化药新药研发其他>方法开发检测 | 通过Biotage微波合成仪以新型的吡咯氨基酸为基础进行羟色胺5-HT2A，5-HT2C以及羟色胺转运蛋白的合成优化by耐士科技-上海鑫欣生物科技有限公司

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应用领域	制药/生物制药
检测样本	化药新药研发
检测项目	其他>方法开发
参考标准	GB/T 8****

In the continuing search for novel compounds targeting serotonin 5-HT2A, 5-HT2C, and serotonin transporter, new arylpiperazine-containing pyrrole 3 carboxamide derivatives were synthesized and evaluated. Based on the lead reported previously, structural modifications regarding N-(3-(4-(2,3-dichlorophenyl) piperazin-1-yl)propyl)-1,2-dimethyl-5-phenyl-1H-pyrrole-3 carboxamide 5, were accomplished for improvements in not only binding affinity against serotonin receptors and transporter, but also in hERG channel inhibition. Along the line, both the forced swimming tests and spontaneous locomotor activity tests were performed to distinguish between antidepressant activity and false positive results. As potential antidepressant agents, both 2,4-dimethyl-5-phenyl-1H-pyrrole-3-carboxamide and 5-tert-butyl-2-methyl-1H-pyrrole-3-carboxamide derivatives exhibited favorable in vitro and in vivo activities, warranting further investigation around these scaffolds.

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上一篇耐士科技：使用Biotage Isolera快速纯化液相制备色谱从库拉索芦荟叶皮提取天然的磷酸二酯酶抑制剂by耐士科技

下一篇 Synthesis and electro-polymerisation of a novel heteropentalene mesomeric betaine preparation of a novel low band-gap conjugated polymer by Biotage Initiator耐士科技

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上海鑫欣生物科技有限公司

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