Anti-Amnesic and Neuroprotective Actions of the Sigma-1 Receptor Agonist (-)-MR22 in Rats with Selective Cholinergic Lesion and Amyloid Infusion

2011 ◽  
Vol 24 (3) ◽  
pp. 569-586 ◽  
Author(s):  
Vuokko Antonini ◽  
Agostino Marrazzo ◽  
Giulio Kleiner ◽  
Marino Coradazzi ◽  
Simone Ronsisvalle ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Sigma 1 Receptor ◽  
Sigma 1 ◽  
Neuroprotective Actions

scholarly journals Cardioprotective Effect of the Selective Sigma-1 Receptor Agonist, SA4503

2014 ◽  
Vol 134 (6) ◽  
pp. 707-713 ◽  
Author(s):  
Kohga Hirano ◽  
Hideaki Tagashira ◽  
Kohji Fukunaga
Keyword(s):  
Receptor Agonist ◽  
Cardioprotective Effect ◽  
Sigma 1 Receptor ◽  
Sigma 1

AF710B, an M1/sigma-1 receptor agonist with long-lasting disease-modifying properties in a transgenic rat model of Alzheimer's disease

2017 ◽  
Vol 14 (6) ◽  
pp. 811-823 ◽  
Author(s):  
Hélène Hall ◽  
Maria Florencia Iulita ◽  
Palma Gubert ◽  
Lisi Flores Aguilar ◽  
Adriana Ducatenzeiler ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Rat Model ◽  
Receptor Agonist ◽  
Transgenic Rat ◽  
Sigma 1 Receptor ◽  
Model Of Alzheimer’S Disease ◽  
Sigma 1 ◽  
Disease Modifying ◽  
Transgenic Rat Model

scholarly journals The Sigma 2 Receptor Promotes and the Sigma 1 Receptor Inhibits Mu-Opioid Receptor-Mediated Antinociception

2020 ◽  
Author(s):  
Pilar Sánchez-Blázquez ◽  
Elsa Cortés-Montero ◽  
María Rodríguez-Muñoz ◽  
Manuel Merlos ◽  
Javier Garzón-Niño
Keyword(s):  
Neuropathic Pain ◽  
Receptor Agonist ◽  
Pain Perception ◽  
Sigma 1 Receptor ◽  
Mu Opioid ◽  
Cannabinoid Type 1 Receptor ◽  
Analgesic Effects ◽  
Sigma 1 ◽  
Regulatory Effects ◽  
Delta Receptor

Abstract The Sigma-1 receptor (σ1R) has emerged as an interesting pharmacological target because it inhibits analgesia mediated by mu-opioid receptors (MOR) and is also implicated in 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 of opioid analgesia and of pain hypersensitivity in σ2R knockout mice. σ2R-/- animals developed mechanical allodynia following establishment of chronic constriction injury-induced neuropathic pain, which was alleviated by the σ1R antagonist S1RA. The analgesic effects of morphine, [D-Ala, N-MePhe, Gly-ol]-encephalin (DAMGO) and β-endorphin increased in σ1R-/- mice and diminished in σ2R-/- mice. The analgesic effect of morphine was increased in σ2R-/- mice by treatment with S1RA. However, σ2R-/- mice and wild-type mice exhibited comparable antinociceptive responses to the delta receptor agonist [D-Pen2,5]-encephalin (DPDPE), the cannabinoid type 1 receptor agonist WIN55212-2 and the alfa2-adrenergic receptor agonist clonidine. These findings suggest that σ2R and σ1R have selective regulatory effects on MOR-mediated analgesia, with σ2R promoting MOR-mediated analgesia and σ1R inhibiting it. Our study may help identify new pharmacological targets for diminishing pain perception and improving opioid detoxification therapies.

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