钙增敏剂MCI-154抗休克作用及其机制  

The antishock effects and its mechanism of a calcium sensitizer--MCI-154

作　　者：胡德耀[1] 梅建民[1] 江其生[1] 殷作明[1] 刘良明[1] 

机构地区：[1]第三军医大学大坪医院野战外科研究所,重庆400042

出　　处：《中国新药杂志》2004年第1期23-27,共5页Chinese Journal of New Drugs

基　　金：中国人民解放军"九五"指令性课题(96L041)

摘　　要：钙增敏剂MCI-154有明显的拮抗失血性休克及内毒素休克的作用,特别是对休克失代偿期有良好的疗效。与传统的加强心肌收缩的药物不同,本品不会明显增加休克动物心肌细胞内的钙超载,而主要通过增加心肌收缩蛋白对Ca2+的敏感性而改善休克动物的心功能,其增加心肌细胞内Ca2+水平及cAMP含量的作用明显比米力农弱。本品降低休克动物血管平滑肌细胞内游离Ca2+浓度,恢复钙调蛋白活性及c蛋白激酶C的表达,以及相对增加Calponin-α的表达,从而改善休克舒张功能。MCI-154,a calcium sensitizer,was found to have obviously beneficial effect for endo-toxic and hemorrhagic shock, especially for the decompensatory period of shock. The superiority of MCI-154 to traditional positive inotropic agents is that it did not increase the cellular calcium overload of shocked animal. MCI-154 improved the cardiac function of shocked animal mainly by increasing the sensitivity of cardiac contractile protein to calcium. However, the effects of MCI-154 increasing [Ca2+]i and cAMP in myocardial cell was much weaker than that of milrinone. MCI-154 could improve the constriction and dilation function of blood vessels by decreasing cytoplasmic free calcium concentration of vascular smooth muscle cell (VSMC) ,and restoring the activity of Calmodulin and the ex- pression of c protein kinase C. Meanwhile MCI-154 could dilate blood vessel by enhancing the expression of calponin-2 in VSMC.

关 键 词：钙增敏剂 MCI-154 休克 钙超载 

分 类 号：R972[医药卫生—药品]