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Editorial: Sigma Receptors [PDF]
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
doaj +5 more sources
Sigma receptors and neurological disorders [PDF]
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
openaire +2 more sources
Sigma Receptor Binding Assays [PDF]
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]
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
openaire +4 more sources
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
openaire +3 more sources
The Sigma Enigma: A Narrative Review of Sigma Receptors
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
openaire +2 more sources
TMEM97 and PGRMC1 do not mediate sigma-2 ligand-induced cell death [PDF]
Sigma-2 receptors have been implicated in both tumor proliferation and neurodegenerative diseases. Recently the sigma-2 receptor was identified as transmembrane protein 97 (TMEM97).
Hawkins, William G. +9 more
core +3 more sources
Sigma-1 Receptor Plays a Negative Modulation on N-type Calcium Channel
The sigma-1 receptor is a 223 amino acids molecular chaperone with a single transmembrane domain. It is resident to eukaryotic mitochondrial-associated endoplasmic reticulum and plasma membranes.
Kang Zhang +7 more
doaj +1 more source
Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine [PDF]
Release of the neuropeptides corticotropin-releasing factor (CRF) and orexin-A in the ventral tegmental area (VTA) play an important role in stress-induced cocaine-seeking behavior.
Aguinaga, David +17 more
core +1 more source
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
doaj +1 more source

