NE 100 hydrochloride is a selective sigma-1 receptor antagonist (IC₅₀=4.16nM)[1-2]. NE 100 hydrochloride can improve cognitive impairment, and possesses neuroprotective and antipsychotic activities. NE 100 hydrochloride can be used in research related to nervous system diseases[3-4].
In vitro, PC12 cells were co-treated with NE 100 hydrochloride (1.0µM) and ifenprodil (10µM) for 4 days in the context of nerve growth factor (NGF) (2.5ng/ml)-induced differentiation. NE 100 hydrochloride significantly inhibited the potentiating effect of ifenprodil on NGF-induced neurite outgrowth[5]. Human pulmonary artery endothelial cells (HPAECs) were pretreated with NE 100 hydrochloride (10µM) for 1 hour, followed by stimulation with LPS ( µg/mL) for 6 hours. NE 100 hydrochloride had no effect on LPS-induced expression of the pro-inflammatory factors VCAM-1 and IL-6, on IκBα degradation, or on thrombin-induced intracellular Ca²⁺ release[6].
In vivo, NE 100 hydrochloride (10mg/kg) and Pridopidine (6mg/kg) were co-administered once daily via intraperitoneal injection to CD-1 mice that had previously received phencyclidine (PCP; 10mg/kg/day) for 10 days; this combined treatment continued for 14 days. NE 100 hydrochloride attenuated the ability of Pridopidine to reverse the PCP-induced deficits in novel object recognition[7]. In a glomerular injury model using C57BL/6J mice, NE 100 hydrochloride (1mg/kg/day) was administered via daily intraperitoneal injection for 14 days. NE 100 hydrochloride had no effect on urinary protein leakage, but blocked the ameliorative effect of SA4503 on proteinuria[8].
References:
[1] Okuyama S, Imagawa Y, Ogawa S, et al. NE-100, a novel sigma receptor ligand: in vivo tests. Life Sci. 1993;53(18):PL285-90.
[2] 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. 1995;56(2):PL39-43.
[3] 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. 1994 Jan 4;251(1):R1-2.
[4] Okuyama S, Imagawa Y, Sakagawa T, et al. NE-100, a novel sigma receptor ligand: effect on phencyclidine-induced behaviors in rats, dogs and monkeys. Life Sci. 1994;55(7):PL133-8.
[5] Ishima T, Hashimoto K. Potentiation of nerve growth factor-induced neurite outgrowth in PC12 cells by ifenprodil: the role of sigma-1 and IP3 receptors. PLoS One. 2012;7(5):e37989.
[6] Mahamed Z, Shadab M, Najar RA, et al. The Protective Role of Mitochondria-Associated Endoplasmic Reticulum Membrane (MAM) Protein Sigma-1 Receptor in Regulating Endothelial Inflammation and Permeability Associated with Acute Lung Injury. Cells. 2023 Dec 19;13(1):5.
[7] Sahlholm K, Valle-León M, Fernández-Dueñas V, et al. Pridopidine Reverses Phencyclidine-Induced Memory Impairment. Front Pharmacol. 2018 Apr 10;9:338.
[8] Tagashira H, Chida S, Bhuiyan MS, et al. SA4503 Mitigates Adriamycin-Induced Nephropathy via Sigma-1 Receptor in Animal and Cell-Based Models. Pharmaceuticals (Basel). 2025 Jan 27;18(2):172.
NE 100 hydrochloride是一种选择性sigma-1受体（IC50=4.16nM）拮抗剂[1-2]。NE 100 hydrochloride可改善认知障碍、具有神经保护和抗精神病活性。NE 100 hydrochloride可用于神经系统疾病的相关研究[3-4]。
在体外，NE 100 hydrochloride（1.0μM）与ifenprodil（10μM）共处理PC12细胞4天，在神经生长因子（NGF）（2.5ng/ml）诱导分化的背景下。NE 100 hydrochloride显著抑制了ifenprodil对NGF诱导的神经突生长的增强作用[5]。NE 100 hydrochloride（10μM）预处理人肺动脉内皮细胞（HPAECs）1小时，随后以LPS（1μg/mL）刺激6小时。NE 100 hydrochloride对LPS诱导的促炎因子VCAM-1和IL-6的表达、IκBα降解以及凝血酶诱导的细胞内Ca2+释放均无影响[6]。
在体内，NE 100 hydrochloride（10mg/kg）与Pridopidine（6mg/kg）通过腹腔注射每日一次共同处理已接受10天苯环利定（PCP；10mg/kg/day）的CD-1小鼠，持续14天。NE 100 hydrochloride减弱了Pridopidine改善CD-1小鼠对新物体识别缺陷的作用[7]。NE 100 hydrochloride（1mg/kg/day）通过每日腹腔注射于肾小球损伤的C57BL/6J小鼠，持续14天。NE 100 hydrochloride对尿蛋白泄漏无影响，但可阻断SA4503对蛋白尿的改善作用[8]。