Pharmacological properties of S1RA, a new sigma‐1 receptor antagonist that inhibits neuropathic pain and activity‐induced spinal sensitization
BACKGROUND AND PURPOSE The sigma‐1 (σ1) receptor is a ligand‐regulated molecular
chaperone that has been involved in pain, but there is limited understanding of the actions …
chaperone that has been involved in pain, but there is limited understanding of the actions …
Sigma 1 receptor: a new therapeutic target for pain
Abstract Sigma 1 receptor (σ 1 receptor) is a unique ligand-regulated molecular chaperone
located mainly in the endoplasmic reticulum and the plasma membrane. σ 1 receptor is …
located mainly in the endoplasmic reticulum and the plasma membrane. σ 1 receptor is …
Pharmacological modulation of the sigma 1 receptor and the treatment of pain
M Merlos, J Burgueño, E Portillo-Salido… - Sigma Receptors: Their …, 2017 - Springer
There is a critical need for new analgesics acting through new mechanisms of action, which
could increase the efficacy with respect to existing therapies and reduce their unwanted …
could increase the efficacy with respect to existing therapies and reduce their unwanted …
Effects of the selective sigma‐1 receptor antagonist S1 RA on formalin‐induced pain behavior and neurotransmitter release in the spinal cord in rats
A Vidal‐Torres, B Fernández‐Pastor… - Journal of …, 2014 - Wiley Online Library
We have previously shown that the selective sigma‐1 receptor (σ1R) antagonist S1 RA (E‐
52862) inhibits neuropathic pain and activity‐induced spinal sensitization in various pre …
52862) inhibits neuropathic pain and activity‐induced spinal sensitization in various pre …
[HTML][HTML] The selective sigma-1 receptor antagonist E-52862 attenuates neuropathic pain of different aetiology in rats
G Gris, E Portillo-Salido, B Aubel, Y Darbaky… - Scientific reports, 2016 - nature.com
E-52862 is a selective σ1R antagonist currently undergoing phase II clinical trials for
neuropathic pain and represents a potential first-in-class analgesic. Here, we investigated …
neuropathic pain and represents a potential first-in-class analgesic. Here, we investigated …
Sigma-1 receptors regulate activity-induced spinal sensitization and neuropathic pain after peripheral nerve injury
B de la Puente, X Nadal, E Portillo-Salido… - Pain, 2009 - Elsevier
Sigma-1 receptor (σ1R) is expressed in key CNS areas involved in nociceptive processing
but only limited information is available about its functional role. In the present study we …
but only limited information is available about its functional role. In the present study we …
[HTML][HTML] Critical role of sigma-1 receptors in central neuropathic pain-related behaviours after mild spinal cord injury in mice
S Castany, G Gris, JM Vela, E Verdú… - Scientific reports, 2018 - nature.com
Abstract Sigma-1 receptor (σ1R) knockout (KO) CD1 mice, generated by homologous
recombination, and separate pharmacological studies in wild type (WT) mice were done to …
recombination, and separate pharmacological studies in wild type (WT) mice were done to …
Investigational sigma-1 receptor antagonists for the treatment of pain
Introduction: The sigma-1 receptor (σ1R) is a ligand-regulated molecular chaperone that
interacts with other proteins, including NMDA and opioid receptors, to modulate their activity …
interacts with other proteins, including NMDA and opioid receptors, to modulate their activity …
Sigma-1 receptor and pain
There is a critical need for new analgesics acting through new mechanisms of action, which
could increase the efficacy respect to existing therapies and/or reduce their unwanted …
could increase the efficacy respect to existing therapies and/or reduce their unwanted …
[HTML][HTML] Characterization of sigma 1 receptor antagonist CM-304 and its analog, AZ-66: novel therapeutics against allodynia and induced pain
TJ Cirino, SO Eans, JM Medina, LL Wilson… - Frontiers in …, 2019 - frontiersin.org
Sigma-1 receptors (S1R) and sigma-2 receptors (S2R) may modulate nociception without
the liabilities of opioids, offering a promising therapeutic target to treat pain. The purpose of …
the liabilities of opioids, offering a promising therapeutic target to treat pain. The purpose of …
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