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基于最近发现的长链芳基哌嗪和磺酰胺的5-HT7配体的药效团比较与开发

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

作者信息

Rague Andrea, Tidgewell Kevin

机构信息

Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, School of Pharmacy, Duquesne University, Pittsburgh, Pennsylvania, United States.

出版信息

Mini Rev Med Chem. 2018;18(7):552-560. doi: 10.2174/1389557517666170913111533.

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.

摘要

血清素系统对中枢神经系统和许多外周系统发挥作用。在14种血清素受体中,5-HT7受体是最近发现的。已证明5-HT7受体与减轻压力、抑郁症和伤害性控制有关。尽管自5-HT7R发现以来已有20年,但真正具有选择性的配体仍然很少。5-HT7R配体的两种常见骨架是长链芳基哌嗪(LCAPs)和含磺酰胺的化合物。本综述重点关注最近开发的(2014 - 2016年)5-HT7R配体、它们对该受体的选择性,并提出这些配体可能的新药理学模型。

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本文引用的文献

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