Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics
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- 作者：Xiao-Wen Chena ; b ; Yuan-Yuan Suna ; Lei Fua ; leifu@sjtu.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Jian-Qi Lib ; lijianqb@126.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Dopamine ; Serotonin ; Multireceptor ; X-ray crystallography ; Atypical antipsychotic
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 November 2016
- 年：2016
- 卷：123
- 期：Complete
- 页码：332-353
- 全文大小：2085 K
文摘
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A series of benzisothiazolylpiperazine derivatives were synthesized.
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Target compounds were evaluated affinities for D2, D3, 5-HT1A and 5-HT2A receptors.
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The proming compound 9j had low affinities for M1 receptors and hERG channels.
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9j showed in vivo activities in animal models with low potential for catalepsy.
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9j displayed favorable brain penetration.