Lack of action potential-prolonging effect of terfenadine on rabbit myocardial tissue preparations.
Lack of action potential-prolonging effect of terfenadine on rabbit myocardial tissue preparations.
复制标题
特非那定对兔心肌组织制剂缺乏动作电位延长作用。
DOI：
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发表时间：
2004
影响因子：
2
通讯作者：
K. Shigenobu
中科院分区：
文献类型：
--
作者：
H. Masumiya;M. Saito;Mie Ito;T. Matsuda;K. Noguchi;N. Iida;Hikaru Tanaka;K. Shigenobu
采用微电极技术检查了特非那定（一种抗过敏药物，也因其延长 QT 和致心律失常活性而闻名）对离体家兔心肌组织制剂动作电位的影响。在浦肯野纤维和心房中，特非那丁浓度依赖性地降低最大上升速率（+.V(max)），而不影响其他动作电位参数。在心室中，特非那定对动作电位构型几乎没有影响。在窦房结中，特非那定 20 microM 主要通过抑制 +.V(max) 来延长周期长度。在与微电极实验相同的实验溶液中，特非那定 1 microM 完全抑制 HEK293 细胞中表达的人乙醚 a go-go 相关基因 (HERG) 通道电流。特非那丁对动作电位持续时间缺乏影响表明，有些药物无法根据其在离体心肌组织制剂中的动作电位延长活性来评估其体内 QT 延长的 HERG 通道抑制作用。
The effects of terfenadine, an antiallergic drug also known for its QT-prolonging and arrhythmogenic activities, on the action potential of isolated myocardial tissue preparations from rabbits were examined with microelectrode techniques. In the Purkinje fibers and atrium, terfenadine concentration dependently decreased the maximum rate of rise (+.V(max)) without affecting other action potential parameters. In the ventricle, terfenadine had little effect on action potential configuration. In the sinoatrial node, terfenadine 20 microM prolonged cycle length mainly through inhibition of +.V(max). Terfenadine 1 microM completely inhibited the human ether a go-go-related gene (HERG) channel current expressed in HEK293 cells in the same experimental solution as in microelectrode experiments. The lack of terfenadine effect on the action potential duration suggests that there are drugs for which the HERG channel inhibitory action underlying in vivo QT prolongation cannot be evaluated based on their action potential-prolonging activity in isolated myocardial tissue preparations.
DOI：
10.1073/pnas.91.8.3438
发表时间：
1994-04-12
影响因子：
11.1
作者：
WARMKE, JW;GANETZKY, B
通讯作者：
GANETZKY, B