Structures of the σ2 receptor enable docking for bioactive ligand discovery
The σ2 receptor has attracted intense interest in cancer imaging, psychiatric disease,
neuropathic pain,–and other areas of biology,. Here we determined the crystal structure of …
neuropathic pain,–and other areas of biology,. Here we determined the crystal structure of …
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 …
Targeting sigma receptors for the treatment of neurodegenerative and neurodevelopmental disorders
DS Malar, P Thitilertdecha, KS Ruckvongacheep… - CNS drugs, 2023 - Springer
The sigma-1 receptor is a 223 amino acid-long protein with a recently identified structure.
The sigma-2 receptor is a genetically unrelated protein with a similarly shaped binding …
The sigma-2 receptor is a genetically unrelated protein with a similarly shaped binding …
Highly specific σ2R/TMEM97 ligand FEM-1689 alleviates neuropathic pain and inhibits the integrated stress response
MS Yousuf, JJ Sahn, H Yang… - Proceedings of the …, 2023 - National Acad Sciences
The sigma 2 receptor (σ2R) was described pharmacologically more than three decades ago,
but its molecular identity remained obscure until recently when it was identified as …
but its molecular identity remained obscure until recently when it was identified as …
Pharmacological properties of S1RA, a new sigma‐1 receptor antagonist that inhibits neuropathic pain and activity‐induced spinal sensitization
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 …
chaperone that has been involved in pain, but there is limited understanding of the actions …
Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy] …
JL Díaz, R Cuberes, J Berrocal… - Journal of medicinal …, 2012 - ACS Publications
The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ1
receptor (σ1R) antagonists are reported. The new compounds were evaluated in vitro in …
receptor (σ1R) antagonists are reported. The new compounds were evaluated in vitro in …
[HTML][HTML] Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice
Sigma-1 (σ1) receptors play a role in different types of pain and in central sensitization
mechanisms; however, it is unknown whether they are involved in chemotherapy-induced …
mechanisms; however, it is unknown whether they are involved in chemotherapy-induced …
Sigma 2 receptor/Tmem97 agonists produce long lasting antineuropathic pain effects in mice
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1
receptor (σ1R) is known to be a potential target for neuropathic pain therapeutics, and …
receptor (σ1R) is known to be a potential target for neuropathic pain therapeutics, and …
Sigma-1 receptors control neuropathic pain and macrophage infiltration into the dorsal root ganglion after peripheral nerve injury
I Bravo Caparrós, MC Ruiz Cantero, G Perazzoli… - 2020 - digibug.ugr.es
Neuron-immune interaction in the dorsal root ganglia (DRG) plays a pivotal role in the
neuropathic pain development after nerve injury. Sigma-1 receptor (Sig-1R) is expressed by …
neuropathic pain development after nerve injury. Sigma-1 receptor (Sig-1R) is expressed by …
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 …