S1R agonist 2

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.

S1R agonist 2 (Compound 8b; 0.1-5 μM) significantly increases the nerve growth factor (NGF) induced neurite outgrowth at all the tested concentrations in a dose-dependent manner^[1].
S1R agonist 2 (24 h) significantly prevents cell damage induced by Rotenone when tested at the concentration of 1 μM in SHSY5Y cells^[1].
S1R agonist 2 (0.1-5 μM; 24 h) demonstrates a neuroprotective effect against NMDA stimuli in SHSY5Y cells^[1].
S1R agonist 2 (0-10 μM; 24-72 h) shows no cytotoxicity against A549, LoVo and Panc-1 cells^[1].

S1R agonist 2 (Compound 8b; 0.1-50 μM; 120 h) does not induce embryo death (100% of embryos alive) at 10 μM, but induces the death of all zebrafish embryo at the highest dose tested (50 μM)^[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.