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

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

  • CNS Neurosci Ther. 2021 Jun;27(6):702-713. doi: 10.1111/cns.13630.
Nana Gao 1,  Wei Zheng 2,  Tiliwaerde Murezati 2,  Wei Gu 3,  Xiaorong Li 2,  Zengliang Jin 2
Affiliations

Affiliations

  • 1 Department of Gastrointestinal Surgery and Clinical Nutrition, Beijing Shijitan Hospital,Captial Medical University, Beijing, China.
  • 2 Department of Pharmacology, School of Basic Medical Sciences, Capital Medical University, Beijing, China.
  • 3 Beijing Guangwei Pharmaceutical Technology Co., Ltd, Beijing, China.
PMID: 33650297 DOI: 10.1111/cns.13630
Abstract

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-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.

Keywords

5-HT2C receptor; GW117; antidepressant; melatonin receptor.

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