QT prolongation in anaesthetized guinea‐pigs: an experimental approach for preliminary screening of torsadogenicity of drugs and drug candidates

QT prolongation in anaesthetized guinea‐pigs: an experimental approach for preliminary screening of torsadogenicity of drugs and drug candidates
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麻醉豚鼠的 QT 延长:初步筛选药物和候选药物扭转致伤性的实验方法

DOI:
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发表时间:
2004
影响因子:
3.3
通讯作者:
E. Martinotti
E. Martinotti
中科院分区:
医学4区
文献类型:
--
作者:
L. Testai;V. Calderone;A. Salvadori;M. Breschi;P. Nieri;E. Martinotti

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许多非心血管药物可以延长心电图的QT间期;这是一种辅助属性,不是其药理作用所必需的,通常与钾通道阻断和心脏复极延迟有关。QT延长可导致危险的快速性心律失常,称为尖端扭矩,并有可能导致致死性的室性fi颤动。实验方法旨在对这一不受欢迎的财产进行早期识别,通常需要复杂而昂贵的设备或使用高级动物物种(狗、灵长类动物),而出于伦理和/或经济原因,这些动物物种不容易使用。
Many non‐cardiovascular drugs can prolong the QT interval of the electrocardiogram (ECG); this is an accessory property not necessary for their pharmacological action and generally linked to the block of the potassium HERG channels and delayed cardiac repolarization. The QT prolongation can lead to a dangerous tachyarrhythmia, called torsade de pointes, and potentially to fatal ventricular fibrillation. The experimental approaches, aimed at an early identification of this undesidered property, often require sophisticated and expensive equipment or the use of superior animal species (dog, primates) that cannot be employed easily for ethical and/or economic reasons.