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).1,2NE-100 suppressed ischemia-induced neuronal cell death in miceviaupregulation 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] SHIGERU OKUYAMA . NE-100, a novel sigma receptor ligand: In vivo tests[J]. Life sciences, 1993, 53 18: Pages PL285-PL290. DOI:
10.1016/0024-3205(93)90588-t[2] NE-100, a novel potent sigma ligand, preferentially binds to sigma 1 binding sites in guinea pig brain
[3] YOKO ONO. A sigma-1 receptor antagonist (NE-100) prevents tunicamycin-induced cell death via GRP78 induction in hippocampal cells[J]. Biochemical and biophysical research communications, 2013, 434 4: Pages 904-909. DOI:
10.1016/j.bbrc.2013.04.055
