Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modeling Laboratory, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki St., PL-20093 Lublin, Poland.
School of Pharmacy, University of Eastern Finland, Yliopistonranta 1, P.O. Box 1627, FI-70211 Kuopio, Finland.
Int J Mol Sci. 2021 Dec 21;23(1):10. doi: 10.3390/ijms23010010.
Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT) receptor facilitated design and discovery of novel compounds with antidepressant action. Eligible papers highlighting the importance of 5-HT receptors in the pathomechanism of the disorder were identified in the content-screening performed on the popular databases (PubMed, Google Scholar). Articles were critically assessed based on their titles and abstracts. The most accurate papers were chosen to be read and presented in the manuscript. The review summarizes current knowledge on the applicability of 5-HT receptor signaling modulators in the treatment of depression. It provides an insight into the structural and physiological features of this receptor. Moreover, it presents an overview of recently conducted virtual screening campaigns aiming to identify novel, potent 5-HT receptor ligands and additional data on currently synthesized ligands acting through this protein.
抑郁症是一种多因素障碍，影响着全球数百万人，目前可用的治疗方法都无法完全治愈它。因此，需要开发新型、有效和更安全的药物。最近对 5-羟色胺 2A（5-HT）受体的结构和功能的药物化学研究结果促进了具有抗抑郁作用的新型化合物的设计和发现。在对流行数据库（PubMed、Google Scholar）进行的内容筛选中，确定了强调 5-HT 受体在该疾病发病机制中的重要性的相关论文。根据论文的标题和摘要对文章进行了批判性评估。选择最准确的论文进行阅读并呈现在手稿中。本综述总结了 5-HT 受体信号调节剂在治疗抑郁症方面的应用的最新知识。它提供了对该受体结构和生理特征的深入了解。此外，还介绍了最近进行的旨在识别新型、强效 5-HT 受体配体的虚拟筛选活动的概述，以及有关通过该蛋白起作用的当前合成配体的其他数据。
