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 …

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 …

Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3, 4-dihydro-2 (1H)-quinolinone scaffold as a potential analgesic

Y Lan, Y Chen, X Xu, Y Qiu, S Liu, X Liu, BF Liu… - European journal of …, 2014 - Elsevier
The synthesis and sigma-1 receptor (σ 1 R) antagonist activity of a new series of 3, 4-dihydro-
2 (1H)-quinolinone derivatives are reported. The new compounds were evaluated in vitro in …

Development of novel alkoxyisoxazoles as sigma-1 receptor antagonists with antinociceptive efficacy

H Sun, M Shi, W Zhang, YM Zheng, YZ Xu… - Journal of Medicinal …, 2016 - ACS Publications
A novel series of sigma (σ) receptor ligands based on an alkoxyisoxazole scaffold has been
designed and synthesized. Preliminary receptor binding assays identified highly potent (K i< …

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 …

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 …

Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity

M Dichiara, FA Ambrosio, SM Lee… - Journal of Medicinal …, 2023 - ACS Publications
The design and synthesis of a series of 2, 7-diazaspiro [4.4] nonane derivatives as potent
sigma receptor (SR) ligands, associated with analgesic activity, are the focus of this work. In …

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 …

Synthesis and pharmacological evaluation of indole-based sigma receptor ligands

C Mésangeau, E Amata, W Alsharif… - European journal of …, 2011 - Elsevier
A series of novel indole-based analogs were prepared and their affinities for sigma
receptors were determined using in vitro radioligand binding assays. The results of this …

S1RA, a selective sigma-1 receptor antagonist, inhibits inflammatory pain in the carrageenan and complete Freund's adjuvant models in mice

G Gris, M Merlos, JM Vela, D Zamanillo… - Behavioural …, 2014 - journals.lww.com
The therapeutic potential of S1RA (E-52862), a selective sigma-1 receptor (σ 1 R)
antagonist, has been explored in experimental neuropathic pain, but not in inflammatory …