Amity Institute of Pharmacy, Amity University Madhya Pradesh, Gwalior-474005, India.
Department of Pharmaceutical Chemistry, K. V. S. R. Siddhartha College of Pharmaceutical Sciences, Siddhartha Nagar, Vijayawada, Andhra Pradesh-520010, India.
Curr Neuropharmacol. 2021;19(9):1545-1559. doi: 10.2174/1570159X18666201015155816.
Depression or Major depressive disorder (MDD) is a prolonged condition of sadness. MDD is the most common mental disorder that affects more than 264 million people worldwide. According to the monoamine hypothesis, serotonin (5-hydroxy tryptamine, 5-HT), dopamine (DA) and norepinephrine (NE) are the major neurotransmitters (NTs) involved in depression.
The methodology adopted for writing this review article is essentially based on the secondary literature search through a systematic literature review. This review mainly focussed on the role of 5-HT receptor antagonists (5-HTRA) in depression and comorbid disorders like anxiety.
Out of three major NTs mentioned above, serotonin has a predominant role in the pathophysiology of depression. The serotonin type-3 receptors (5-HTR) are well renowned to be expressed in the central nervous system (CNS) in regions which have significance in the vomiting reflex, perception of pain, the reward system, cognition, depression and anxiety control. 5-HTR are the receptors of serotonergic family that belong to ligand-gated ion channel. 5-HTRA inhibit the binding of serotonin to postsynaptic 5-HTR and increases its availability to other receptors like 5- HT, and as well as 5-HT receptors and produces anti-depressant-like effect. 5-HTRA also have an important role in mood and stress disorders. Some of the studies have shown the effectiveness of these agents in stress disorder.
The present article focussed on the role of 5-HTR and their antagonists in the treatment of depression and anxiety. Further studies are warranted to prove their efficacy with respect to other standard anti-depressants.
抑郁或重性抑郁障碍(MDD)是一种长期的悲伤状态。MDD 是最常见的精神障碍,影响全球超过 2.64 亿人。根据单胺假说,血清素(5-羟色胺,5-HT)、多巴胺(DA)和去甲肾上腺素(NE)是与抑郁相关的主要神经递质(NTs)。
撰写这篇综述文章所采用的方法主要基于通过系统文献综述进行的二次文献检索。本综述主要关注 5-HT 受体拮抗剂(5-HTRA)在抑郁和焦虑等共病障碍中的作用。
在上述三种主要 NT 中,血清素在抑郁的病理生理学中起主要作用。5-羟色胺 3 型受体(5-HTR)在中枢神经系统(CNS)中表达广泛,在呕吐反射、疼痛感知、奖励系统、认知、抑郁和焦虑控制等方面具有重要意义。5-HTR 是属于配体门控离子通道的血清素能家族的受体。5-HTRA 抑制血清素与突触后 5-HTR 的结合,增加其与其他受体如 5-HT、以及 5-HT 受体的结合,产生抗抑郁样作用。5-HTRA 在情绪和应激障碍中也具有重要作用。一些研究表明这些药物在应激障碍中的有效性。
本文重点介绍了 5-HTR 及其拮抗剂在治疗抑郁和焦虑中的作用。需要进一步的研究来证明它们相对于其他标准抗抑郁药的疗效。