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艾司西酞普兰,一种选择性5-羟色胺再摄取抑制剂,可抑制冠状动脉平滑肌细胞中的电压依赖性钾通道。

Escitalopram, a selective serotonin reuptake inhibitor, inhibits voltage-dependent K channels in coronary arterial smooth muscle cells.

作者信息

Kim Han Sol, Li Hongliang, Kim Hye Won, Shin Sung Eun, Seo Mi Seon, An Jin Ryeol, Ha Kwon-Soo, Han Eun-Taek, Hong Seok-Ho, Choi Il-Whan, Choi Grace, Lee Dae-Sung, Park Won Sun

机构信息

Department of Physiology, Kangwon National University School of Medicine, Chuncheon 24341, Korea.

Department of Molecular and Cellular Biochemistry, Kangwon National University School of Medicine, Chuncheon 24341, Korea.

出版信息

Korean J Physiol Pharmacol. 2017 Jul;21(4):415-421. doi: 10.4196/kjpp.2017.21.4.415. Epub 2017 Jun 26.

Abstract

We investigated the inhibitory effect of escitalopram, a selective serotonin reuptake inhibitor (SSRI), on voltage-dependent K (Kv) channels in freshly separated from rabbit coronary arterial smooth muscle cells. The application of escitalopram rapidly inhibited vascular Kv channels. Kv currents were progressively inhibited by an increase in the concentrations of escitalopram, suggesting that escitalopram inhibited vascular Kv currents in a concentration-dependent manner. The IC value and Hill coefficient for escitalopram-induced inhibition of Kv channels were 9.54±1.33 µM and 0.75±0.10, respectively. Addition of escitalopram did not alter the steady-state activation and inactivation curves, suggesting that the voltage sensors of the channels were not affected. Pretreatment with inhibitors of Kv1.5 and/or Kv2.1 did not affect the inhibitory action of escitalopram on vascular Kv channels. From these results, we concluded that escitalopram decreased the vascular Kv current in a concentration-dependent manner, independent of serotonin reuptake inhibition.

摘要

我们研究了选择性5-羟色胺再摄取抑制剂(SSRI)艾司西酞普兰对从兔冠状动脉平滑肌细胞中新鲜分离出的电压依赖性钾(Kv)通道的抑制作用。艾司西酞普兰的应用迅速抑制了血管Kv通道。Kv电流随着艾司西酞普兰浓度的增加而逐渐受到抑制,这表明艾司西酞普兰以浓度依赖性方式抑制血管Kv电流。艾司西酞普兰诱导的Kv通道抑制的IC值和希尔系数分别为9.54±1.33µM和0.75±0.10。添加艾司西酞普兰并未改变稳态激活和失活曲线,这表明通道的电压传感器未受影响。用Kv1.5和/或Kv2.1抑制剂进行预处理并不影响艾司西酞普兰对血管Kv通道的抑制作用。从这些结果中,我们得出结论,艾司西酞普兰以浓度依赖性方式降低血管Kv电流,且与5-羟色胺再摄取抑制无关。

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