CAS NO: | 54143-56-5 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 474.39 |
Cas No. | 54143-56-5 |
Formula | C19H24F6N2O5 |
Synonyms | Tambocor |
Solubility | ≥23.7 mg/mL in H2O with gentle warming and ultrasonic; ≥47.4 mg/mL in DMSO; ≥47.4 mg/mL in EtOH |
Chemical Name | acetic acid;N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide |
Canonical SMILES | CC(=O)O.C1CCNC(C1)CNC(=O)C2=C(C=CC(=C2)OCC(F)(F)F)OCC(F)(F)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Flecainide作为无选择性Na(+)通道阻断剂,是1C类抗心律失常药,尤其用于室上性心律失常的治疗。Flecainide广泛用于促进长期窦性节律(SR)恢复并减轻房颤症状。
Flecainide能够抑制心Nav1.5钠通道,延长心肌动作电位。Flecainide能够降低完整大鼠心肌细胞的Ca+放电、波动频率和Ca+波速。另外,Flecainide能在I(Na)激活的时候降低Ca(2+)波。有证据表明Flecainide能够显著提高Na(+)/Ca(2+)-交换泵 (NCX)介导的Ca(2+)外流[1]。
Flecainide能够延长心室复极化,在左心室外膜与右心室外膜连接处作用更强。Flecainide作用于心内膜能够比心外膜更能促进有效不应期(ERP)延长,导致穿过心室壁的ERP离散显著增加[2]。
Flecainide剂量依赖性减少全身性压力(0.8 μg/ml时32%)和外围血管压力(0.8 μg/ml时15%)。大鼠后肢灌注模型中,治疗性血浆浓度0.8 μg/ml Flecainide能够显著降低心率(55次/分)并提高QRS间隔(9.9毫秒)[3]。
参考文献:
1. Sikkel MB1, Collins TP, Rowlands C, Shah M, O'Gara P, Williams AJ, Harding SE, Lyon AR, MacLeod KT. Flecainide reduces Ca(2+) spark and wave frequency via inhibition of the sarcolemmal sodium current. Cardiovasc Res. 2013 May 1;98(2):286-96. doi: 10.1093/cvr/cvt012. Epub 2013 Jan 19.
2. Osadchii OE.Flecainide-induced proarrhythmia is attributed to abnormal changes in repolarization and refractoriness in perfused guinea-pig heart. J Cardiovasc Pharmacol. 2012 Nov;60(5):456-66. doi: 10.1097/FJC.0b013e31826b86cf.
3. Allison B1, Yang Y, Pourrier M, Gibson JK. Comparison of the in vivo hemodynamic effects of the antiarrhythmic agents vernakalant and flecainide in a rat hindlimb perfusion model. J Cardiovasc Pharmacol. 2011 Apr;57(4):463-8. doi: 10.1097/FJC.0b013e318210276b.