WLB-87848具有良好的物理化学性质和ADMET特性,在结合免疫球蛋白(BiP)/σ1R关联测定中显示出σ1R激动剂特征,在体外β-淀粉样肽中毒模型中表现出诱导神经元活力增强的作用,口服给予WLB-87848对海马内注射Aβ肽诱导的大鼠认知障碍具有改善效果。综合这些结果,WLB-87848是一个极具前景的神经保护候选药物,为神经退行性疾病...
During agonist-dependent dissociation from the main chaperone ER BiP (GRP 78, HSPA5) [41,60], Sigma1R stabilizes the ER stress sensor IRE1, prolonging its dimerization, enhancing endonuclease activity and production of a functionally active transcription factor XBP1, which induces expression of ...