NE-100 is a potent and selective σ1 receptor antagonist.
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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.
