Synthesis and opioid receptor activity of indolopropellanes
文献类型：期刊论文
| 作者 | Li, Fuying3; Gaob, Linghuan2; Yin, Chenlei2; Chen, Jie1; Liu, Jinggen1 ; Xie, Xin2; Zhang, Ao3
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2009-08-15 |
| 卷号 | 19期号:16页码:4603-4606 |
| 关键词 | Opioid receptor Indolopropellane Structure-activity relationship Morphinans |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2009.06.093 |
| 文献子类 | Article |
| 英文摘要 | A series of skeletal rearranged indolomorphinans 7a-d were obtained by N-demethylation of 3-methoxy-N-methyl-14-hydroxymorphinan-6-one 12 followed by N-realkylation, reduction and Fischer indole cyclization. The structure of the novel skeleton was confirmed by X-ray analysis. These new indoles displayed moderate binding affinity and selectivity at the mu receptor, with compound 7b showing the highest affinity at this receptor with a K-i value of 40 nM, and 6-and 25-fold selectivity against delta and kappa receptors, respectively. Function assays showed that indolopropellanes 7b and 7c possessed full agonistic activity at all the opioid receptors indicating a different interaction model existed. (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MU-AGONIST/DELTA ANTAGONIST ; 4-HYDROXYL GROUP ; BIOLOGICAL EVALUATION ; MORPHINE ; ELIMINATION ; DERIVATIVES ; NALTRINDOLE ; LIGANDS ; ANALOGS ; SELECTIVITY |
| 资助项目 | Hundred Talent Project of the Chinese Academy of Sciences[00000000] ; Chinese National Science Foundation[30772625] ; Shanghai Commission of Science and Technology[07pj14104] ; Shanghai Institute of Materia Medica[SIMM0809KF-02] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000268358800016 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279156]  |
| 专题 | 药理学第二研究室 药物化学研究室 国家新药筛选中心 |
| 通讯作者 | Liu, Jinggen |
| 作者单位 | 1.Chinese Acad Sci, Neuropharmacol Lab, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Synthet Organ & Med Chem Lab, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Fuying,Gaob, Linghuan,Yin, Chenlei,et al. Synthesis and opioid receptor activity of indolopropellanes[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(16):4603-4606. |
| APA | Li, Fuying.,Gaob, Linghuan.,Yin, Chenlei.,Chen, Jie.,Liu, Jinggen.,...&Zhang, Ao.(2009).Synthesis and opioid receptor activity of indolopropellanes.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(16),4603-4606. |
| MLA | Li, Fuying,et al."Synthesis and opioid receptor activity of indolopropellanes".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.16(2009):4603-4606. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。