Investigations on the 1-(2-Biphenyl)piperazine Motif: Identification of New Potent and Selective Ligands for the Serotonin7 (5-HT7) Receptor with Agonist or Antagonist Action in

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• 作者：Enza Lacivita ; Daniela Patarnello ; Nikolas Stroth ; Antonia Caroli ; Mauro Niso ; Marialessandra Contino ; Paola De Giorgio ; Pantaleo Di Pilato ; Nicola A. Colabufo ; Francesco Berardi ; Roberto Perrone ; Per Svenningsson ; Peter B. Hedlund ; Marcello Leopoldo
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：July 26, 2012
• 年：2012
• 卷：55
• 期：14
• 页码：6375-6380
• 全文大小：332K
• 年卷期：v.55,no.14(July 26, 2012)
• ISSN：1520-4804

文摘

Here we report the design, synthesis, and 5-HT₇ receptor affinity of a set of 1-(3-biphenyl)- and 1-(2-biphenyl)piperazines. The effect on 5-HT₇ affinity of various substituents on the second (distal) phenyl ring was analyzed. Several compounds showed 5-HT₇ affinities in the nanomolar range and >100-fold selectivity over 5-HT_1A and adrenergic 伪₁ receptors. 1-[2-(4-Methoxyphenyl)phenyl]piperazine (9a) showed 5-HT₇ agonist properties in a guinea pig ileum assay but blocked 5-HT-mediated cAMP accumulation in 5-HT₇-expressing HeLa cells.