S1R agonist 1

Names

[ CAS No. ]:
193354-70-0

[ Name ]:
S1R agonist 1

Biological Activity

[Description]:

S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 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:0.93 nM (Ki)

Sigma 2 Receptor:72 nM (Ki)

[In Vitro]

S1R agonist 1 (Compound 6b; 0.1-5 μM) 在 PC12 细胞中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 1 (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 1 (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 1 (0-10 μM; 24-72 h) 对 A549、LoVo 和 Panc-1 细胞无细胞毒性[1]。

[In Vivo]

S1R agonist 1 (Compound 6b; 0.1-50 μM; 120 h) 在 10 μM 下诱导 8 只斑马鱼胚胎中的 4 只死亡[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 ]:
C₂₀H₂₅NO

[ Molecular Weight ]:
295.42

Related Compounds

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