Description
NE-100 (149409-57-4) 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?NE-100 suppressed ischemia-induced neuronal cell death in mice?via?upregulation of GRP78 through the ATF6 pathway resulting in suppression of ER stress-induced cell death in a sigma-1-independent manner.3
Uses
NE-100 is a potent and selective σ1 receptor antagonist.
Biological Activity
Potent and selective σ 1 receptor antagonist (K i = 0.86 nM) that displays > 55-fold selectivity over σ 2 receptors and > 6000-fold selectivity over D 1 , D 2 , 5-HT 1A , 5-HT 2 and PCP receptors. Exhibits reversible binding (K d = 1.2 nM) and displays antipsychotic activity in vivo . Orally active.
Biochem/physiol Actions
NE-100 is a potent and selective σ1 receptor antagonist with an IC50 value of 1.54 +/- 0.26 nM for σ1 receptors, > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors.
References
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 antagonist (NE-100) prevents tunicamycin-induced cell death via GRP78 induction in hippocampal cells; Biochem. Biophys. Res. Commun.?434?904
