[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 …

[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 …

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 …

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 …

[HTML][HTML] Examination of the novel sigma-1 receptor antagonist, SI 1/28, for antinociceptive and anti-allodynic efficacy against multiple types of nociception with fewer …

LL Wilson, SO Eans, I Ramadan-Siraj… - International Journal of …, 2022 - mdpi.com
Neuropathic pain is a significant problem with few effective treatments lacking adverse
effects. The sigma-1 receptor (S1R) is a potential therapeutic target for neuropathic pain, as …

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 …

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 …

Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one …

S Intagliata, A Sharma, TI King, C Mesangeau… - The AAPS Journal, 2020 - Springer
The sigma-2 receptor has been cloned and identified as Tmem97, which is a
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …

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 …