Physicochemical and biological properties of novel amide-based steroidal inhibitors of NMDA receptors

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• 作者：Santosh Kumar Adla^a ; Barbora Slavikova^a ; Marketa Smidkova^a ; Eva Tloustova^a ; Martin Svoboda^a ; Vojtech Vyklicky^b ; Barbora Krausova^b ; Pavla Hubalkova^b ; ^d ; Michaela Nekardova^a ; ^c ; Kristina Holubova^b ; Karel Vales^b ; Milos Budesinsky^a ; Ladislav Vyklicky^b ; Hana Chodounska^a ; Eva Kudova^a ; ^{kudova@uochb.cas.cz}
• 关键词：Neurosteroid ; NMDA receptor ; Structure-activity relationship ; Amide ; Blood-brain-barrier permeability ; Caco-2 assay
• 刊名：Steroids
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：117
• 期：Complete
• 页码：52-61
• 全文大小：975 K
• 卷排序：117

文摘

Synthesis of new amide-based inhibitors of NMDA receptors. Strong inhibitors of NMDA currents. The Caco-2 assay was used to evaluate permeability of new compounds. Compounds with minimal or no adverse hepatic effect. Amide-based inhibitors of NMDA receptors are able to cross blood-brain-barrier.