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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 ...
Aydar, Ebru +4 more
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The Role of Sigma Receptors in Depression
Journal of Pharmacological Sciences, 2005 Behavioral models used to test potential antidepressants have shown that ligands that bind to sigma receptors possess "antidepressant-like" properties. The focus of this review is to discuss the literature concerning sigma receptors and their ligands, with respect to their antidepressants properties.
Bermack, Jordanna E., Debonnel, Guy
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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.
Agnieszka Anna Piechal +2 more
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The Sigma Enigma: A Narrative Review of Sigma Receptors
Cureus, 2023 The sigma-1 and sigma-2 receptors were first discovered in the 1960s and were thought to be a form of opioid receptors initially. Over time, more was gradually learned about these receptors, which are actually protein chaperones, and many of their unique or unusual properties can contribute to a range of important new therapeutic applications.
Pergolizzi, Joseph +6 more
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Sigma Receptor Binding Assays [PDF]
Current Protocols in Pharmacology, 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.
Uyen B, Chu, Arnold E, Ruoho
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The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception [PDF]
Molecular Brain, 2020 Abstract 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. Based on these findings, the recent cloning of the Sigma-2 receptor (σ2R) led us to investigate its potential role as a regulator ...
Pilar Sánchez-Blázquez +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. Clinical trials with Sig1R ligands are underway testing therapies for the treatment of drug-resistant seizures, developmental and epileptic encephalopathies, and photosensitive epilepsy. However,
Vavers, Edijs +2 more
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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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Cardiac Sigma Receptors – An Update
Physiological Research, 2018 More than four decades passed since sigma receptors were first mentioned. Since then, existence of at least two receptor subtypes and their tissue distributions have been proposed. Nowadays, it is clear, that sigma receptors are unique ubiquitous proteins with pluripotent function, which can interact with so many different classes of proteins.
T, Stracina, M, Novakova
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Sigma Receptor Photolabeling and Sigma Receptor-mediated Modulation of Potassium Channels in Tumor Cells [PDF]
Journal of Biological Chemistry, 1999 Recent work has indicated that sigma receptor ligands can modulate potassium channels. However, the only sigma receptor characterized at the molecular level has a novel structure unlike any other receptor known to modulate ion channels. This 26-kDa protein has a hydropathy profile suggestive of a single membrane-spanning domain, with no apparent ...
R A, Wilke +5 more
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