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The pharmacology of sigma-1 receptors [PDF]
Pharmacology & Therapeutics, 2009 Originally considered an enigmatic protein, the sigma-1 receptor has recently been identified as a unique ligand-regulated molecular chaperone in the endoplasmic reticulum of cells. This discovery causes us to look back at the many proposed roles of this receptor, even before its molecular function was identified, in many diseases such as ...
Tangui, Maurice, Tsung-Ping, Su
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Frontiers in Pharmacology, 2020 Sigma-1 and sigma-2 receptors are emerging therapeutic targets. Although the molecular identity of the sigma-2 receptor has recently been determined, receptor quantitation has used, and continues to use, the sigma-1 selective agents (+) pentazocine or ...
Haider Abbas +5 more
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Biochemical Pharmacology of the Sigma-1 Receptor [PDF]
Molecular Pharmacology, 2016 The sigma-1 receptor (S1R) is a 223 amino acid two transmembrane (TM) pass protein. It is a non-ATP-binding nonglycosylated ligand-regulated molecular chaperone of unknown three-dimensional structure. The S1R is resident to eukaryotic mitochondrial-associated endoplasmic reticulum and plasma membranes with broad functions that regulate cellular calcium
Uyen B, Chu, Arnold E, Ruoho
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Molecular Brain, 2020 The Sigma-1 receptor (σ1R) has emerged as an interesting pharmacological target because it inhibits analgesia mediated by mu-opioid receptors (MOR), and also facilitates the development of neuropathic pain.
Pilar Sánchez-Blázquez +4 more
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Sigma-1 Receptor Chaperones and Diseases [PDF]
Central Nervous System Agents in Medicinal Chemistry, 2009 Chaperones are proteins that assist the correct folding of other protein clients either when the clients are being synthesized or at their functional localities. Chaperones are responsible for certain diseases. The sigma-1 receptor is recently identified as a receptor chaperone whose activity can be activated/deactivated by specific ligands.
Shang-Yi, Tsai +3 more
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Highly Specific Sigma Receptor Ligands Exhibit Anti-Viral Properties in SARS-CoV-2 Infected Cells
Pathogens, 2021 (1) Background: There is a strong need for prevention and treatment strategies for COVID-19 that are not impacted by SARS-CoV-2 mutations emerging in variants of concern.
David A. Ostrov +15 more
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Frontiers in Pharmacology, 2021 In traumatic spinal cord injury, the initial trauma is followed by a cascade of impairments, including excitotoxicity and calcium overload, which ultimately induces secondary damages. The sigma-1 receptor is widely expressed in the central nervous system
Alise Lattard +6 more
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Sigma-1 receptor agonists directly inhibit Nav1.2/1.4 channels.
PLoS ONE, 2012 (+)-SKF 10047 (N-allyl-normetazocine) is a prototypic and specific sigma-1 receptor agonist that has been used extensively to study the function of sigma-1 receptors.
Xiao-Fei Gao +4 more
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International Journal of Cardiology: Heart & Vasculature, 2020 Sigma-1 receptors are ligand-regulated chaperone proteins, involved in several cellular mechanisms. The aim of this systematic review was to examine the effects that the sigma-1 receptor has on the cardiovascular system.
Rebecca Lewis +4 more
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Scientific Reports, 2023 Sigma-1 Receptor has been shown to localize to sites of peripheral nerve injury and back pain. Radioligand probes have been developed to localize Sigma-1 Receptor and thus image pain source.
Ethan Schonfeld +6 more
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