Vasodilatation produced by Fasudil Mesylate in vivo and in vitro
Vasodilatation produced by Fasudil Mesylate in vivo and in vitro
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DOI：
10.1016/j.vph.2011.06.005
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发表时间：
2011-11-01
影响因子：
4
通讯作者：
Guo, Lianjun
中科院分区：
文献类型：
--
作者：
Li, Qin;Chen, Yuhua;Guo, Lianjun
研究甲磺酸法舒地尔（FM）的体内外血管舒张作用。采用在体脑血管痉挛（CVS）模型和离体主动脉环模型，研究了FM的舒张作用。FM（0.35，1.2，3.5 mg.kg（-1））在体内呈剂量依赖性增加脑血管流量（CVF）和股动脉血流量（FBF），但FM对脑血管的舒张作用远强于外周血管：FM在体外对甲氧胺（Met）或KCl收缩的离体主动脉环显示剂量依赖性舒张作用。FM和Prasozin（Pra）对Met收缩的兔主动脉环的舒张IC（50）分别为27.54 μ M和0.01 μ M，FM对KCl收缩的兔和大鼠主动脉环的舒张IC（50）分别为37.15 μ M和0.74 μ M。此外，内皮完整组与内皮去除组之间无明显差异。FM（0.3，3 μ M）使Met量效关系曲线明显右移，E（max）降低（P
To investigate the vasorelaxant effect of fasudil mesylate (FM) in vivo and in vitro. The relaxation effect of FM was studied using cerebral vasospasm (CVS) model in vivo and isolated aortic rings in vitro. FM (0.35, 1.2, 3.5 mg.kg(-1)) increased cerebrovascular flow (CVF) and femoral blood flow (FBF) dose-dependently in vivo, however, the relaxation effects of FM on cerebral vessels were much stronger than on peripheral vessels: FM showed dose-dependent relaxation of isolated aortic rings contracted by Methoxamine (Met) or KCl in vitro. The relaxation IC(50) of FM and Prasozin (Pra) to the rabbit aortic rings contracted by Met are 27.54 mu M and 0.01 mu M respectively, and the relaxation IC(50) of FM to the rabbit and rat aortic rings contracted by KCl are 37.15 mu M and 0.74 mu M respectively. In addition, there is no obvious difference between endothelium-intact and endothelium-removal groups. The Met dose-effect relationship curve was significantly shifted to right by FM (0.3, 3 mu M), and E(max) was decreased (P