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Structural manipulation on the catecholic fragment of dopamine D-1 receptor agonist 1-phenyl-N-methyl-benzazepines

文献类型：期刊论文

作者Zhang, Jing1,4; Huang, Jiye3; Song, Zilan1,4; Guo, Lin2; Cai, Wenxian3; Wang, Yun2; Zhen, Xuechu2,3; Zhang, Ao1,4
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2014-10-06
卷号85页码:16-26
关键词Arylbenzazepine Dopamine receptor Serotonin 5-HT2A receptor Structural modification Catecholic fragment
ISSN号0223-5234
DOI10.1016/j.ejmech.2014.07.059
文献子类Article
英文摘要A series of new benzazepines with modification on the catecholic fragment were designed. The 8-hydroxyl group, other than the 7-hydroxyl was confirmed crucial to the interaction with the dopamine D-1 receptor. Subsequent replacement of the 7-hydroxyl with benzylamino groups was found tolerable. 7-(m-Chlorophenyl)methylamino- and 7-(m- or o-tolyl)methylamino-substituted benzazepines 13b-d displayed K-i values of 270-370 nM at the D-1 receptor, which were slightly more potent than that of parent compound I. In addition, 7-(arylmethyl)amino-benzazepines 13a-c were found possessing high binding affinities less than 10 nM at the 5-HT2A receptor. Among them, the non-substituted 7-benzylamino analogue 13a was the most potent showing a K-i values of 4.5 nM at the 5-HT2A receptor and a 5-HT2A/D-1 selectivity of 147. (C) 2014 Elsevier Masson SAS. All rights reserved.
WOS关键词POTENT ; IDENTIFICATION ; DERIVATIVES ; ANTAGONISTS ; INHIBITORS ; AGENTS ; MOUSE
资助项目Chinese National Sciences Foundation[81125021] ; Chinese National Sciences Foundation[81373277] ; Chinese National Sciences Foundation[81130023] ; Chinese National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program'[2012ZX09103-101-035] ; Chinese National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program'[2012ZX09301001-001] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2009CB522000] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2011CB5C4403] ; "Interdisciplinary Cooperation Team" Program for Science and Technology Innovation (CAS)[00000000] ; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica[SIMM1302KF-08]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000342859700002
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/276871]  
专题药理学第二研究室
药物化学研究室
通讯作者Zhang, Ao
作者单位1.Chinese Acad Sci, Synthet Organ & Med Chem Lab, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.Soochow Univ, Dept Pharmacol, Coll Pharmaceut Sci, Suzhou 215123, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Pharmacol, Shanghai, Peoples R China;
4.Chinese Acad Sci, CAS Key Lab Receptor Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Zhang, Jing,Huang, Jiye,Song, Zilan,et al. Structural manipulation on the catecholic fragment of dopamine D-1 receptor agonist 1-phenyl-N-methyl-benzazepines[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,85:16-26.
APA Zhang, Jing.,Huang, Jiye.,Song, Zilan.,Guo, Lin.,Cai, Wenxian.,...&Zhang, Ao.(2014).Structural manipulation on the catecholic fragment of dopamine D-1 receptor agonist 1-phenyl-N-methyl-benzazepines.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,85,16-26.
MLA Zhang, Jing,et al."Structural manipulation on the catecholic fragment of dopamine D-1 receptor agonist 1-phenyl-N-methyl-benzazepines".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 85(2014):16-26.

入库方式： OAI收割

来源：上海药物研究所

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