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.
NE-100 is a potent and selective σ1 receptor antagonist.
Progress in neuro-psychopharmacology & biological psychiatry, 32(7), 1656-1659 (2008-07-24)
In addition to acetylcholinesterase (AChE) inhibition, donepezil binds to sigma-1 receptors. In this study, we examined the effects of donepezil on nerve growth factor (NGF)-induced neurite outgrowth in PC12 cells. Donepezil significantly potentiated the NGF-induced neurite outgrowth in a concentration-dependent
We evaluated the role of sigma(1) receptors on capsaicin-induced mechanical hypersensitivity and on nociceptive pain induced by punctate mechanical stimuli, using wild-type and sigma(1) receptor knockout (sigma(1)-KO) mice and selective sigma(1) receptor-acting drugs. Mutation in sigma(1)-KO mice was confirmed by
Expert opinion on therapeutic targets, 14(10), 1009-1022 (2010-08-21)
We here investigated the effect of sigma-1 receptor (Sig-1R) stimulation with fluvoxamine on myocardial hypertrophy, cardiac functional recovery and defined mechanisms underlying its cardioprotective action. Wistar rats subjected to bilateral ovariectomy (OVX) were treated with abdominal aortic banding between the
Current drug metabolism, 7(2), 135-146 (2006-02-14)
The purpose of this study was to propose a new method to predict in vivo drug-drug interactions (DDIs) for a high clearance drug from in vitro data. As the high clearance drug, NE-100 (N, N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine monohydrochloride) was used. First, approach
Journal of neurochemistry, 119(4), 839-847 (2011-09-03)
Chloroquine, a widely used anti-malarial and anti-rheumatoid agent, has been reported to induce apoptotic and non-apoptotic cell death. Accumulating evidence now suggests that chloroquine can sensitize cancer cells to cell death and augment chemotherapy-induced apoptosis by inhibiting autophagy. However, chloroquine
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