GW117: A novel serotonin (5-HT2C) receptor antagonist and melatonin (MT1/MT2) receptor agonist with potential antidepressant-like activity in rodents

被引：10
作者：
Gao, Nana [1 ]
Zheng, Wei [2 ]
Murezati, Tiliwaerde [2 ]
Gu, Wei [3 ]
Li, Xiaorong [2 ]
Jin, Zengliang [2 ]
机构：
[1] Captial Med Univ, Beijing Shijitan Hosp, Dept Gastrointestinal Surg & Clin Nutr, Beijing, Peoples R China
[2] Capital Med Univ, Sch Basic Med Sci, Dept Pharmacol, Beijing 100069, Peoples R China
[3] Beijing Guangwei Pharmaceut Technol Co Ltd, Beijing, Peoples R China
来源：
CNS NEUROSCIENCE & THERAPEUTICS | 2021年 / 27卷 / 06期
基金：
中国国家自然科学基金;
关键词：
5‐ HT2C receptor; antidepressant; GW117; melatonin receptor; REUPTAKE INHIBITORS; AGOMELATINE; NOREPINEPHRINE; DRUGS; MODEL; DEPRESSION; STRESS; RATS;
D O I：
10.1111/cns.13630
中图分类号：
Q189 [神经科学];
学科分类号：
071006 ;
摘要：
Aims To evaluate the antidepressant-like effect of compound GW117 in rodents using in vitro binding and uptake assays as well in vivo behavioral tests. Methods We investigated the target profile of GW117 using [S-35]-GTP gamma S and [H-3]PIP binding. Using the forced swimming test and chronic unpredictable stress in rats, tail suspension test in mice and rats, and learned helplessness model in mice, we further revealed the antidepressant-like and anxiolytic-like effects of GW117. Results The current study suggests that GW117 displays serotonin 2C (5-HT2C) receptor antagonist and melatonin type 1 and 2 (MT1/MT2) receptor agonist properties, as well as evident antidepressant and anxiolytic effects. Conclusion These data suggest that GW117 is probably a potent antidepressant.
引用
收藏
页码：702 / 713
页数：12
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