Structure-activity relationships of inhibitor of terpenoids in GABA(A) receptor
文献类型：期刊论文
| 作者 | Ren Tian-Rui; Zhao Bao-Feng; Hu Yuan-Dong; Ci Su-Qin |
| 刊名 | CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 |
| 出版日期 | 2006-07-01 |
| 卷号 | 27期号:7页码:1262-1265 |
| 关键词 | inhibitors of terpenoids insecticide pharmacophore model GABA(A) receptor comparative molecular field analysis(CoMFA) |
| ISSN号 | 0251-0790 |
| 其他题名 | Chem. J. Chin. Univ.-Chin. |
| 中文摘要 | A variety of terpenoids of plant origin such as anisatin, picrotoxinin and picrodendrins were shown to be non-competitive antagonists of GABAA receptors. The results show the selectivity toward the insect receptor and thus represent new leads toward selective insecticides. Two pharmacophore models of rat and housefly's GABAA receptors for terpenoids inhibitors were studied by DISCOtech methodology. Two pharmacophore models were verified by the study of the three-dimensional quantitative structure and activity relationships, which gave two predictive CoMFA models with q(rat)(2)= 0.713 and q(fly)(2) = 0.738. According to these results, it was found that that negatively charged particle of inhibitor contributed strongly to binding at the rat receptor but showed almost no contribution to the housefly receptor. So these findings will lay a foundation of finding leading compounds and give some guidance on synthesizing insecticides with selectivity activity. |
| 英文摘要 | A variety of terpenoids of plant origin such as anisatin, picrotoxinin and picrodendrins were shown to be non-competitive antagonists of GABAA receptors. The results show the selectivity toward the insect receptor and thus represent new leads toward selective insecticides. Two pharmacophore models of rat and housefly's GABAA receptors for terpenoids inhibitors were studied by DISCOtech methodology. Two pharmacophore models were verified by the study of the three-dimensional quantitative structure and activity relationships, which gave two predictive CoMFA models with q(rat)(2)= 0.713 and q(fly)(2) = 0.738. According to these results, it was found that that negatively charged particle of inhibitor contributed strongly to binding at the rat receptor but showed almost no contribution to the housefly receptor. So these findings will lay a foundation of finding leading compounds and give some guidance on synthesizing insecticides with selectivity activity. |
| WOS标题词 | Science & Technology ; Physical Sciences |
| 类目[WOS] | Chemistry, Multidisciplinary |
| 研究领域[WOS] | Chemistry |
| 关键词[WOS] | SECO-PREZIZAANE |
| 收录类别 | SCI |
| 原文出处 | |
| 语种 | 英语 |
| WOS记录号 | WOS:000239259000019 |
| 公开日期 | 2013-10-24 |
| 版本 | 出版稿 |
| 源URL | [http://ir.ipe.ac.cn/handle/122111/4081]  |
| 专题 | 过程工程研究所_研究所（批量导入） |
| 作者单位 | 1.Chinese Acad Sci, Inst Proc Engn, State Key Lab Biochem Engn, Beijing 100080, Peoples R China 2.Grad Univ, Chinese Acad Sci, Beijing 100039, Peoples R China 3.Beijing Inst Pharmacol & Toxicol, Beijing 100850, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ren Tian-Rui,Zhao Bao-Feng,Hu Yuan-Dong,et al. Structure-activity relationships of inhibitor of terpenoids in GABA(A) receptor[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,2006,27(7):1262-1265. |
| APA | Ren Tian-Rui,Zhao Bao-Feng,Hu Yuan-Dong,&Ci Su-Qin.(2006).Structure-activity relationships of inhibitor of terpenoids in GABA(A) receptor.CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,27(7),1262-1265. |
| MLA | Ren Tian-Rui,et al."Structure-activity relationships of inhibitor of terpenoids in GABA(A) receptor".CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE 27.7(2006):1262-1265. |
入库方式： OAI收割
来源：过程工程研究所
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