Molecules, Vol. 26, Pages 1212: Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia
Molecules, Vol. 26, Pages 1212: Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia
Molecules doi: 10.3390/molecules26051212
Authors:
Jun-Jie Shi
Qi-Hui Jiang
Tian-Ning Zhang
Hao Sun
Wen-Wen Shi
Hendra Gunosewoyo
Fan Yang
Jie Tang
Tao Pang
Li-Fang Yu
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.
Source: Molecules - Category: Chemistry Authors: Jun-Jie Shi Qi-Hui Jiang Tian-Ning Zhang Hao Sun Wen-Wen Shi Hendra Gunosewoyo Fan Yang Jie Tang Tao Pang Li-Fang Yu Tags: Article Source Type: research