This review compares the biological and physiological function of Sigma receptors [σRs] and their potential therapeutic roles. Sigma receptors are widespread in the central nervous system and across multiple peripheral tissues. σRs consist of sigma receptor one (σ1R) and sigma receptor two (σ2R) and are expressed in numerous regions of the brain. The sigma receptor was originally proposed as a subtype of opioid receptors and was suggested to contribute to the delusions and psychoses induced by benzomorphans such as SKF-10047 and pentazocine. Later studies confirmed that σRs are non-opioid receptors (not an µ opioid receptor) and play a more diverse role in intracellular signaling, apoptosis and metabolic regulation. σ1Rs are intracellular receptors acting as chaperone proteins that modulate Ca2+ signaling through the IP3 receptor. They dynamically translocate inside cells, hence are transmembrane proteins. The σ1R receptor, at the mitochondrial-associated endoplasmic reticulum membrane, is responsible for mitochondrial metabolic regulation and promotes mitochondrial energy depletion and apoptosis. Studies have demonstrated that they play a role as a modulator of ion channels (K+ channels; N-methyl-d-aspartate receptors [NMDAR];...Continue Reading
Serotonergic and non-serotonergic neurons of the dorsal raphe: reciprocal changes in firing induced by peripheral nerve stimulation
Acute elevations of serum luteinizing hormone induced by kainic acid, N-methyl aspartic acid or homocysteic acid
Habenular and other midbrain raphe afferents demonstrated by a modified retrograde tracing technique
Epidermal growth factor selectively enhances NMDA receptor-mediated increase of intracellular Ca2+ concentration in rat hippocampal neurons
Characterization of the binding of [3H](+)-pentazocine to sigma recognition sites in guinea pig brain
Evidence for a glutamate receptor of the AMPA subtype which mediates insulin release from rat perfused pancreas
The metabotropic excitatory amino acid receptor agonist 1S,3R-ACPD selectively potentiates N-methyl-D-aspartate-induced brain injury
Pregnenolone sulfate augments NMDA receptor mediated increases in intracellular Ca2+ in cultured rat hippocampal neurons
Modulation by sigma ligands of N-methyl-D-aspartate-induced [3H]noradrenaline release in the rat hippocampus: G-protein dependency
Activation of hippocampal metabotropic excitatory amino acid receptors leads to seizures and neuronal damage
Autoradiographic identification and characterization of sigma receptors in guinea pig brain using [3H]1(cyclopropylmethyl)-4-(2'-(4''-fluorophenyl)-2'-oxoethyl) piperidine ([3H]DuP 734), a novel sigma receptor ligand
Tryptophan-deficient diet and amino acid drink deplete plasma tryptophan and induce a relapse of depression in susceptible patients
Increase of extracellular acetylcholine level in rat frontal cortex induced by (+)N-allylnormetazocine as measured by brain microdialysis
EEG and auditory evoked potential P300 compared with psychometric tests in assessing vigilance after benzodiazepine sedation and antagonism
Regulation of sigma receptors and responsiveness to guanine nucleotides following repeated exposure of rats to haloperidol: further evidence for multiple sigma binding sites
Electrogenic uptake of glutamate and aspartate into glial cells isolated from the salamander (Ambystoma) retina
Evidence for an anti-amnesic effect of JO 1784 in the rat: a potent and selective ligand for the sigma receptor
Anxiolytic effects of 3 alpha-hydroxy-5 alpha[beta]-pregnan-20-one: endogenous metabolites of progesterone that are active at the GABAA receptor
Isolation and characterization of alternatively spliced variants of the mouse sigma1 receptor gene, Sigmar1
Structural Insights into σ₁ Receptor Interactions with Opioid Ligands by Molecular Dynamics Simulations
In vitro and in vivo Human Metabolism of (S )-[18 F]Fluspidine - A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET)
The Roles of Intracellular Chaperone Proteins, Sigma Receptors, in Parkinson's Disease (PD) and Major Depressive Disorder (MDD)
Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors.
Contribution of Lysosome and Sigma Receptors to Neuroprotective Effects of Memantine Against Beta-Amyloid in the SH-SY5Y Cells
High-throughput screen for compounds that modulate neurite growth of human induced pluripotent stem cell-derived neurons
Sigma-1 Receptor Engages an Anti-Inflammatory and Antioxidant Feedback Loop Mediated by Peroxiredoxin in Experimental Colitis
The sigma-1 receptor as a regulator of dopamine neurotransmission: A potential therapeutic target for methamphetamine addiction
Engineering the Interface between Inorganic Nanoparticles and Biological Systems through Ligand Design.
Development of New Benzylpiperazine Derivatives as σ1 Receptor Ligands with in Vivo Antinociceptive and Anti-Allodynic Effects.
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
Icaritin Exacerbates Mitophagy and Synergizes with Doxorubicin to Induce Immunogenic Cell Death in Hepatocellular Carcinoma
An Endocannabinoid Uptake Inhibitor from Black Pepper Exerts Pronounced Anti-Inflammatory Effects in Mice
Yiqi Huoxue preserves heart function by upregulating the Sigma-1 receptor in rats with myocardial infarction.
Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis
Cell Biology of Lipids
Lipids are essential in many biological functions, including membrane structure, energy storage, and cell signaling. Find the latest research on the cell biology of lipids here.
Brain developing: Influences & Outcomes
This feed focuses on influences that affect the developing brain including genetics, fetal development, prenatal care, and gene-environment interactions. Here is the latest research in this field.