Villas-Boas Gustavo R, Lavorato Stefânia N, Paes Marina M, de Carvalho Pablinny M G, Rescia Vanessa C, Cunha Mila S, de Magalhães-Filho Manoel F, Ponsoni Luis F, de Carvalho Adryano Augustto Valladao, de Lacerda Roseli B, da S Leite Lais, da S Tavares-Henriques Matheus, Lopes Luiz A F, Oliveira Luiz G R, Silva-Filho Saulo E, da Silveira Ana P S, Cuman Roberto K N, de S Silva-Comar Francielli M, Comar Jurandir F, do A Brasileiro Luana, Dos Santos Jussileide N, de Freitas William R, Leão Katyuscya V, da Silva Jonatas G, Klein Raphael C, Klein Mary H F, da S Ramos Bruno H, Fernandes Cristiane K C, de L Ribas Dayane G, Oesterreich Silvia A
Research Group on Development of Pharmaceutical Products (P & DProFar), Center for Biological and Health Sciences, Federal University of Western Bahia, Rua Bertioga, 892, Morada Nobre II, Barreiras CEP 47810-059, BA, Brazil.
Department of Pharmacology, Center for Biological Sciences, Federal University of Paraná, Jardim das Américas, Caixa. postal 19031, Curitiba CEP 81531-990, PR, Brazil.
Pharmaceuticals (Basel). 2021 Feb 12;14(2):148. doi: 10.3390/ph14020148.
Serotonin (5-HT) receptors are found throughout central and peripheral nervous systems, mainly in brain regions involved in the neurobiology of anxiety and depression. 5-HT receptors are currently promising targets for discovering new drugs for treating disorders ranging from migraine to neuropsychiatric upsets, such as anxiety and depression. It is well described in the current literature that the brain expresses seven types of 5-HT receptors comprising eighteen distinct subtypes. In this article, we comprehensively reviewed 5-HT1-7 receptors. Of the eighteen 5-HT receptors known today, thirteen are G protein-coupled receptors (GPCRs) and represent targets for approximately 40% of drugs used in humans. Signaling pathways related to these receptors play a crucial role in neurodevelopment and can be modulated to develop effective therapies to treat anxiety and depression. This review presents the experimental evidence of the modulation of the "serotonergic receptosome" in the treatment of anxiety and depression, as well as demonstrating state-of-the-art research related to phytochemicals and these disorders. In addition, detailed aspects of the pharmacological mechanism of action of all currently known 5-HT receptor families were reviewed. From this review, it will be possible to direct the rational design of drugs towards new therapies that involve signaling via 5-HT receptors.
血清素（5-羟色胺，5-HT）受体遍布中枢神经系统和外周神经系统，主要存在于与焦虑和抑郁神经生物学相关的脑区。5-HT受体目前是发现治疗从偏头痛到神经精神紊乱（如焦虑和抑郁）等疾病新药的有前景靶点。当前文献充分描述了大脑表达七种类型的5-HT受体，包含十八种不同亚型。在本文中，我们全面综述了5-HT1 - 7受体。在如今已知的十八种5-HT受体中，有十三种是G蛋白偶联受体（GPCRs），并且是约40%用于人类的药物的靶点。与这些受体相关的信号通路在神经发育中起关键作用，并且可以被调节以开发治疗焦虑和抑郁的有效疗法。本综述展示了“血清素受体体”在治疗焦虑和抑郁方面调节作用的实验证据，以及展示了与植物化学物质和这些疾病相关的前沿研究。此外，还综述了所有目前已知的5-HT受体家族药理作用机制的详细方面。通过本综述，将有可能针对涉及通过5-HT受体信号传导的新疗法进行药物的合理设计。
