Examination of the novel sigma-1 receptor antagonist, SI 1/28, for antinociceptive and anti-allodynic efficacy against multiple types of nociception with fewer liabilities …
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 …
effects. The sigma-1 receptor (S1R) is a potential therapeutic target for neuropathic pain, as …
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 …
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 …
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 …
Antinociceptive effects of a new sigma-1 receptor antagonist (N-(2-morpholin-4-yl-ethyl)-2-(1-naphthyloxy) acetamide) in two types of nociception
BA García-Martínez, OA Jaramillo-Morales… - European Journal of …, 2016 - Elsevier
Pain has become an active clinical challenge due its etiological heterogeneity, symptoms
and mechanisms of action. In the search for new pharmacological therapeutic alternatives …
and mechanisms of action. In the search for new pharmacological therapeutic alternatives …
Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain
Y Lan, Y Chen, X Cao, J Zhang, J Wang… - Journal of Medicinal …, 2014 - ACS Publications
The discovery and synthesis of a new series of pyrimidines as potent sigma-1 receptor (σ1R)
antagonists, associated with pharmacological antineuropathic pain activity, are the focus of …
antagonists, associated with pharmacological antineuropathic pain activity, are the focus of …
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain
J Xiong, J Jin, L Gao, C Hao, X Liu, BF Liu… - European journal of …, 2020 - Elsevier
We designed and synthesized a novel series of piperidine propionamide derivatives as
potent sigma-1 (σ 1) receptor antagonists and mu (μ) opioid receptor agonists, and …
potent sigma-1 (σ 1) receptor antagonists and mu (μ) opioid receptor agonists, and …
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 …
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 …
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 …
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …
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