Pharmacophore Comparison and Development of Recently Discovered Long Chain Arylpiperazine and Sulfonamide Based 5-HT7 Ligands

Author(s): Andrea Rague, Kevin Tidgewell*

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 18 , Issue 7 , 2018

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Graphical Abstract:


The serotonin system exerts its effects on the CNS and many peripheral systems. Of the 14 serotonin receptors, the 5-HT7 receptor is the most recently discovered. The 5-HT7 receptor has been shown to be involved in stress reduction, depression, and nociceptive control. Despite the 20 years since the discovery of 5-HT7R, there are still few truly selective ligands. Two of the common scaffolds for 5-HT7R ligands are long chain arylpiperazines (LCAPs) and sulfonamide containing compounds. This review focuses on recently developed (2014-2016) 5-HT7R ligands, their selectivity for the receptor, and suggests the possible new pharmacophore models for these ligands.

Keywords: Arylpiperazine, CNS, drug design, 5-HT7, pharmacophore, serotonin.

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Article Details

Year: 2018
Published on: 13 September, 2017
Page: [552 - 560]
Pages: 9
DOI: 10.2174/1389557517666170913111533
Price: $65

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