scholarly journals The sigma-1 receptor mediates the beneficial effects of pridopidine in a mouse model of Huntington disease

2017 ◽  
Vol 97 ◽  
pp. 46-59 ◽  
Author(s):  
Daniel Ryskamp ◽  
Jun Wu ◽  
Michal Geva ◽  
Rebecca Kusko ◽  
Iris Grossman ◽  
...  
Keyword(s):  
Mouse Model ◽  
Huntington Disease ◽  
Sigma 1 Receptor ◽  
Beneficial Effects ◽  
Sigma 1

ANAVEX®2-73 (blarcamesine), a Sigma-1 receptor agonist, ameliorates neurologic impairments in a mouse model of Rett syndrome

2019 ◽  
Vol 187 ◽  
pp. 172796 ◽  
Author(s):  
Walter E. Kaufmann ◽  
Jeffrey Sprouse ◽  
Nell Rebowe ◽  
Taleen Hanania ◽  
Daniel Klamer ◽  
...  
Keyword(s):  
Mouse Model ◽  
Rett Syndrome ◽  
Receptor Agonist ◽  
Sigma 1 Receptor ◽  
Sigma 1

scholarly journals Sigma-1 Receptor Engages an Anti-Inflammatory and Antioxidant Feedback Loop Mediated by Peroxiredoxin in Experimental Colitis

Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1081
Author(s):  
Nikoletta Almási ◽  
Szilvia Török ◽  
Zsuzsanna Valkusz ◽  
Máté Tajti ◽  
Ákos Csonka ◽  
...  
Keyword(s):  
Experimental Colitis ◽  
The Body ◽  
Male Rats ◽  
Trinitrobenzenesulfonic Acid ◽  
Simultaneous Treatment ◽  
Sigma 1 Receptor ◽  
Beneficial Effects ◽  
Chronic Inflammatory Condition ◽  
Sigma 1 ◽  
Inflammatory Bowel

Inflammatory bowel disease (IBD), comprising Crohn’s disease (CD) and ulcerative colitis (UC), is a chronic inflammatory condition of the gastrointestinal tract. Since the treatment of IBD is still an unresolved issue, we designed our study to investigate the effect of a novel therapeutic target, sigma-1 receptor (σ1R), considering its ability to activate antioxidant molecules. As a model, 2,4,6-trinitrobenzenesulfonic acid (TNBS) was used to induce colitis in Wistar–Harlan male rats. To test the beneficial effects of σ1R, animals were treated intracolonically (i.c.): (1) separately with an agonist (fluvoxamine (FLV)), (2) with an antagonist of the receptor (BD1063), or (3) as a co-treatment. Our results showed that FLV significantly decreased the severity of inflammation and increased the body weight of the animals. On the contrary, simultaneous treatment of FLV with BD1063 diminished the beneficial effects of FLV. Furthermore, FLV significantly enhanced the levels of glutathione (GSH) and peroxiredoxin 1 (PRDX1) and caused a significant reduction in 3-nitrotyrosine (3-NT) levels, the effects of which were abolished by co-treatment with BD1063. Taken together, our results suggest that the activation of σ1R in TNBS-induced colitis through FLV may be a promising therapeutic strategy, and its protective effect seems to involve the antioxidant pathway system.

scholarly journals Sigma‐1 receptor modulates neuroinflammation associated with mechanical hypersensitivity and opioid tolerance in a mouse model of osteoarthritis pain

2019 ◽  
Vol 176 (20) ◽  
pp. 3939-3955 ◽  
Author(s):  
Mireia Carcolé ◽  
Sami Kummer ◽  
Leonor Gonçalves ◽  
Daniel Zamanillo ◽  
Manuel Merlos ◽  
...  
Keyword(s):  
Mouse Model ◽  
Opioid Tolerance ◽  
Sigma 1 Receptor ◽  
Mechanical Hypersensitivity ◽  
Osteoarthritis Pain ◽  
Sigma 1

scholarly journals Optimal timing for activation of sigma 1 receptor in the Pde6b/J (rd10) mouse model of retinitis pigmentosa

2021 ◽  
Vol 202 ◽  
pp. 108397
Author(s):  
Jing Wang ◽  
Haiyan Xiao ◽  
Shannon Barwick ◽  
Yutao Liu ◽  
Sylvia B. Smith
Keyword(s):  
Mouse Model ◽  
Retinitis Pigmentosa ◽  
Optimal Timing ◽  
Sigma 1 Receptor ◽  
Sigma 1

scholarly journals Known Drugs Identified by Structure-Based Virtual Screening Are Able to Bind Sigma-1 Receptor and Increase Growth of Huntington Disease Patient-Derived Cells

2021 ◽  
Vol 22 (3) ◽  
pp. 1293
Author(s):  
Theo Battista ◽  
Gianmarco Pascarella ◽  
David Sasah Staid ◽  
Gianni Colotti ◽  
Jessica Rosati ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Huntington Disease ◽  
Drug Repositioning ◽  
3D Structure ◽  
Disease Patient ◽  
Neuroprotective Activity ◽  
Computational Docking ◽  
Sigma 1 Receptor ◽  
Sigma 1

Huntington disease (HD) is a devastating and presently untreatable neurodegenerative disease characterized by progressively disabling motor and mental manifestations. The sigma-1 receptor (σ1R) is a protein expressed in the central nervous system, whose 3D structure has been recently determined by X-ray crystallography and whose agonists have been shown to have neuroprotective activity in neurodegenerative diseases. To identify therapeutic agents against HD, we have implemented a drug repositioning strategy consisting of: (i) Prediction of the ability of the FDA-approved drugs publicly available through the ZINC database to interact with σ1R by virtual screening, followed by computational docking and visual examination of the 20 highest scoring drugs; and (ii) Assessment of the ability of the six drugs selected by computational analyses to directly bind purified σ1R in vitro by Surface Plasmon Resonance and improve the growth of fibroblasts obtained from HD patients, which is significantly impaired with respect to control cells. All six of the selected drugs proved able to directly bind purified σ1R in vitro and improve the growth of HD cells from both or one HD patient. These results support the validity of the drug repositioning procedure implemented herein for the identification of new therapeutic tools against HD.

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