc Pharmacol. 1995 Sep;26(3): 453-61.
[4]. Breitenstein A，et al. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol. 2012 Nov;107(6): 302. doi: 10.1007/s00395-012-0302-4. Epub 2012 Sep 29. |
| Unit |
Bottle |
| Specification |
5mg |
English
中文
Manual Download
