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S1R agonist 2

Names

[ CAS No. ]:
150085-21-5

[ Name ]:
S1R agonist 2

Biological Activity

[Description]:

S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

[Target]

Sigma 1 Receptor:1.1 nM (Ki)

Sigma 2 Receptor:88 nM (Ki)


[In Vitro]

S1R agonist 2 (Compound 8b; 0.1-5 μM) 均能显著增加神经生长因子 (NGF) 诱导的神经突生长，且呈剂量依赖性[1]。 S1R agonist 2 (24 h) 在 SHSY5Y 细胞中浓度为 1 μM 时对 Rotenone (HY-B1756) 诱导的细胞损伤有显著的抑制作用[1]。 S1R agonist 2 (0.1-5 μM; 24 h) 在 SHSY5Y 细胞中对 NMDA 刺激有神经保护作用[1]。 S1R agonist 2 (0-10 μM; 24-72 h) 对 A549、LoVo 和 Panc-1 细胞无细胞毒性[1]。

[In Vivo]

S1R agonist 2 (Compound 8b; 0.1-50 μM; 120 h) 在 10 μM 浓度下不诱导胚胎死亡 (100%存活胚胎)，但在最高剂量 (50 μM) 下诱导所有胚胎死亡[1]。

[References]

[1]. Linciano P, et al. Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents. Eur J Med Chem. 2023 Mar 5;249:115163.  

Chemical & Physical Properties

[ Molecular Formula ]:
C21H27NO

[ Molecular Weight ]:
309.45

Related Compounds