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甘丙肽受体作为新型抗抑郁药的药物靶点:综述

Galanin Receptors as Drug Target for Novel Antidepressants: Review.

作者信息

Demsie Desalegn Getnet, Altaye Birhanetensay Masresha, Weldekidan Etsay, Gebremedhin Hagazi, Alema Niguse Meles, Tefera Mulugeta Mihrete, Bantie Abere Tilahun

机构信息

College of Medicine and Health Sciences, Department of Pharmacy, Adigrat University, Adigrat, Ethiopia.

College of Health Sciences, Debre Berhan University, Debre Berhan, Ethiopia.

出版信息

Biologics. 2020 Apr 21;14:37-45. doi: 10.2147/BTT.S240715. eCollection 2020.

Abstract

Galanin (GAL) is a 29-amino-acid neuropeptide that serves multiple physiological functions throughout the central and peripheral nervous system. Its role involves in a range of physiological and pathological functions including control of food intake, neuro-protection, neuronal regeneration, energy expenditure, reproduction, water balance, mood, nociception and various neuroendocrine functions. The use of currently available antidepressant drugs raises concerns regarding efficacy and onset of action; therefore, the need for antidepressants with novel mechanisms is increasing. Presently, various studies revealed the link between GAL and depression. Attenuation of depressive symptoms is achieved through inhibition of GalR1 and GalR3 and activation of GalR2. However, lack of receptor selectivity of ligands has limited the complete elucidation of effects of different receptors in depression-like behavior. Studies have suggested that GAL enhances the action of selective serotonin reuptake inhibitors (SSRIs) and promotes availability of transcription proteins. This review addresses the role of GAL, GAL receptors (GALRs) ligands including selective peptides, and the mechanism of ligand receptor interaction in attenuating depressive symptoms.

摘要

甘丙肽(GAL)是一种由29个氨基酸组成的神经肽,在中枢和外周神经系统中发挥多种生理功能。其作用涉及一系列生理和病理功能,包括控制食物摄入、神经保护、神经元再生、能量消耗、生殖、水平衡、情绪、痛觉感受以及各种神经内分泌功能。目前可用的抗抑郁药物的使用引发了对其疗效和起效时间的担忧;因此,对具有新机制的抗抑郁药的需求不断增加。目前,各种研究揭示了GAL与抑郁症之间的联系。通过抑制GalR1和GalR3以及激活GalR2可减轻抑郁症状。然而,配体缺乏受体选择性限制了对不同受体在抑郁样行为中作用的完整阐释。研究表明,GAL增强了选择性5-羟色胺再摄取抑制剂(SSRI)的作用,并促进转录蛋白的可用性。本综述探讨了GAL、包括选择性肽在内的GAL受体(GALRs)配体的作用,以及配体-受体相互作用在减轻抑郁症状中的机制。

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