Further SAR study on 11-O-substituted aporphine analogues: Identification of highly potent dopamine D-3 receptor ligands
文献类型：期刊论文
| 作者 | Ye, Na2; Wu, QianQian1; Zhu, Liyuan1; Zheng, Longtai3; Gao, Bo3; Zhen, Xuechu1,3; Zhang, Ao2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2011-03-15 |
| 卷号 | 19期号:6页码:1999-2008 |
| 关键词 | Aporphine analogues Dopamine D-3 receptor 5-HT1A receptor Arylpiperazine Click reaction |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2011.01.053 |
| 文献子类 | Article |
| 英文摘要 | A series of new aporphine analogues (aporlogues) were prepared from appropriate aporphine precursors and arylpiperazines using the Click reaction protocol. These compounds displayed good to high affinity at the D-3 receptor, low or no affinity at the D-1 and D-2 receptors. Compounds 7f and 11c stood out as the most potent at the D-3 receptor among our newly synthesized aporlogues with K-i values of 2.67 and 1.14 nM, respectively. Further assay at the 5-HT1A receptor revealed that aporlogues 7f and 11c also showed high affinity at this receptor with K-i values of 9.68 and 7.59 nM, respectively. They were 3.6- and 6.6-fold more potent at the D-3 over 5-HT1A receptors. Such D-3/5-HT1A dual property of these compounds may be useful in the treatment of several brain disorders. (C) 2011 Elsevier Ltd. All rights reserved. |
| WOS关键词 | D3 RECEPTOR ; PARKINSONS-DISEASE ; 5-HT1A AGONIST ; SEROTONIN ; ANTAGONISTS ; THERAPY ; TARGET ; RATS ; COMPLICATIONS ; THERAPEUTICS |
| 资助项目 | Chinese National Science Foundation[81072528] ; Chinese National Science Foundation[30772625] ; Chinese National Science Foundation[30825042] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program'[2009ZX09301-001] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program'[2009ZX09103-062] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program'[2009ZX09102-023] ; Shanghai Commission of Science and Technology[10410702600] ; Shanghai Commission of Science and Technology[10JC1417100] ; Shanghai Commission of Science and Technology[10dz1910104] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000288196900017 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278582]  |
| 专题 | 药物化学研究室 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 药理学第二研究室 |
| 通讯作者 | Zhen, Xuechu |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, SOMCL, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Soochow Univ Pharmaceut Sci, Dept Pharmacol, Suzhou, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ye, Na,Wu, QianQian,Zhu, Liyuan,et al. Further SAR study on 11-O-substituted aporphine analogues: Identification of highly potent dopamine D-3 receptor ligands[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(6):1999-2008. |
| APA | Ye, Na.,Wu, QianQian.,Zhu, Liyuan.,Zheng, Longtai.,Gao, Bo.,...&Zhang, Ao.(2011).Further SAR study on 11-O-substituted aporphine analogues: Identification of highly potent dopamine D-3 receptor ligands.BIOORGANIC & MEDICINAL CHEMISTRY,19(6),1999-2008. |
| MLA | Ye, Na,et al."Further SAR study on 11-O-substituted aporphine analogues: Identification of highly potent dopamine D-3 receptor ligands".BIOORGANIC & MEDICINAL CHEMISTRY 19.6(2011):1999-2008. |
入库方式： OAI收割
来源：上海药物研究所
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