甲磺酸法舒地尔在体内和体外产生的血管扩张作用。

Vasodilatation produced by fasudil mesylate in vivo and in vitro.

机构信息

Department of Pharmacology, Tongji Medical College of Huazhong University of Science and Technology, Wuhan, China.

出版信息

Vascul Pharmacol. 2011 Nov-Dec;55(5-6):121-6. doi: 10.1016/j.vph.2011.06.005. Epub 2011 Jul 6.

DOI:10.1016/j.vph.2011.06.005

Abstract

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 IC₅₀ of FM and Prasozin (Pra) to the rabbit aortic rings contracted by Met are 27.54 μM and 0.01 μM respectively, and the relaxation IC₅₀ of FM to the rabbit and rat aortic rings contracted by KCl are 37.15 μM and 0.74 μM 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 μM), and E(max) was decreased (P<0.05). The relaxation effect of FM on cerebral vessels was much stronger than on peripheral vessels in vivo, and the action is in an endothelium-independent manner.

摘要

目的

研究甲磺酸法舒地尔（FM）的体内和体外血管舒张作用。

方法

采用体内脑血管痉挛（CVS）模型和体外分离的主动脉环研究 FM 的舒张作用。FM（0.35、1.2、3.5 mg·kg⁻¹）体内给药剂量依赖性增加脑血管血流量（CVF）和股血流量（FBF），但 FM 对脑血管的舒张作用明显强于对外周血管的舒张作用；FM 体外对甲氧基肾上腺素（Met）或氯化钾（KCl）收缩的主动脉环呈剂量依赖性舒张。FM 和 Prazozin（Pra）对 Met 收缩的兔主动脉环的舒张 IC₅₀分别为 27.54 μM 和 0.01 μM，FM 对 KCl 收缩的兔和大鼠主动脉环的舒张 IC₅₀分别为 37.15 μM 和 0.74 μM。此外，内皮完整组和去内皮组之间无明显差异。FM（0.3、3 μM）使 Met 剂量-效应关系曲线明显右移，E（max）降低（P<0.05）。FM 对脑血管的舒张作用明显强于体内的外周血管，作用呈非内皮依赖性。