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GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents
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 unpredic...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8111499/ https://www.ncbi.nlm.nih.gov/pubmed/33650297 http://dx.doi.org/10.1111/cns.13630 |
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author | Gao, Nana Zheng, Wei Murezati, Tiliwaerde Gu, Wei Li, Xiaorong Jin, Zengliang |
author_facet | Gao, Nana Zheng, Wei Murezati, Tiliwaerde Gu, Wei Li, Xiaorong Jin, Zengliang |
author_sort | Gao, Nana |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-8111499 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-81114992021-05-18 GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents Gao, Nana Zheng, Wei Murezati, Tiliwaerde Gu, Wei Li, Xiaorong Jin, Zengliang CNS Neurosci Ther Original Articles 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. John Wiley and Sons Inc. 2021-03-01 /pmc/articles/PMC8111499/ /pubmed/33650297 http://dx.doi.org/10.1111/cns.13630 Text en © 2021 The Authors. CNS Neuroscience & Therapeutics Published by John Wiley & Sons Ltd. https://creativecommons.org/licenses/by/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Articles Gao, Nana Zheng, Wei Murezati, Tiliwaerde Gu, Wei Li, Xiaorong Jin, Zengliang GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents |
title | GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents |
title_full | GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents |
title_fullStr | GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents |
title_full_unstemmed | GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents |
title_short | GW117: A novel serotonin (5‐HT(2C)) receptor antagonist and melatonin (MT(1)/MT(2)) receptor agonist with potential antidepressant‐like activity in rodents |
title_sort | gw117: a novel serotonin (5‐ht(2c)) receptor antagonist and melatonin (mt(1)/mt(2)) receptor agonist with potential antidepressant‐like activity in rodents |
topic | Original Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8111499/ https://www.ncbi.nlm.nih.gov/pubmed/33650297 http://dx.doi.org/10.1111/cns.13630 |
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