Biochemicals & reagents
1) Okuyama et al. (1994), NE-100, a novel sigma receptor ligand: in vivo tests; Life Sci. 53 PL285 2) Chaki et al. (1994)), NE-100,a novel potent sigma ligand, preferentially binds to sigma 1 binding sites in guinea pig brain; Eur.J.Pharmacol. 251 R1 3) Ono et al. (2013), A sigma-1 receptor antaqonist (NE-100) prevents tunicamycin-induced cell death via GRP78 induction in hippocampal cells; Biochem.Biophys.Res.Commun. 434 904
NE-100 is potent inhibitor of the sigma receptor (σ) with selectivity for sigma-1 (IC50 = 1.5 nM) over sigma-2 (IC50 = 85 nM) (1,2). This compound suppressed ischemia-induced neuronal cell death in mice via upregulation of GPR78 through the ATF6 pathway resulting in suppression of ER stress-induced cell death in a sigma 1 independent manner (3).