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Novel object recognition test as an alternative approach to assessing the pharmacological profile of sigma-1 receptor ligands
BackgroundAlthough the terms “agonist” and “antagonist” have been used to classify sigma-1 receptor (σ 1 R) ligands, an unambiguous definition of the...
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Insight into binding of endogenous neurosteroid ligands to the sigma-1 receptor
The sigma-1 receptor (σ1R) is a non-opioid membrane receptor, which responds to a diverse array of synthetic ligands to exert various pharmacological...
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A unique sigma/anti-sigma system in the actinomycete Actinoplanes missouriensis
Bacteria of the genus Actinoplanes form sporangia that contain dormant sporangiospores which, upon contact with water, release motile spores...
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An open-like conformation of the sigma-1 receptor reveals its ligand entry pathway
The sigma-1 receptor (σ 1 R) is a non-opioid transmembrane receptor which has been implicated in many diseases, including neurodegenerative disorders...
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Targeting Sigma Receptors for the Treatment of Neurodegenerative and Neurodevelopmental Disorders
The sigma-1 receptor is a 223 amino acid-long protein with a recently identified structure. The sigma-2 receptor is a genetically unrelated protein...
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Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3,3-dialkyl-γ-butyrolactones as sigma-2 ligands
The sigma-2 (σ 2 ) receptor has been linked to several diseases and conditions including cancer, neuropathic drug addiction, Alzheimer’s disease,...
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Structures of the σ2 receptor enable docking for bioactive ligand discovery
The σ 2 receptor has attracted intense interest in cancer imaging
1 , psychiatric disease2 , neuropathic pain3 –5 and other areas of biology6 ,7 . Here we...
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Schwann Cell-Derived Exosomes Induced Axon Growth after Spinal Cord Injury by Decreasing PTP-σ Activation on CSPGs via the Rho/ROCK Pathway
Spinal cord injury (SCI) is a severe neurological condition that involves a lengthy pathological process. This process leads to the upregulation of...
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CGI1746 targets σ1R to modulate ferroptosis through mitochondria-associated membranes
Ferroptosis is iron-dependent oxidative cell death. Labile iron and polyunsaturated fatty acid (PUFA)-containing lipids are two critical factors for...
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Discovery of oxazolidinone-based heterocycles as subtype selective sigma-2 ligands
The sigma-2 (σ 2 ) receptor, also known as the Transmembrane Protein 97 (TMEM97, and MAC30 (Meningioma-associated protein), has been linked to a number...
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The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception
The Sigma-1 receptor (σ1R) has emerged as an interesting pharmacological target because it inhibits analgesia mediated by mu-opioid receptors (MOR),...
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Sigma-1 Receptor Activation Suppresses Microglia M1 Polarization via Regulating Endoplasmic Reticulum–Mitochondria Contact and Mitochondrial Functions in Stress-Induced Hypertension Rats
Exposure to stress plays a detrimental role in the pathogenesis of hypertension via neuroinflammation pathways. Microglial neuroinflammation in the...
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Synthesis and evaluation of novel, selective, functionalized γ-butyrolactones as sigma-2 ligands
The sigma-2 (σ 2 ) receptor was discovered nearly 40 years ago and was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30...
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σ2R/TMEM97 in retinal ganglion cell degeneration
The sigma 2 receptor (σ 2 R) was recently identified as an endoplasmic reticulum (ER) membrane protein known as transmembrane protein 97 (TMEM97)....
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Discovery of novel, selective, functionalized 5-(2-(5-arylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)-γ-butyrolactone sigma-2 ligands
The sigma-2 (σ 2 ) receptor was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein)). This...
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In vitro and in vivo evaluation of [125/123I]-2-[4-(2-iodophenyl)piperidino]cyclopentanol([125/123I]-OI5V) as a potential sigma-1 receptor ligand for SPECT
IntroductionWe investigated the characteristics of radio-iodinated 2-[4-(2-iodophenyl)piperidino]cyclopentanol (OI5V) as a single photon emission...
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Role of Sigma-1 Receptors in the Regulation of Heart Function: II. Cardioprotective Role of Sigma-1 Receptors
AbstractPart II of the review considers the literature data that pronounced cardioprotective activity is possessed by sigma-1 receptors (σ 1 Rs) and...
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Microscale Thermophoresis (MST) to Study Rapid Alkalinization Factor (RALF)-Receptor Interactions
Microscale thermophoresis (MST) is a simple but powerful tool to study the in vitro interaction among biomolecules, and to quantify binding...
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Design, synthesis, and evaluation of novel, selective γ-butyrolactones sigma-2 ligands
Nearly 40 years after the first disclosure of sigma receptors, the sigma-2 (σ2) receptor was recently identified as the Transmembrane Protein 97...
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Generative Modelling of Cortical Receptor Distributions from Cytoarchitectonic Images in the Macaque Brain
Neurotransmitter receptor densities are relevant for understanding the molecular architecture of brain regions. Quantitative in vitro receptor...
