Pharmacological properties of S1RA, a new sigma‐1 receptor antagonist that inhibits neuropathic pain and activity‐induced spinal sensitization

L Romero, D Zamanillo, X Nadal… - British journal of …, 2012 - Wiley Online Library
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 …

Sigma 1 receptor: a new therapeutic target for pain

D Zamanillo, L Romero, M Merlos, JM Vela - European Journal of …, 2013 - Elsevier
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 …

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 …

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 …

[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 …

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 …

[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 …

Investigational sigma-1 receptor antagonists for the treatment of pain

JM Vela, M Merlos, C Almansa - Expert Opinion on Investigational …, 2015 - Taylor & Francis
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 …

Sigma-1 receptor and pain

M Merlos, L Romero, D Zamanillo… - … Proteins: Evolution of …, 2017 - Springer
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 …

[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 …