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| K-受体激动剂U-50488类似物的合成及其镇痛作用 | |
| 引用本文： | 马斯才,杨玉龙,袁小妹. K-受体激动剂U-50488类似物的合成及其镇痛作用[J]. 药学学报, 1991, 26(12): 902-905 |
| 作者姓名： | 马斯才 杨玉龙 袁小妹 |
| 作者单位： | 南京军区南京总医院药物研究所，南京军区南京总医院药物研究所，南京军区南京总医院药物研究所 南京 210002，南京 210002，南京 210002 中国人民解放军药物化学研究所，北京 102205 |
| 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。 |
| 关 键 词： | 镇痛活性 κ-受体激动剂 U-50488结构类似物 |
| 收稿时间： | 1990-12-17 |
SYNTHESIS AND ANALGESIC ACTIVITY OF ANALOGS OF U-50488, AN OPIATE KAPPA-AGONIST |
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| SC Ma,YL Yang and XM Yuan. SYNTHESIS AND ANALGESIC ACTIVITY OF ANALOGS OF U-50488, AN OPIATE KAPPA-AGONIST[J]. Acta pharmaceutica Sinica, 1991, 26(12): 902-905 | |
| Authors: | SC Ma YL Yang XM Yuan |
| Affiliation: | Institute of Materia Medical of general Hospital of Nanjing 210002 |
| Abstract: | 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. |
| Keywords: | Analgesic activity Kappa-receptor agonist Analogs of U- 50488 |
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