N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands
文献类型：期刊论文
| 作者 | Liu, Zhili2; Chen, Xuetao1; Sun, Peihua1; Yu, Leiping1; Zhen, Xuechu1; Zhang, Ao2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2008-09-15 |
| 卷号 | 16期号:18页码:8335-8338 |
| 关键词 | apomorphine aporphine analog dopamine receptor serotonin receptor monoester |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2008.08.056 |
| 文献子类 | Article |
| 英文摘要 | A small series of N-propylnoraporphin-11-O-yl carboxylic esters with variant ester lengths were synthesized and their binding potencies at dopamine receptors (D(1), D(2)) and serotonin receptors (5-HT(1A), 5HT(2A)) were evaluated. Monoesters 3a-f showed binding potency of 100 nM or less for the D(2) receptor, and potency of 10 -30 nM for the 5-HT(1A) receptor. Butyryl ester 3d was found to be the best compound possessing the highest potency for both receptors, with K(i) values of 55 and 12 nM for D(2) and 5-HT(1A) receptors, respectively. There is no correlation between the binding potency and the length of the monoesters, but the diesters 9 and 10 were inactive for the D(2) receptor. The dual binding profile of these monoesters for the D(2) and 5-HT(1A) receptors may be useful for the treatment of neuropsychiatric disorders. (C) 2008 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PHARMACOLOGY ; APOMORPHINE ; AGONIST |
| 资助项目 | Chinese National Science Foundation[30672517] ; Shanghai Commission of Science and Technology[07pj14104] ; Ministry of Science and Technology[2007AA022163] ; Chinese Academy of Sciences[00000000] ; Shanghai Institute of Materia Medica[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000259173400002 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272809]  |
| 专题 | 药理学第二研究室 药物化学研究室 |
| 通讯作者 | Zhen, Xuechu |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Neuropharmacol Lab, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, SOMCL, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Zhili,Chen, Xuetao,Sun, Peihua,et al. N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(18):8335-8338. |
| APA | Liu, Zhili,Chen, Xuetao,Sun, Peihua,Yu, Leiping,Zhen, Xuechu,&Zhang, Ao.(2008).N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands.BIOORGANIC & MEDICINAL CHEMISTRY,16(18),8335-8338. |
| MLA | Liu, Zhili,et al."N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands".BIOORGANIC & MEDICINAL CHEMISTRY 16.18(2008):8335-8338. |
入库方式： OAI收割
来源：上海药物研究所
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