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1篇 您的检索式:作者名="Heling Niu"
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1Design and synthesis of novel α-aminoamides derivatives as Nav1.7 inhibitors for antinociception显示文摘Three novel series of α-aminoamides derivatives were designed and synthesized based on ralfinamide,and their Nav1.7 inhibitory activities were evaluated using manual patch clamp electrophysiology. Active compounds inhibited Nav1.7 with half maximal inhibitory concentration(IC_(50)) values ranging from2.9 μmol/L to 21.4 μmol/L. Among them, the most potent compound 19h exhibited about 12-fold potency better than ralfinamide. The investigation of their structure-activity relationship gives a strategy to improve the Nav1.7 inhibition of ralfinamide analogues. Compound 19h was efficacious in antinociception in the mouse spared nerve injury(SNI) model of neuropathic pain without causing sedation in the open field test.Dengqi Xue Yani Liu Yilin Zheng Heling Niu Liying Dong Xiangshuo Ouyang Siyu Song Denggao Zhang Qianwei Ge Kewei Wang Liming Shao 2022Chinese Chemical Letters2022,33,3:0
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