| Literature DB >> 29395980 |
Mingshuo Xu1, Yu Wang2, Feipu Yang2, Chunhui Wu3, Zhen Wang2, Bin Ye3, Xiangrui Jiang2, Qingjie Zhao2, Jianfeng Li2, Yongjian Liu3, Junchi Zhang2, Guanghui Tian3, Yang He4, Jingshan Shen5, Hualiang Jiang2.
Abstract
In previous study, a series of benzamides was identified as potent antipsychotic agents. As a continuation of the program to discover novel antipsychotics, herein we reported the evaluation of a series of pyridinecarboxamide derivatives. The most promising compound 7h not only held good activities on dopamine D2, serotonin 5-HT1A and 5-HT2A receptors, but also exhibited low potency for α1A, H1 and 5-HT2C receptors, indicating a low propensity of side effects like orthostatic hypotension and weight gain. Furthermore, 7h exhibited more potent antipsychotic-like effect than aripiprazole in behavioral studies. The preliminary results were promising enough for further research around this scaffold.Entities:
Keywords: 5-HT(1A) receptor; Antipsychotic; Multi-receptor; PCP-induced hyperlocomotion; Pyridinecarboxamide
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Year: 2018 PMID: 29395980 DOI: 10.1016/j.bmcl.2018.01.038
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823