摘要
Sigma-2受体是一种广泛分布的蛋白,它可以介导细胞增殖并涉及肿瘤发病机制。光亲和标记技术证实其分子大小约为18kDa。近期研究表明sigma-2受体可以调节细胞内钙离子浓度、多巴胺神经传递和可卡因诱导的成瘾性。一些sigma-2受体配体(ditolylguanidine、afobazole等)显示神经保护作用。 虽然sigma-2受体还没有被克隆,但是在过去10年已经证实成千上万的sigma-2受体配体显示了高亲和性和高选择性。本综述中,我们主要关注这一系列的高选择性的sigma-2受体配体,他们的神经心理学作用及追踪中枢神经系统中sigma-2受体的分子探针。
关键词: 上瘾,钙,神经保护,探针,sigma-2受体
Current Medicinal Chemistry
Title:Sigma-2 Receptor Ligands: Neurobiological Effects
Volume: 22 Issue: 8
Author(s): Lin Guo and Xuechu Zhen
Affiliation:
关键词: 上瘾,钙,神经保护,探针,sigma-2受体
摘要: 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.
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Cite this article as:
Lin Guo and Xuechu Zhen , Sigma-2 Receptor Ligands: Neurobiological Effects, Current Medicinal Chemistry 2015; 22 (8) . https://dx.doi.org/10.2174/0929867322666150114163607
DOI https://dx.doi.org/10.2174/0929867322666150114163607 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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