Design, Synthesis, and Evaluation of Indolebutylamines as a Novel Class of Selective Dopamine D3 Receptor Ligands
文献类型：期刊论文
| 作者 | Du, Peng2,3,4; Xu, Lili2,3,4; Huang, Jiye5; Yu, Kunqian5 ; Zhao, Rui1; Gao, Bo1; Jiang, Hualiang5; Zhao, Weili2,3,4; Zhen, Xuechu1; Fu, Wei2,3,4
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| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
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| 出版日期 | 2013-09 |
| 卷号 | 82期号:3页码:326-335 |
| 关键词 | dopamine 3 receptor indolebutylamine pharmacophore model selectivity structure-activity relationship |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/cbdd.12158 |
| 文献子类 | Article |
| 英文摘要 | A series of indolebutylamine derivatives were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine 3 receptor. The most potent compound 11q binds to dopamine 3 receptor with a K-i value of 124nm and displays excellent selectivity over the dopamine 1 receptor and dopamine 2 receptor. Investigation based on structural information indicates that site S182 located in extracellular loop 2 may account for high selectivity of compounds. Interaction models of the dopamine 3 receptor-11q complex and structure-activity relationships were discussed by integrating all available experimental and computational data with the eventual aim to discover potent and selective ligands to dopamine 3 receptor. |
| WOS关键词 | FUNCTIONALIZED LINKING CHAINS ; D-3 RECEPTOR ; THERAPEUTIC AGENTS ; ANTAGONISTS ; AGONISTS ; POTENT ; SUBTYPE ; BINDING ; TARGET ; SERIES |
| 资助项目 | National Natural Science Foundation of China[81172919] ; National Natural Science Foundation of China[81130023] ; National Natural Science Foundation of China[30825042] ; National High Technology Research and Development Program of China (863 Program)[2012AA020301] ; State Key Program of Basic Research of China[2009CB918502] ; State Key Program of Basic Research of China[2010CB912601] ; State Key Program of Basic Research of China[2009CB522000] ; State Key Program of Basic Research of China[2011CB5C4403] ; National Drug Innovative Program[2009ZX09301-011] ; Priority Academic Program Development of Jiangsu Higher Education Institutes (PAPD)[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000323376300010 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277489]  |
| 专题 | 药物发现与设计中心 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.Soochow Univ, Dept Pharmacol, Coll Pharmaceut Sci, Suzhou 215123, Peoples R China 2.Fudan Univ, Dept Med Chem, Minist Educ, Shanghai 201203, Peoples R China; 3.Fudan Univ, Key Lab Smart Drug Delivery, Minist Educ, Shanghai 201203, Peoples R China; 4.Fudan Univ, PLA, Sch Pharm, Shanghai 201203, Peoples R China; 5.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Du, Peng,Xu, Lili,Huang, Jiye,et al. Design, Synthesis, and Evaluation of Indolebutylamines as a Novel Class of Selective Dopamine D3 Receptor Ligands[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2013,82(3):326-335. |
| APA | Du, Peng.,Xu, Lili.,Huang, Jiye.,Yu, Kunqian.,Zhao, Rui.,...&Fu, Wei.(2013).Design, Synthesis, and Evaluation of Indolebutylamines as a Novel Class of Selective Dopamine D3 Receptor Ligands.CHEMICAL BIOLOGY & DRUG DESIGN,82(3),326-335. |
| MLA | Du, Peng,et al."Design, Synthesis, and Evaluation of Indolebutylamines as a Novel Class of Selective Dopamine D3 Receptor Ligands".CHEMICAL BIOLOGY & DRUG DESIGN 82.3(2013):326-335. |
入库方式： OAI收割
来源：上海药物研究所
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