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5-羟色胺 5-HT 受体配体的构效关系:综述。

Structure-activity relationships of serotonin 5-HT receptors ligands: A review.

机构信息

Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie Univ, UNICAEN, 14000, Caen, France.

Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie Univ, UNICAEN, 14000, Caen, France.

出版信息

Eur J Med Chem. 2019 Dec 1;183:111705. doi: 10.1016/j.ejmech.2019.111705. Epub 2019 Sep 16.

Abstract

5-HT receptors are the most recently discovered serotonergic receptors, for which numerous physiological implications in the central and the peripheral nervous systems as well as the endocrine system are described. A current public health challenge is to propose new and more efficient treatments against neuropsychiatric disorders such as epilepsy or Alzheimer's disease. In this context, 5-HT receptors represent an interesting target for the treatment and prevention of those pathologies, as an alternative or in association with other medicines. Thus, numerous chemical series of agonists and antagonists have been developed. Some of these molecules have shown a therapeutic potential in various in vivo studies. This review aims to present an overview of 5-HT receptors and of the medicinal chemistry programs that led to the identification of new, potent and selective 5-HT receptors ligands. Structure-activity relationships studies based on molecular docking and pharmacophoric approaches are also described.

摘要

5-HT 受体是最近发现的血清素能受体,其在中枢和外周神经系统以及内分泌系统中的许多生理作用已被描述。当前的公共卫生挑战是提出新的、更有效的治疗方法来对抗神经精神疾病,如癫痫或阿尔茨海默病。在这种情况下,5-HT 受体作为一种替代或与其他药物联合使用的方法,代表了治疗和预防这些疾病的一个有趣的靶点。因此,已经开发了许多激动剂和拮抗剂的化学系列。其中一些分子在各种体内研究中显示出了治疗潜力。这篇综述旨在介绍 5-HT 受体以及导致新的、有效和选择性 5-HT 受体配体的药物化学研究计划。还描述了基于分子对接和药效团方法的构效关系研究。

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