S1R agonist 1 hydrochloride

S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

S1R agonist 1 (Compound 6b; 0.1-5 μM) hydrochloride significantly increases the nerve growth factor (NGF) induced neurite outgrowth at all the tested concentrations in a dose-dependent manner in PC12 cell lines^[1].
S1R agonist 1 (24 h) hydrochloride significantly prevents cell damage induced by Rotenone when tested at the concentration of 1 μM in SHSY5Y cells^[1].
S1R agonist 1 (0.1-5 μM; 24 h) hydrochloride demonstrates a neuroprotective effect against NMDA stimuli in SHSY5Y cells^[1].
S1R agonist 1 (0-10 μM; 24-72 h) hydrochloride shows no cytotoxicity against A549, LoVo and Panc-1 cells^[1].

S1R agonist 1 (Compound 6b; 0.1-50 μM; 120 h) hydrochloride induces the death of 4 Zebrafish embryos out of 8 at 10 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.