Akotkar Likhit, Aswar Urmila, Ganeshpurkar Ankit, Rathod Kundlik, Bagad Pradnya, Gurav Shailendra
Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India.
Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune411038, India.
ACS Pharmacol Transl Sci. 2024 Jun 4;7(6):1694-1710. doi: 10.1021/acsptsci.4c00084. eCollection 2024 Jun 14.
The 5-hydroxytryptamine-3 receptor (5-HTR), a subtype of serotonin receptor, is a ligand-gated ion channel crucial in mediating fast synaptic transmission in the central and peripheral nervous systems. This receptor significantly influences various neurological activities, encompassing neurotransmission, mood regulation, and cognitive processing; hence, it may serve as an innovative target for neurological disorders. Multiple studies have revealed promising results regarding the beneficial effects of these phytoconstituents and extracts on conditions such as nausea, vomiting, neuropathic pain depression, anxiety, Alzheimer's disease, cognition, epilepsy, sleep, and dyskinesia via modulation of 5-HTR in the pathophysiology of neurological disorder. The review delves into a detailed exploration of , , and studies and clinical studies that discussed phytoconstituents acting on 5-HTR and attenuates difficulties in neurological diseases. The diverse mechanisms by which plant-derived phytoconstituents influence 5-HTR activity offer exciting avenues for developing innovative therapeutic interventions. Besides producing an agonistic or antagonistic effect, some phytoconstituents exert modulatory effects on 5-HTR activity through multifaceted mechanisms. These include γ-aminobutyric acid and cholinergic neuronal pathways, interactions with neurokinin (NK)-1, NK2, serotonergic, and γ-aminobutyric acid(GABA)ergic systems, dopaminergic influences, and mediation of calcium ions release and inflammatory cascades. Notably, the phytoconstituent's capacity to reduce oxidative stress has also emerged as a significant factor contributing to their modulatory role. Despite the promising implications, there is currently a dearth of exploration needed to understand the effect of phytochemicals on the 5-HTR. Comprehensive preclinical and clinical research is of the utmost importance to broaden our knowledge of the potential therapeutic benefits associated with these substances.
5-羟色胺-3受体（5-HTR）是血清素受体的一种亚型，是一种配体门控离子通道，在介导中枢和外周神经系统的快速突触传递中起关键作用。该受体显著影响各种神经活动，包括神经传递、情绪调节和认知加工；因此，它可能成为神经疾病的一个创新靶点。多项研究表明，这些植物成分和提取物通过调节神经疾病病理生理学中的5-HTR，对恶心、呕吐、神经性疼痛、抑郁、焦虑、阿尔茨海默病、认知、癫痫、睡眠和运动障碍等病症具有有益作用，取得了令人鼓舞的结果。本综述深入探讨了讨论作用于5-HTR并减轻神经疾病困难的植物成分的、和研究以及临床研究。植物源性植物成分影响5-HTR活性的多种机制为开发创新治疗干预措施提供了令人兴奋的途径。除了产生激动或拮抗作用外，一些植物成分还通过多方面机制对5-HTR活性发挥调节作用。这些机制包括γ-氨基丁酸和胆碱能神经元途径、与神经激肽（NK）-1、NK2、5-羟色胺能和γ-氨基丁酸（GABA）能系统的相互作用、多巴胺能影响以及钙离子释放和炎症级联反应的介导。值得注意的是，植物成分降低氧化应激的能力也已成为其发挥调节作用的一个重要因素。尽管有这些有前景的意义，但目前对于了解植物化学物质对5-HTR的影响仍缺乏探索。全面开展临床前和临床研究对于拓宽我们对这些物质潜在治疗益处的认识至关重要。
