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一种抑制钾通道的抗心律失常药物;一种快速激活净延迟整流K+电流内向整流成分的抑制剂(豚鼠心肌细胞中的IC50=31.5nM);在1µM时具有致心律失常活性,在细胞中诱导早期后去极化,并在10mg/kg剂量下在兔子中诱导尖端扭转型室性心动过速以检测其致心律失常特性。An antiarrythmic agent that inhibits potassium channels; an inhibitor of the rapidly activating inward rectifying component of net delayed rectifier K+ current (IC50 = 31.5 nM in guinea pig cardiomyocytes); has pro-arrhythmic activity at 1 µM, inducing early afterdepolarizations in cells and Torsade de Pointes in a rabbit screen for proarrhythmic properties at a dose of 10 mg/kg.
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文献和实验相关实验
A High-Throughput Binding Assay for HERG
. However, these are time-consuming and expensive, and so a simple assay, suitable for general laboratory use, would be beneficial. The authors have established a radioligand binding assay that utilizes [3 H]dofetilide and membranes prepared from HEK293 cells stably
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Dofetilide
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