Cited by 66

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Sigma-2 Receptor Ligands: Neurobiological Effects

Guo, Lin, Zhen, Xuechu·2015·Current Medicinal Chemistry

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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Crossref · 10.2174/0929867322666150114163607

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  • Sigma-2 receptors have been studied for more than four decades and are drug targets for several conditions including cancer, pain and diverse CNS disorders.

    “Sigma-2 receptors have been studied for more than four decades and are drug targets for several conditions including cancer, pain and diverse CNS disorders [22, 58]; and most notably, a Sigma-2 modulator, CT1812, is in clinical development in Phase 2 trials for Alzheimer’s disease and dementia with Lewy bodies [11, 21].”

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Metadata

Authors
Guo, L., & Zhen, X.
Venue
Current Medicinal Chemistry
Published
2015-02-16
Volume
22
Issue
8
Pages
989-1003
ISSN
0929-8673
Cited by
66
References
1
Language
en

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