中国药理学通报2018，Vol.34Issue(3)：382-387,6.DOI:10.3969/j.issn.1001-1978.2018.03.017
新型AMPA受体正向变构调节剂抗疲劳活性筛选
Anti-fatigue activity screening of novel positive allosteric modulators on AMPA receptor
摘要
Abstract
Aim To explore the novel anti-fatigue a-gents targeting AMPA receptor. Methods Three ben-zoic acids of different methoxy substitutions were em-ployed, including piperonylic acid, 3,4,5-trimethoxy benzoic acid and 3,4-dimethoxy benzoic acid, which as mother nucleus and cyclic aliphatic amine or pheny-lpiperazine derivatives were introduced to modify the nitrogen atoms connecting to amino bonds. Forty-three compounds were synthesized and identified by 1 H-NMR. MTT assay, then pentobarbital induced hypno-sis experiment and mice burden swimming experiment were applied respectively to evaluate the new synthesized compounds’ cytotoxicity, CNS excitability and anti-fatigue activity. Results Compound 2j had low cytotoxicity,presenting certain central excitability and significant advantages on anti-fatigue. Conclusion The further development of compounds 2j with good anti-fatigue activities could be cultivated in further study.关键词
AMPA受体/苯甲酰胺类/细胞毒性/中枢兴奋性/负重游泳/抗疲劳Key words
AMPA receptor/benzamide/cytotoxicity/central excitability/burden swimming experiment/an-ti-fatigue分类
医药卫生引用本文复制引用
陈瑶,马淑梅,梅其炳,刘莉..新型AMPA受体正向变构调节剂抗疲劳活性筛选[J].中国药理学通报,2018,34(3):382-387,6.基金项目
上海市生物物质成药性评价专业技术服务平台(No 15DZ2291700) （No 15DZ2291700）
