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羟苯氨酮激活家兔血管平滑肌细胞钙敏感钾通道
引用本文:李安龙,刘忠武,朱丽霞,张德昌,叶益新. 羟苯氨酮激活家兔血管平滑肌细胞钙敏感钾通道[J]. 药学学报, 2004, 39(2): 101-104
作者姓名:李安龙  刘忠武  朱丽霞  张德昌  叶益新
作者单位:1. 中国医学科学院、中国协和医科大学,基础医学研究所,药理室,北京,100005
2. 中国中医研究院,针灸所,北京,100700
基金项目:国家自然科学新药基金 ( 392 2 2 0 0 3)
摘    要:目的研究羟苯氨酮(oxyphenamone,Oxy)扩张血管作用机理。方法用全细胞膜片钳技术,监测家兔肠系膜阻力血管平滑肌细胞钙敏感钾通道电流变化以及Oxy对其的影响。结果0.1 μmol·L-1 Oxy明显增加钙敏感钾通道电流,冲洗后恢复至给药前水平;0.01~10 μmol·L-1 Oxy明显增加钙敏感钾通道电流,且呈现浓度依赖性。结论 Oxy呈浓度依赖性和可逆性的增大血管平滑肌细胞钙敏感钾通道电流。

关 键 词:羟苯氨酮  全细胞膜片钳  血管平滑肌细胞  钙敏感钾通道  钙增敏剂
收稿时间:2003-04-08

Activation of Ca2+-activated K+ channels by oxyphenamone in rabbit mesenteric vascular smooth muscle cells
LI An-long,LIU Zhong-wu,ZHU Li-xia,ZHANG De-chang,YE Yi-xin. Activation of Ca2+-activated K+ channels by oxyphenamone in rabbit mesenteric vascular smooth muscle cells[J]. Acta pharmaceutica Sinica, 2004, 39(2): 101-104
Authors:LI An-long  LIU Zhong-wu  ZHU Li-xia  ZHANG De-chang  YE Yi-xin
Affiliation:Department of Pharmacology, Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100005, China.
Abstract:AIM: To study the effects of oxyphenamone (Oxy) on activation of Ca(2+)-activated K+ channels in rabbit mesenteric vascular smooth muscle cells. METHODS: To measure the effect of Oxy on the Ca(2+)-activated K+ channel (BK (Ca) channel) activity in rabbit mesenteric vascular smooth muscle cells by using whole cell patch clamp techniques. RESULTS: Oxy reversibly increase BK (Ca) channel activity in rabbit mesenteric artery smooth muscle cells. Application of Oxy (0.1 mumol.L-1) to the perfusion solution caused significant increase in outward currents and its effect was completely abolished by washout; The outward currents K+ was inhibited by TEA (7.5 mmol.L-1); Oxy activated the BK (Ca) channel in a dose-dependent manner (0.01-10 mumol.L-1). CONCLUSION: Oxy directly increase the activity of BK (Ca) channel activity in rabbit mesenteric vascular smooth muscle cells in dose-dependent manner.
Keywords:oxyphenamone  whole cell patch clamp  vascular smooth muscle cell  Ca 2 -a ctivated K channel  calcium sensitizer
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