摘要
本文报道了某些к-型阿片受体激动剂U-50488结构类似物的合成。在小白鼠热板试验和扭体试验的结果表明,反式环己二胺结构中2位氨基为五元环吡咯啉基时对к-活性有重要作用。以六元环氯基(哌啶基、哌嗪基,吗啉基)取代2位五元环氯基导致,к-活性降低。另外,也探讨了1位芳酰氨基结构改变对к-活性的影响。
In this paper, we report the synthesis and analgesic activities in mouse hot plate test and writhing test of some analogs of U- 50488, a κ-agonist. Results showed that compounds in which the amino group was pyrrolinyl had higher κ-agonist activity and the substitution of two chlorine atoms in 3 and 4-positions of the benzene nucleus was very important to κ-activity. Furthermore, all of compounds in which the amino group was piperidyl, piperazinyl or morpholinyl exhibited very weak κ-agonist activity.
出处
《药学学报》
CAS
CSCD
北大核心
1991年第12期902-905,共4页
Acta Pharmaceutica Sinica
关键词
镇痛活性
K-受体激动剂
合成
Analgesic activity
Kappa-receptor agonist
Analogs of U- 50488
