Rague Andrea, Tidgewell Kevin
Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, School of Pharmacy, Duquesne University, Pittsburgh, Pennsylvania, United States.
Mini Rev Med Chem. 2018;18(7):552-560. doi: 10.2174/1389557517666170913111533.
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.
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。