中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
Continuation of structure-activity relationship study of novel benzamide derivatives as potential antipsychotics

文献类型：期刊论文

作者Xu, Mingshuo1,3; Guo, Shuang1,3; Yang, Feipu3; Wang, Yu3; Wu, Chunhui2; Jiang, Xiangrui3; Zhao, Qingjie3; Chen, Weiming2; Tian, Guanghui2; Zhu, Fuqiang2
刊名ARCHIV DER PHARMAZIE
出版日期2019-04-01
卷号352期号:4页码:13
关键词5-HT1A 5-HT2A catalepsy D-2 PCP-induced hyperactivity
ISSN号0365-6233
DOI10.1002/ardp.201800306
通讯作者Wang, Zhen(wangzhen@simm.ac.cn) ; He, Yang(heyang@simm.ac.cn)
英文摘要A series of benzamide derivatives possessing potent dopamine D-2, serotonin 5-HT1A, and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. Among them, 5-(4-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)butoxy)-N-cyclopropyl-2-fluorobenzamide (4k) held the best pharmacological profile. It not only exhibited potent and balanced activities for the D-2, 5-HT1A, and 5-HT2A receptors, but was also endowed with low to moderate activities for the 5-HT2C, H-1, and M-3 receptors, suggesting a low propensity for inducing weight gain or diabetes. In animal models, compound 4k reduced phencyclidine-induced hyperactivity with a high threshold for catalepsy or muscle relaxation induction. On the basis of its robust in vitro potency and in vivo efficacy in preclinical models of schizophrenia, 4k was selected as a candidate for further development.
WOS关键词SEROTONIN 5-HT1A RECEPTORS ; BIOLOGICAL EVALUATION ; SCHIZOPHRENIA ; SERIES ; DEPRESSION ; DRUGS ; RISK
资助项目Special Foundation of Chinese Academy of Sciences[XDA12040105] ; National Science Foundation for Young Scientists of China[81703338]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000462879700001
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/290197]  
专题中国科学院上海药物研究所
通讯作者Wang, Zhen; He, Yang
作者单位1.Chinese Acad Sci, Shanghai Inst Materia Med, CAS Key Lab Receptor Res, Shanghai, Peoples R China
2.Topharman Shanghai Co Ltd, Shanghai, Peoples R China
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Xu, Mingshuo,Guo, Shuang,Yang, Feipu,et al. Continuation of structure-activity relationship study of novel benzamide derivatives as potential antipsychotics[J]. ARCHIV DER PHARMAZIE,2019,352(4):13.
APA Xu, Mingshuo.,Guo, Shuang.,Yang, Feipu.,Wang, Yu.,Wu, Chunhui.,...&Shen, Jingshan.(2019).Continuation of structure-activity relationship study of novel benzamide derivatives as potential antipsychotics.ARCHIV DER PHARMAZIE,352(4),13.
MLA Xu, Mingshuo,et al."Continuation of structure-activity relationship study of novel benzamide derivatives as potential antipsychotics".ARCHIV DER PHARMAZIE 352.4(2019):13.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。