【摘要】 目的 为了了解抗脑缺血新化合物SIPI5052是否具有钙拮抗作用，本研究观察它对去甲肾上腺素或高钾诱导的离体血管收缩功能的影响。方法 采用计算机化离体血管功能测定系统观察SIPI5052对离体大鼠胸主动脉、家兔胸主动脉和肠系膜动脉收缩功能的影响。结果 SIPI5052可明显抑制受试血管去甲肾上腺素或高钾诱导的收缩反应，呈剂量依赖性。在大鼠血管上，起效浓度为3×10-6mol/L，IC50为1.66×10-4mol/L，100%抑制浓度为3×10-3mol/L。在家兔血管上，起效浓度为3×10-4mol/L，IC50为4.17×10-4～5.37×10-4mol/L，100%抑制浓度≥3×10-3mol/L。结论 SIPI5052具有钙拮抗作用。大鼠血管对SIPI5052的反应较家兔血管敏感。钙拮抗作用很可能是SIPI5052的抗脑缺血作用机制之一。

    【关键词】 哌嗪类；主动脉；肠系膜动脉；收缩反应；钙通道；抗脑缺血

    Effect of SIPI5052, a new chemical entity, on the contraction of isolated arteries

    XU Tian-ying, MIAO Chao-yu.Second Military Medical University, Shanghai 200433, China

    【Abstract】 Objective To study the effect of a new anti-stroke chemical entity SIPI5052 on Ca2+ channels, by observing its effect on norepinephrine or KCl induced contraction in isolated blood vessels.Methods Using IOX computerized system (EMKA Technologies, Paris, France) to record the changes of isometric tension in isolated rat aorta, rabbit aorta and rabbit mesenteric artery.Results SIPI5052 can significantly inhibit norepinephrine or KCl induced contraction in the examined blood vessels and the effect is concentration-dependent. The minimum inhibitory concentration in rat aorta is 3×10-6mol/L, with the IC50value of 1.66×10-4mol/L. The minimum inhibitory concentration in rabbit aorta and mesenteric artery is 3×10-4mol/L, and the IC50value is between 4.17×10-4 and 5.37×10-4mol/L.Conclusion SIPI5052 can block Ca2+ channels. Rat isolated blood vessels are more sensitive to SIPI5052 than rabbit isolated blood vessels. Ca2+ channel blocking may be involved in the anti-stroke action of SIPI5052. ......