In vitro and in vivo sigma 1 receptor imaging studies in different disease states

H Agha, CR McCurdy - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
The sigma receptor system has been classified into two distinct subtypes, sigma 1 (σ1R) and
sigma 2 (σ2R). Sigma 1 receptors (σ1Rs) are involved in many neurodegenerative diseases …

Comparison of sigma 1 receptor ligands SA4503 and PRE084 to (+)-pentazocine in the rd10 mouse model of RP

J Wang, H Xiao, SR Barwick… - … ophthalmology & visual …, 2020 - iovs.arvojournals.org
Purpose: Sigma 1 receptor is a novel therapeutic target for retinal disease. Its activation,
using a high-affinity, high-specificity ligand (+)-pentazocine ((+)-PTZ), rescues photoreceptor …

[HTML][HTML] The Glu102 mutation disrupts higher-order oligomerization of the sigma 1 receptor

AM Abramyan, H Yano, M Xu, L Liu, S Naing… - Computational and …, 2020 - Elsevier
The sigma 1 receptor (σ1R) is a unique endoplasmic reticulum membrane protein. Its
ligands have been shown to possess therapeutic potential for neurological and substance …

Amyloid toxicity is enhanced after pharmacological or genetic invalidation of the σ1 receptor

T Maurice, M Strehaiano, F Duhr… - Behavioural brain research, 2018 - Elsevier
Abstract The sigma-1 receptor (S1R) is a molecular chaperone which activity modulates
several intracellular signals including calcium mobilization at mitochondria-associated …

Role of sigma-1 receptor in calcium modulation: Possible involvement in cancer

I Pontisso, L Combettes - Genes, 2021 - mdpi.com
Ca2+ signaling plays a pivotal role in the control of cellular homeostasis and aberrant
regulation of Ca2+ fluxes have a strong impact on cellular functioning. As a consequence of …

Drug screening identifies sigma-1-receptor as a target for the therapy of VWM leukodystrophy

A Atzmon, M Herrero, R Sharet-Eshed… - Frontiers in molecular …, 2018 - frontiersin.org
Vanishing white matter (VWM) disease is an autosomal genetic leukodystrophy caused by
mutations in subunits of eukaryotic translation initiation factor 2B (eIF2B). The clinical …

Novel high affinity sigma-1 receptor ligands from minimal ensemble docking-based virtual screening

S Dvorácskó, L Lázár, F Fülöp, M Palkó… - International Journal of …, 2021 - mdpi.com
Sigma-1 receptor (S1R) is an intracellular, multi-functional, ligand operated protein that also
acts as a chaperone. It is considered as a pluripotent drug target in several pathologies. The …

Design and Synthesis of New Acyl Urea Analogs as Potential σ1R Ligands

R Thapa, R Flores, KH Cheng, B Mochona, D Sikazwe - Molecules, 2023 - mdpi.com
In search of synthetically accessible open-ring analogs of PD144418 or 5-(1-propyl-1, 2, 5, 6-
tetrahydropyridin-3-yl)-3-(p-tolyl) isoxazole, a highly potent sigma-1 receptor (σ1R) ligand …

[HTML][HTML] Reduced GFAP expression in bergmann glial cells in the cerebellum of sigma-1 receptor knockout mice determines the neurobehavioral outcomes after …

G Stelfa, E Vavers, B Svalbe, R Serzants… - International Journal of …, 2021 - mdpi.com
Neuroprotective effects of Sigma-1 receptor (S1R) ligands have been observed in multiple
animal models of neurodegenerative diseases. Traumatic brain injury (TBI)-related …

Sigma 1 receptor co-localizes with NRF2 in retinal photoreceptor cells

SR Barwick, MS Siddiq, J Wang, H Xiao, B Marshall… - Antioxidants, 2021 - mdpi.com
Sigma 1 receptor (Sig1R), a modulator of cell survival, has emerged as a novel target for
retinal degenerative disease. Studies have shown that activation of Sig1R, using the high …