Open AccessGW117: A novel serotonin (5‐HT 2C ) receptor antagonist and melatonin (MT 1 /MT 2 ) receptor agonist with potential antidepressant‐like activity in rodents
Author(s) -
Gao Nana,
Zheng Wei,
Murezati Tiliwaerde,
Gu Wei,
Li Xiaorong,
Jin Zengliang
Publication year - 2021
Publication title -
cns neuroscience and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.403
H-Index - 69
eISSN - 1755-5949
pISSN - 1755-5930
DOI - 10.1111/cns.13630
Subject(s) - melatonin receptor , melatonin , agonist , antidepressant , serotonin , 5 ht receptor , pharmacology , antagonist , receptor antagonist , receptor , chemistry , endocrinology , medicine , hippocampus
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 [ 35 S]‐GTPγS and [ 3 H]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‐HT 2C ) receptor antagonist and melatonin type 1 and 2 (MT 1 /MT 2 ) receptor agonist properties, as well as evident antidepressant and anxiolytic effects. Conclusion These data suggest that GW117 is probably a potent antidepressant.