产品描述 | NE 100 is a potent antagonist of sigma-1 (σ1) receptors (IC50 = 4.16 nM).[1],[2],[3] It only weakly antagonizes dopamine, serotonin, and PCP receptors, but may indirectly alter receptor activity through its effects on σ1.[1],[2],[3] NE 100 is commonly used to study the role of σ1 receptor signaling in cells or animals.[4],[5] Reference: [1]. Chaki, S., Tanaka, M., Muramatsu, M., et al. NE-100, a novel potent sigma ligand, preferentially binds to sigma 1 binding sites in guinea pig brain. Eur. J. Pharmacol. 251(1), R1-2 (1994). [2]. Okuyama, S., Imagawa, Y., Ogawa, S., et al. NE-100, a novel sigma receptor ligand: in vivo tests. Life Sci. 53(18), PL285-PL290 (1993). [3]. Yamamoto, H., Yamamoto, T., Sagi, N., et al. NE-100, a novel sigma ligand: Effects on [3H]TCP binding to intact primary cultured neuronal cells. Life Sci. 56(2), PL39-PL43 (1995). [4]. Dalwadi, D.A., Kim, S., and Schetz, J.A. Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia. Neurochem Int. 105(5), 27-31 (2017). [5]. Hong, J., Sha, S., Zhou, L., et al. Sigma-1 receptor deficiency reduces MPTP-induced parkinsonism and death of dopaminergic neurons. Cell Death Dis. 6, e1832 (2015). |