吗啉环和哌嗪环类衍生物的抗血栓作用及其分子机制  

Antithrombotic effects of morpholine and piperazine ring derivatives and their molecular mechanism

作　　者：陈冬梅[1] 陈凯[1] 汪海[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《药学学报》2003年第9期641-645,共5页Acta Pharmaceutica Sinica

基　　金：国家重点基础研究发展规划项目 (G19980 5 112 ) ;北京赛德维康医药研究院新药研究基金项目

摘　　要：目的　研究吗啉环和哌嗪环类衍生物对血栓形成的影响及分子机制。方法　利用小鼠尾动脉血栓模型 ,观察新化合物对血栓形成的影响。结果　化合物MOPMC ,2FBMPC ,MPTMBC ,DMHPPP和PPVP在 1 0mg·kg- 1 可显著降低成栓率 ;而结构类似的化合物MAPC ,4C3FBMOC ,mTBMPC ,MONVP和MPNVP对血栓形成均无明显影响 ;化合物DMHPPP对凝血系统和血小板聚集功能无显著影响 ,但可升高血浆中t PA和PGI2 含量 ,降低PAI 1的活性和TXA2 的含量。Aim To investigate the antithrombotic effects of morpholine and piperazine ring derivatives and their mechanisms. Methods In isolated rat aorta precontracted with norepinephrine (NE), the vasodilatory effects of compounds with novel structure were investigated. Mice was given kappa carrageenin ip and kept at the temperature of (20-21)℃. Results and Conclusion Active candidate compounds including MOPMC, 2FBMPC, MPTMBC, DMHPPP and PPVP were shown to antagonize thrombosis at the dose of 1 mg·kg -1 ...

关 键 词：血管内皮细胞 乙酰胆碱 血栓 角叉菜胶 

分 类 号：R965[医药卫生—药理学]