SIPI5047的合成及非阿片类中枢镇痛活性研究  

Synthesis and central none-opioid analgesic activity of SIPI5047

作　　者：李建其[1] 黄丽瑛[1] 陈新建[2] 翁志洁[1] 张椿年[1] 

机构地区：[1]上海医药工业研究院,上海200040 [2]中国科学院上海药物研究所,上海201203

出　　处：《药学学报》2008年第6期611-618,共8页Acta Pharmaceutica Sinica

基　　金：国家重点科技攻关计划专题(96-901-01-68)

摘　　要：为研究芳烷酮哌嗪类新化合物SIPI5047的非阿片类中枢镇痛活性,以哌嗪为起始原料经5步反应合成SIPI5047,通过多种动物模型研究SIPI5047的体内镇痛活性、作用机制、作用类型及药物成瘾性。研究表明:SIPI5047具有明显镇痛活性,其镇痛强度与吗啡相当,远强于目前临床广泛应用的镇痛药对乙酰氨基酚。SIPI5047不具有解热和抗炎作用,但有明显的中枢抑制作用。SIPI5047与μ阿片受体无明显亲和力,对NMDA受体多胺位点具有较强的抑制作用。SIPI5047多次用药不产生身体与精神依赖作用。SIPI5047是一种作用于中枢的新型非阿片类镇痛剂,具有作为非成瘾性镇痛新药深入研究开发的价值。Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paraeetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the w-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate.

关 键 词：SIPI5047 合成 非阿片类中枢镇痛剂 

分 类 号：R916.2[医药卫生—药学]