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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.
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.
  • Shi JJ; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
  • Jiang QH; New Drug Screening Center, Jiangsu Center for Pharmacodynamics Research and Evaluation, Institute of Pharmaceutical Sciences, China Pharmaceutical University, Nanjing 210009, China.
  • Zhang TN; New Drug Screening Center, Jiangsu Center for Pharmacodynamics Research and Evaluation, Institute of Pharmaceutical Sciences, China Pharmaceutical University, Nanjing 210009, China.
  • Sun H; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
  • Shi WW; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
  • Gunosewoyo H; School of Pharmacy and Biomedical Sciences, Faculty of Health Sciences, Curtin University, Bentley, Perth, WA 6102, Australia.
  • Yang F; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
  • Tang J; Shanghai Key Laboratory of Green Chemistry and Chemical Process, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
  • Pang T; New Drug Screening Center, Jiangsu Center for Pharmacodynamics Research and Evaluation, Institute of Pharmaceutical Sciences, China Pharmaceutical University, Nanjing 210009, China.
  • Yu LF; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
Molecules ; 26(5)2021 Feb 24.
Article en En | MEDLINE | ID: mdl-33668340
ABSTRACT
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.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxazoles / Receptores sigma / Recuperación de la Función / Infarto de la Arteria Cerebral Media / Quinasas MAP Reguladas por Señal Extracelular / Proyección Neuronal / Actividad Motora Límite: Animals Idioma: En Año: 2021 Tipo del documento: Article
Texto completo
Imprimir
XML
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxazoles / Receptores sigma / Recuperación de la Función / Infarto de la Arteria Cerebral Media / Quinasas MAP Reguladas por Señal Extracelular / Proyección Neuronal / Actividad Motora Límite: Animals Idioma: En Año: 2021 Tipo del documento: Article