Discovery of a Novel Dopamine D-3 Receptor Inhibitor
文献类型：期刊论文
| 作者 | Deng Xin-Xian1,2; Shen Qing1,2; Xu Li-Li1,2; Xiong Zi-Jun1,2; Zhao Wei-Li1,2; Zhen Xue-Chu3; Fu Wei1,2 |
| 刊名 | CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 |
| 出版日期 | 2011-08-10 |
| 卷号 | 32期号:8页码:1779-1784 |
| 关键词 | Dopamine D-3 receptor Pharmacophore model Database screening Inhibitor |
| ISSN号 | 0251-0790 |
| 文献子类 | Article |
| 英文摘要 | Dopamine D-3 receptor regulates the synthesis and release of dopamine in brain. It is implicated in many neurological processes, including motivation, pleasure, cognition, memory, learning, and fine motor control. It is involved in the pathology of psychotic diseases, such as schizophrenia, Parkinson's disease and drug addiction. It is of great significance to discover novel D-3 inhibitors through pharmacophore-based virtual screening for the development of anti-psychotic drugs. In this study, we employed the latest discovered high-resolution crystal. structure of human D-3 receptor to conduct active-site-analysis, build the receptor-based pharmacophore model and screen the Asinex GOLD Collection database. 7 hits were purchased and tested by pharmacological experiments. A novel inhibitor 04932482 with a high activity against D-3 receptor was obtained [K-i = (806.75 +/- 34.58) nmol/L]. The structure analysis was conducted and the ligand-receptor interaction was further investigated by docking to guide the structure modification and optimization of compound 04932482. |
| WOS关键词 | MECHANISMS ; SCHIZOPHRENIA ; ANTAGONISTS ; MODEL |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:4304121 |
| WOS记录号 | WOS:000294578000024 |
| 出版者 | HIGHER EDUCATION PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278444]  |
| 专题 | 药理学第二研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Fu Wei |
| 作者单位 | 1.Fudan Univ, Minist Educ, Dept Med Chem, Key Lab Smart Drug Delivery,Sch Pharm, Shanghai 201203, Peoples R China; 2.Fudan Univ, PLA, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Deng Xin-Xian,Shen Qing,Xu Li-Li,et al. Discovery of a Novel Dopamine D-3 Receptor Inhibitor[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,2011,32(8):1779-1784. |
| APA | Deng Xin-Xian.,Shen Qing.,Xu Li-Li.,Xiong Zi-Jun.,Zhao Wei-Li.,...&Fu Wei.(2011).Discovery of a Novel Dopamine D-3 Receptor Inhibitor.CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,32(8),1779-1784. |
| MLA | Deng Xin-Xian,et al."Discovery of a Novel Dopamine D-3 Receptor Inhibitor".CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE 32.8(2011):1779-1784. |
入库方式： OAI收割
来源：上海药物研究所
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