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Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia
Sigma-1 (σ-1) receptor agonists are considered as potential treatment for stroke. TS-157 is an alkoxyisoxazole-based σ-1 receptor agonist previously discovered in our group. The present study describes TS-157 profile in a battery of tests for cerebral ischemia. Initial evaluation demonstrated the co...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7956808/ https://www.ncbi.nlm.nih.gov/pubmed/33668340 http://dx.doi.org/10.3390/molecules26051212 |
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author | Shi, Jun-Jie Jiang, Qi-Hui Zhang, Tian-Ning Sun, Hao Shi, Wen-Wen Gunosewoyo, Hendra Yang, Fan Tang, Jie Pang, Tao Yu, Li-Fang |
author_facet | Shi, Jun-Jie Jiang, Qi-Hui Zhang, Tian-Ning Sun, Hao Shi, Wen-Wen Gunosewoyo, Hendra Yang, Fan Tang, Jie Pang, Tao Yu, Li-Fang |
author_sort | Shi, Jun-Jie |
collection | PubMed |
description | Sigma-1 (σ-1) receptor agonists are considered as potential treatment for stroke. TS-157 is an alkoxyisoxazole-based σ-1 receptor agonist previously discovered in our group. The present study describes TS-157 profile in a battery of tests for cerebral ischemia. Initial evaluation demonstrated the compound’s safety profile and blood–brain barrier permeability, as well as its ability to induce neurite outgrowth in vitro. The neurite outgrowth was shown to be mediated via σ-1 receptor agonism and involves upregulation of ERK phosphorylation (pERK). In particular, TS-157 also significantly accelerated the recovery of motor function in rats with transient middle cerebral artery occlusion (tMCAO). Overall, the results herein support the notion that σ-1 receptor agonists are potential therapeutics for stroke and further animal efficacy studies are warranted. |
format | Online Article Text |
id | pubmed-7956808 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-79568082021-03-16 Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia Shi, Jun-Jie Jiang, Qi-Hui Zhang, Tian-Ning Sun, Hao Shi, Wen-Wen Gunosewoyo, Hendra Yang, Fan Tang, Jie Pang, Tao Yu, Li-Fang Molecules Article Sigma-1 (σ-1) receptor agonists are considered as potential treatment for stroke. TS-157 is an alkoxyisoxazole-based σ-1 receptor agonist previously discovered in our group. The present study describes TS-157 profile in a battery of tests for cerebral ischemia. Initial evaluation demonstrated the compound’s safety profile and blood–brain barrier permeability, as well as its ability to induce neurite outgrowth in vitro. The neurite outgrowth was shown to be mediated via σ-1 receptor agonism and involves upregulation of ERK phosphorylation (pERK). In particular, TS-157 also significantly accelerated the recovery of motor function in rats with transient middle cerebral artery occlusion (tMCAO). Overall, the results herein support the notion that σ-1 receptor agonists are potential therapeutics for stroke and further animal efficacy studies are warranted. MDPI 2021-02-24 /pmc/articles/PMC7956808/ /pubmed/33668340 http://dx.doi.org/10.3390/molecules26051212 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Shi, Jun-Jie Jiang, Qi-Hui Zhang, Tian-Ning Sun, Hao Shi, Wen-Wen Gunosewoyo, Hendra Yang, Fan Tang, Jie Pang, Tao Yu, Li-Fang Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia |
title | Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia |
title_full | Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia |
title_fullStr | Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia |
title_full_unstemmed | Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia |
title_short | Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia |
title_sort | sigma-1 receptor agonist ts-157 improves motor functional recovery by promoting neurite outgrowth and perk in rats with focal cerebral ischemia |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7956808/ https://www.ncbi.nlm.nih.gov/pubmed/33668340 http://dx.doi.org/10.3390/molecules26051212 |
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