IR@PKUHSC  > 北京大学第三临床医学院  > 心血管内科
学科主题临床医学
Pharmacological effects of carvedilol on T-type calcium current in murine HL-1 cells
Deng, Chunyu2; Rao, Fang2; Wu, Shulin2; Kuang, Sujuan2; Liu, Xiaoying2; Zhou, Zhiling2; Shan, Zhixin2; Lin, Quxiong2; Qian, Weimin2; Yang, Min2; Geng, Qingshan2; Zhang, Youyi3; Yu, Xiyong1,2; Lin, Shuguang2
关键词Carvedilol Hl-1 Cells T-type Calcium Current (i(Ca Whole-cell Patch-clamp Technique t))
刊名EUROPEAN JOURNAL OF PHARMACOLOGY
2009-10-25
DOI10.1016/j.ejphar.2009.08.032
621期:1-3页:19-25
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]CHANNEL BLOCKER ; CA2+ CHANNEL ; VENTRICULAR MYOCYTES ; HEART ; PROLIFERATION ; ANTIOXIDANT ; EXPRESSION ; MIBEFRADIL ; PREVENTS ; DRUG
英文摘要

Carvedilol is widely used in the treatment of cardiovascular diseases including atrial fibrillation. T-type Ca(2+) channels have been recognized recently in the mechanisms underlying atrial arrhythmias. However, it is unclear whether carvedilol may affect the T-type Ca(2+) channel. The present study evaluated the pharmacological effects of carvedilol on T-type calcium current (I(Ca,T)) in the murine HL-1 cell line. I(Ca,T) was recorded by the whole-cell patch-clamp technique. Calcium transient was monitored by the fluorescent dye Fluo-4/AM and confocal laser scanning microscopy. Carvedilol reversibly inhibited I(Ca,T) in a concentration-dependent manner, with an IC50 of 2.1 mu M. 3 mu M carvedilol was found to decrease the peak I(Ca,T) amplitude at -20 mV from 20.1 +/- 1.8 pA/pF to 10.9 +/- 2.1 pA/pF. Carvedilol significantly shifted the steady-state inactivation curve of I(Ca,T) towards more negative potential by 12.8 mV, while the activation curve was not significantly altered. Carvedilol delayed recovery from inactivation of I(Ca,T), time constant (tau) Was 112.4 +/- 3.5 ms in control and 270.1 +/- 4.7 ms in carvedilol. Carvedilol-induced inhibition rate in I(Ca,T) Was enhanced with the increase in stimuli frequency, the inhibitory rate was 23.2 +/- 4.1% at 0.2 Hz and 47.2 +/- 0.6% at 2 Hz. Carvedilol still produced the significant decrease in the amplitude of I(Ca,T) in the presence of H-89, PKA inhibitor. Carvedilol significantly inhibited the amplitude of the calcium transient in a concentration-dependent manner. These findings indicate that carvedilol inhibits I(Ca,T) in atrial cells by mechanisms involving preferential interaction with the inactivated state of T-type Ca(2+) channel. (C) 2009 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000271153000003
项目编号30672077 ; 30700328 ; 30772620 ; 2006CB503806 ; A2006002
资助机构National Natural Science Foundation of China ; National Key Basic Research Program (NKBRP) of China ; Medical Science Foundation of Guangdong
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52760
专题北京大学第三临床医学院_心血管内科
作者单位1.Guangdong Gen Hosp, Guangdong Acad Med Sci, Med Res Ctr, Guangzhou 510080, Guangdong, Peoples R China
2.Guangdong Prov Cardiovasc Inst, Dept Cardiol, Guangzhou 510080, Guangdong, Peoples R China
3.Peking Univ, Hosp 3, Inst Vasc Med, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Deng, Chunyu,Rao, Fang,Wu, Shulin,et al. Pharmacological effects of carvedilol on T-type calcium current in murine HL-1 cells[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2009,621(1-3):19-25.
APA Deng, Chunyu.,Rao, Fang.,Wu, Shulin.,Kuang, Sujuan.,Liu, Xiaoying.,...&Lin, Shuguang.(2009).Pharmacological effects of carvedilol on T-type calcium current in murine HL-1 cells.EUROPEAN JOURNAL OF PHARMACOLOGY,621(1-3),19-25.
MLA Deng, Chunyu,et al."Pharmacological effects of carvedilol on T-type calcium current in murine HL-1 cells".EUROPEAN JOURNAL OF PHARMACOLOGY 621.1-3(2009):19-25.
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