Sigma-2 Receptor Ligands: Neurobiological Effects
Sigma-2 Receptor Ligands: Neurobiological Effects
复制标题
Sigma-2 受体配体：神经生物学效应
DOI：
10.2174/0929867322666150114163607
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发表时间：
2015-01-01
影响因子：
4.1
通讯作者：
Zhen, Xuechu
中科院分区：
文献类型：
--
作者：
Guo, Lin;Zhen, Xuechu
Sigma-2受体是一种分布广泛的蛋白质，可以调节细胞增殖并参与肿瘤的发病机制。光亲和标记技术证明其分子大小约为18 kDa。最近的研究表明，sigma-2 受体调节胞质 Ca2+ 浓度、多巴胺能传递和可卡因诱导的成瘾行为。一些sigma-2受体配体（二甲苯胍、阿福巴唑等）显示出神经保护作用。尽管sigma-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sigma-2受体配体。在这篇综述中，我们主要关注这一系列选择性sigma-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sigma-2受体的分子探针。
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.