Abstract
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.
Keywords: Addiction, calcium, neuroprotection, probe, sigma-2 receptor.
Current Medicinal Chemistry
Title:Sigma-2 Receptor Ligands: Neurobiological Effects
Volume: 22 Issue: 8
Author(s): Lin Guo and Xuechu Zhen
Affiliation:
Keywords: Addiction, calcium, neuroprotection, probe, sigma-2 receptor.
Abstract: 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:
Guo Lin and Zhen Xuechu, 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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