受体
Sigma-1受体
兴奋剂
西格玛
西格玛受体
抗抑郁药
体内
药理学
化学
敌手
离体
计算生物学
生物
体外
神经科学
生物化学
遗传学
物理
量子力学
海马体
作者
Rémi Quirion,Wayne D. Bowen,Yossef Itzhak,J.L. Junien,José M. Musacchio,Richard B. Rothman,Tsung‐Ping Su,S. William Tam,Duncan P. Taylor
标识
DOI:10.1016/0165-6147(92)90030-a
摘要
The most intriguing characteristic of the sigma-1 receptor is its ability to regulate multiple functional proteins directly via protein-protein interactions, giving the sigma-1 receptor the powerful ability to regulate several survival and metabolic functions in cells, fine tune neuronal excitability, and regulate the transmission of information within brain circuits. This characteristic makes sigma-1 receptors attractive candidates for the development of new drugs. Hypidone hydrochloride (YL-0919), a novel structured antidepressant candidate developed in our laboratory, possess a selective sigma-1 receptor agonist profile, as evidenced by molecular docking, radioligand receptor binding assays, and receptor functional experiments. In vivo studies have revealed that YL-0919 elicits a fast-onset antidepressant activity (within one week) that can be attenuated with pretreatment of the selective sigma-1 receptor antagonist, BD-1047. Taken together, the findings of the current study suggest that YL-0919 activates the sigma-1 receptor to partially mediate the rapid onset antidepressant effects of YL-0919. Thus, YL-0919 is a promising candidate as a fast-onset antidepressant that targets the sigma-1 receptor.
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