Advances with the discovery and development of novel sigma 1 receptor antagonists for the management of pain
M Burns, N Guadagnoli… - Expert Opinion on Drug …, 2023 - Taylor & Francis
Introduction Interest in sigma-1 receptors (S1Rs) has significantly increased in the last 25
years and more recently for their role in pain modulation. S1Rs are novel chaperone …
years and more recently for their role in pain modulation. S1Rs are novel chaperone …
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 …
Selective sigma-1 receptor antagonists for the treatment of pain
C Almansa, JM Vela - Future medicinal chemistry, 2014 - Taylor & Francis
The sigma-1 receptor (σ1R) is located in areas of the CNS key for pain control and belongs
to a unique target class with chaperoning functions over different molecular targets involved …
to a unique target class with chaperoning functions over different molecular targets involved …
[HTML][HTML] Characterization of CM-398, a novel selective sigma-2 receptor ligand, as a potential therapeutic for neuropathic pain
LL Wilson, AR Alleyne, SO Eans, TJ Cirino, HM Stacy… - Molecules, 2022 - mdpi.com
Sigma receptors modulate nociception, offering a potential therapeutic target to treat pain,
but relatively little is known regarding the role of sigma-2 receptors (S2R) in nociception. The …
but relatively little is known regarding the role of sigma-2 receptors (S2R) in nociception. The …
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 …
[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 …
Sigma-1 receptor antagonists: Promising players in fighting neuropathic pain
P Linciano, G Rossino, R Listro, D Rossi… - Pharmaceutical Patent …, 2020 - Taylor & Francis
Sigma-1 receptors (S1Rs) are strongly correlated to neuropathic pain (NP), since their
inactivation may decrease allodynia or dysesthesia, promoting analgesic effects. In the …
inactivation may decrease allodynia or dysesthesia, promoting analgesic effects. In the …
[HTML][HTML] Discovery of RC-752, a Novel Sigma-1 receptor antagonist with antinociceptive activity: a promising tool for fighting neuropathic pain
Neuropathic pain (NP) is a chronic condition resulting from damaged pain-signaling
pathways. It is a debilitating disorder that affects up to 10% of the world's population …
pathways. It is a debilitating disorder that affects up to 10% of the world's population …
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 …
[HTML][HTML] The emerging role of sigma receptors in pain medicine
J Pergolizzi Jr, G Varrassi - Cureus, 2023 - ncbi.nlm.nih.gov
Sigma receptors are protein chaperones with the unexpected characteristic of being
activated by ligand binding. As such, they represent intriguing new targets for potential drug …
activated by ligand binding. As such, they represent intriguing new targets for potential drug …
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