Guo Lin, Zhen Xuechu
Department of Pharmacology, College of Pharmaceutical Sciences, Soochow University, 199 Ren'ai Road, Suzhou, Jiangsu Province, China.
Curr Med Chem. 2015;22(8):989-1003. doi: 10.2174/0929867322666150114163607.
Sigma-2 receptor is a widely distributed protein, which can modulate cell proliferation and involved in the pathogenesis of tumor. Photoaffinity labelling techniques testified that its molecular size is about 18 kDa. Recent studies indicated that sigma-2 receptor modulates the cytosolic Ca2+ concentration, dopaminergic transmission, and cocaine-induced addiction behavior. Some sigma-2 receptor ligands (ditolylguanidine, afobazole, etc) display the neuroprotective effect. Although sigma-2 receptor hasn't been cloned, tens of sigma-2 receptor ligands, which demonstrate high affinity and selectivity, have been identified in the past decade. In this review, we mainly focus on these series of selective sigma-2 receptor ligands, their neuropsychological effects, and molecular probes for tracing sigma-2 receptors in central nervous system.
西格玛-2受体是一种广泛分布的蛋白质，它可调节细胞增殖并参与肿瘤的发病机制。光亲和标记技术证实其分子大小约为18千道尔顿。最近的研究表明，西格玛-2受体可调节胞质钙离子浓度、多巴胺能传递以及可卡因诱导的成瘾行为。一些西格玛-2受体配体（二苯胍、阿伏唑等）具有神经保护作用。尽管西格玛-2受体尚未被克隆，但在过去十年中已鉴定出数十种具有高亲和力和选择性的西格玛-2受体配体。在本综述中，我们主要关注这一系列选择性西格玛-2受体配体、它们的神经心理学效应以及用于追踪中枢神经系统中西格玛-2受体的分子探针。
