Highly Specific Sigma Receptor Ligands Exhibit Anti-Viral Properties in SARS-CoV-2 Infected Cells [PDF]
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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Sigma Receptor Binding Assays. [PDF]
Curr Protoc Pharmacol, 2015 AbstractSigma receptors, both Sigma‐1(S1R) and Sigma‐2 (S2R), are small molecule‐regulated, primarily endoplasmic reticulum (ER) membrane‐associated sites. A number of drugs bind to sigma receptors, including the antipsychotic haloperidol and (+)‐pentazocine, an opioid analgesic.
Chu UB, Ruoho AE.
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The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception [PDF]
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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Advancing depression treatment: the role of sigma receptor ligands [PDF]
Frontiers in NeuroscienceDepression, one of the most prevalent neuropsychiatric disorders, continues to pose escalating global health challenges. Despite the discovery of numerous antidepressants, their clinical applications are limited, and there is still an urgent need to ...
Peng Zhang +6 more
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Editorial: Sigma Receptors [PDF]
Frontiers in Pharmacology, 2020 Sigma receptors were initially described as opioid receptors (Martin et al., 1976). They are now considered neither related to other types of receptor nor to each other. While several ligands used to study these receptors [e.g., di-O-tolyl guanidine (DTG) and haloperidol] have similar affinities for the sigma-1 and sigma-2 receptors, these proteins ...
Ebru Aydar +4 more
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Study of the Relationship between Sigma Receptor Expression Levels and Some Common Sigma Ligand Activity in Cancer Using Human Cancer Cell Lines of the NCI-60 Cell Line Panel [PDF]
Biomedicines, 2021 Sigma (σ) receptors have attracted great interest since they are implicated in various cellular functions and biological processes and diseases, including various types of cancer. The receptor family consists of two subtypes: sigma-1 (σ1) and sigma-2 (σ2)
Evangelia Sereti +4 more
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Pharmacological Research, 2023 Over the last decade, sigma-1 receptor (Sig1R) has been recognized as a valid target for the treatment of seizure disorders and seizure-related comorbidities.
Edijs Vavers +2 more
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Lysosomal Membrane Permeabilization is an Early Event in Sigma-2 Receptor Ligand Mediated Cell Death in Pancreatic Cancer [PDF]
Journal of Experimental & Clinical Cancer Research, 2012 Background Sigma-2 receptor ligands have been studied for treatment of pancreatic cancer because they are preferentially internalized by proliferating cells and induce apoptosis.
Hornick John R +7 more
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Sigma Receptor Ligands Are Potent Antiprion Compounds that Act Independently of Sigma Receptor Binding. [PDF]
ACS Chem NeurosciPrion diseases are invariably fatal neurodegenerative diseases of humans and other animals for which there are no effective treatment options. Previous work from our laboratory identified phenethylpiperidines as a novel class of anti-prion compounds. While working to identify the molecular target(s) of these molecules, we unexpectedly discovered ten ...
Mercer RCC +5 more
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Sigma receptors and neurological disorders [PDF]
Pharmacological Reports, 2021 AbstarctSigma receptors were identified relatively recently, and their presence has been confirmed in the central nervous system and peripheral organs. Changes in sigma receptor function or expression may be involved in neurological diseases, and thus sigma receptors represent a potential target for treating central nervous system disorders.
Piechal, Agnieszka +2 more
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