中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities

文献类型:期刊论文

作者Zhang, Jing1; Chen, Xuetao2; Yu, Leiping2; Zhen, Xuechu2; Zhang, Ao1
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2008-11-01
卷号16期号:21页码:9425-9431
关键词Dopamine receptor Serotonin receptor 1-Phenylbenzazepine SKF-38393 SKF-83959
ISSN号0968-0896
DOI10.1016/j.bmc.2008.09.049
文献子类Article
英文摘要A series of racemic 6-aryl substituted 1-phenylbenzazepines 7a-e, and 17a,b were prepared. All these compounds showed binding potencies compatible to or much higher than that of the prototypic (+/-)-SKF- 38393 ((+/-)-1) and (+/-)-SKF-83959 (3) for the D(1) receptor. Among analogs of (+/-)-SKF-38393, compounds 7b, 7c and 7e possess 10-, 2- and 7-fold enhancement in binding for the D(1) receptor, respectively. Lower but compatible potency to that of (+/-)-1 was observed for compounds 7a and 7d. The optimal 6-substituents (m-tolyl, and 2 '-naphthyl) were applied to the skeleton of (+/-)-SKF-83959 (3). The resulting compounds 17a, b displayed high affinity at the D(1) receptor, only slightly lower than that of (3). These two compounds also showed good binding at the D(2) receptor. (C) 2008 Elsevier Ltd. All rights reserved.
WOS关键词CROSS-COUPLING REACTIONS ; CONVENIENT SYNTHESIS ; AGONISTS ; ANALOGS ; AGENTS
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:000260134400004
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/279444]  
专题药理学第二研究室
通讯作者Zhen, Xuechu
作者单位1.Chinese Acad Sci, SOMCL, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Neuropharmacol Lab, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714
Zhang, Jing,Chen, Xuetao,Yu, Leiping,et al. Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(21):9425-9431.
APA Zhang, Jing,Chen, Xuetao,Yu, Leiping,Zhen, Xuechu,&Zhang, Ao.(2008).Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.BIOORGANIC & MEDICINAL CHEMISTRY,16(21),9425-9431.
MLA Zhang, Jing,et al."Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities".BIOORGANIC & MEDICINAL CHEMISTRY 16.21(2008):9425-9431.

入库方式: OAI收割

来源:上海药物研究所

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