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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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Pharmacological and Pathological Implications of Sigma-1 Receptor in Neurodegenerative Diseases [PDF]
Originally identified as a potential receptor for opioids, the sigma-1 receptor is now recognized as an intracellular chaperone protein associated with mitochondria-associated membranes at the endoplasmic reticulum (ER).
Noah Drewes +3 more
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Endoplasmic reticulum (ER) protein sigma-1 receptor represents unique chaperone activity in the central nervous system, and it exerts a potent influence on a number of neurotransmitter systems. Several lines of evidence suggest that activation of sigma-1
Kenji Hashimoto
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The sigma receptors were classified into sigma-1 and sigma-2 receptor based on their different pharmacological profiles. In the past two decades, our understanding of the biological and pharmacological properties of the sigma-1 receptor is increasing ...
Kai Yang +5 more
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Sigma-1 receptor: The novel intracellular target of neuropsychotherapeutic drugs
Sigma-1 receptor ligands have been long expected to serve as drugs for treatment of human diseases such as neurodegenerative disorders, depression, idiopathic pain, drug abuse, and cancer.
Teruo Hayashi
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Allosteric Modulators of Sigma-1 Receptor: A Review [PDF]
Allosteric modulators of sigma-1 receptor (Sig1R) are described as compounds that can increase the activity of some Sig1R ligands that compete with (+)-pentazocine, one of the classic prototypical ligands that binds to the orthosteric Sig1R binding site.
Edijs Vavers +3 more
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The Sigma-1 Receptor in Cellular Stress Signaling [PDF]
After decades of research, the sigma-1 receptor (Sig-1R)’s structure, and molecular functions are being unveiled. Sig-1R is an integral endoplasmic reticulum (ER) membrane protein which forms an oligomer and binds a variety of psychotropic drugs.
Teruo Hayashi
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The sigma-1 receptor as a neurohomeostatic decision hub for GABARAP-mediated receptor trafficking and macroautophagy [PDF]
Gamma-aminobutyric acid receptor-associated protein (GABARAP) is a multifunctional member of the autophagy-related (ATG8) protein family, playing key roles in two distinct cellular pathways: macroautophagy and plasma membrane protein trafficking.
Marius Wilhelm Baeken +4 more
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Sigma-1 Receptors in Depression: Mechanism and Therapeutic Development
Depression is the most common type of neuropsychiatric illness and has increasingly become a major cause of disability. Unfortunately, the recent global pandemic of COVID-19 has dramatically increased the incidence of depression and has significantly ...
Peng Ren +7 more
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Viewpoints Sigma-1 receptor agonist fluvoxamine for multiple sclerosis [PDF]
Accumulating evidence suggests that the Epstein-Barr virus (EBV) plays a key role in the development of multiple sclerosis (MS). Additionally, depressive symptoms often precede the onset of MS.
Kenji Hashimoto
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