The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT_1A receptor over α₁-adrenoceptor and D₂-like receptor subtypes

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• 作者：Fabio Del Bello^a ; ¹ ; Alessandro Bonifazi^a ; ^b ; ¹ ; Mario Giannella^a ; Gianfabio Giorgioni^a ; Alessandro Piergentili^a ; Riccardo Petrelli^a ; Carlo Cifani^a ; Maria Vittoria Micioni Di Bonaventura^a ; Thomas M. Keck^b ; ^c ; ^d ; Angelica Mazzolari^e ; Giulio Vistoli^e ; Antonio Cilia^f ; Elena Poggesi^f ; Rosanna Matucci^g ; Wilma Quaglia^a ; ^{wilma.quaglia@unicam.it}
• 关键词：5-HT1A receptor ; α1-Adrenoceptor subtypes ; D2-like receptor subtypes ; Selective 5-HT1A receptor agonists ; Docking studies ; Anxiolytic effect
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：233-244
• 全文大小：1640 K
• 卷排序：125

文摘

A potent 5-HT1A agonist selective over α1-ARs and D2-like receptors is discovered. It significantly reduces anxiety-linked behaviors in the light/dark paradigm. Docking analysis supports the structure-activity relationship studies. Correlative studies involves the generation of reliable predictive models.