Sigma-2 receptor plays key roles in promoting tumor cell apoptosis, enhancing efficacy of anti-tumor drugs, blocking signal transduction controlled by Aβ oligomers, regulating Ca²⁺ homeostasis and protecting nerve cells. Studies indicated that sigma-2 receptor may be closely coupled with ROS, LDL, mTOR, RAS, PLC/PKC, lysosomal autophagy and mitochondrial super oxidative stress. In addition, the high expression of this receptor in proliferating cells and nerve cells indicates that sigma-2 receptor is an ideal molecular target for imaging and therapeutic development for cancer, Alzheimer's disease, schizophrenia and traumatic brain injury. Various sigma-2 agonists have shown promising anticancer activities, while sigma-2 antagonists have displayed neuroprotection and inhibition of Aβ oligomers in the brain of Alzheimer's disease patients. Thus, both sigma-2 agonists and antagonists are potentially useful therapeutics for the management of cancer and neurodegenerative disorders.

Sigma-2受体在促进肿瘤细胞凋亡、增强抗肿瘤药物疗效、阻断Aβ寡聚体控制的信号转导、调节Ca ^{2+等方面发挥关键作用}稳态和保护神经细胞。研究表明，sigma-2 受体可能与 ROS、LDL、mTOR、RAS、PLC/PKC、溶酶体自噬和线粒体超氧化应激密切相关。此外，该受体在增殖细胞和神经细胞中的高表达表明 sigma-2 受体是癌症、阿尔茨海默病、精神分裂症和创伤性脑损伤成像和治疗开发的理想分子靶点。各种 sigma-2 激动剂已显示出有希望的抗癌活性，而 sigma-2 拮抗剂已显示出对阿尔茨海默病患者大脑中 Aβ 寡聚体的神经保护和抑制作用。因此，sigma-2 激动剂和拮抗剂都是用于治疗癌症和神经退行性疾病的潜在有用疗法。