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Sigma-1 receptor

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https://www.readbyqxmd.com/read/28716934/sigma-1-receptors-control-immune-driven-peripheral-opioid-analgesia-during-inflammation-in-mice
#1
Miguel A Tejada, Angeles Montilla-García, Shane J Cronin, Domagoj Cikes, Cristina Sánchez-Fernández, Rafael González-Cano, M Carmen Ruiz-Cantero, Josef M Penninger, José M Vela, José M Baeyens, Enrique J Cobos
Sigma-1 antagonism potentiates the antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioid drug-induced analgesia. The pathophysiological role of this process is unknown. We aimed to investigate whether sigma-1 antagonism reduces inflammatory pain through the disinhibition of the endogenous opioidergic system in mice. The selective sigma-1 antagonists BD-1063 and S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute (3 h) inflammation...
July 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28702490/sigma-2-receptor-ligands-qsar-model-dataset
#2
Antonio Rescifina, Giuseppe Floresta, Agostino Marrazzo, Carmela Parenti, Orazio Prezzavento, Giovanni Nastasi, Maria Dichiara, Emanuele Amata
The data have been obtained from the Sigma-2 Receptor Selective Ligands Database (S2RSLDB) and refined according to the QSAR requirements. These data provide information about a set of 548 Sigma-2 (σ2) receptor ligands selective over Sigma-1 (σ1) receptor. The development of the QSAR model has been undertaken with the use of CORAL software using SMILES, molecular graphs and hybrid descriptors (SMILES and graph together). Data here reported include the regression for σ2 receptor pKi QSAR models. The QSAR model was also employed to predict the σ2 receptor pKi values of the FDA approved drugs that are herewith included...
August 2017: Data in Brief
https://www.readbyqxmd.com/read/28700244/targeted-yttrium-89-doxorubicin-drug-eluting-bead-a-safety-and-feasibility-pilot-study-in-a-rabbit-liver-cancer-model
#3
Johannes M Ludwig, Minzhi Xing, Yongkang Gai, Lingyi Sun, Dexing Zeng, Hyun S Kim
PURPOSE: To evaluate feasibility and safety of the cancer targeting (Radio)-Chemoembolization drug eluting bead (TRCE-DEB) concept drug SW43-DOX-L-NETA(89Y) DEB for the intra-arterial treatment of VX2 rabbit liver tumors. The treatment compound comprises of the Sigma-2 receptor ligand SW43 for cancer targeting, Doxorubicin (DOX), and 89Yttrium (89Y) as non-radioactive surrogate for therapeutic (Yttrium-90, Lutetium-177) and imaging (Yttrium-86) radioisotopes via the chelator L-NETA. MATERIAL AND METHODS: Ten New Zealand white rabbits with VX2 tumor allografts were used...
July 12, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28687423/an-increase-of-sigma-1-receptor-in-the-penumbra-neuron-after-acute-ischemic-stroke
#4
Xiaotian Zhang, Fangfang Wu, Yun Jiao, Tianyu Tang, Li Yang, Chunqiang Lu, Yanhong Zhang, Yuan Zhang, Ying Bai, Jie Chao, Gaojun Teng, Honghong Yao
BACKGROUND: Penumbra salvage from infarction by early reperfusion within the time window is the target of acute ischemic stroke therapies. Although the penumbral imaging is potently usable in clinic trial, additional work needs to be performed to advancing the field with better-defined, evaluated, and validated imaging measures. METHODS: Mice were subjected to permanent stroke by right middle cerebral artery (MCA) occlusion. Multimodel magnetic resonance imaging (MRI) method was assessed to define the penumbra as that brain region in which the perfusion and diffusion-weighted MR images are mismatched (perfusion-weighted imaging [PWI]-diffusion-weighted imaging [DWI] mismatch)...
July 4, 2017: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/28682953/role-of-sigma-1-receptor-p38-mapk-inhibition-in-acupoint-catgut-embedding-mediated-analgesic-effects-in-complete-freund-s-adjuvant-induced-inflammatory-pain
#5
Kairong Du, Xue Wang, Laiting Chi, Wenzhi Li
BACKGROUND: The endoplasmic reticulum chaperone protein Sigma-1 receptor (Sig-1 R) and mitogen-activated protein kinases (MAPKs) are involved in the mechanism of pain. Acupoint stimulation exerts an exact antihyperalgesic effect in inflammatory pain. However, whether Sig-1 R and MAPKs are associated with the acupoint stimulation-induced analgesic effects is not clear. This study investigated the analgesic effect of acupoint catgut embedding (ACE) and the inhibition of Sig-1 R and MAPKs in ACE analgesia...
July 4, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28667101/sigmar1-regulates-endoplasmic-reticulum-stress-induced-c-ebp-homologous-protein-chop-expression-in-cardiomyocytes
#6
Shafiul Alam, Chowdhury S Abdullah, Richa Aishwarya, A Wayne Orr, James Traylor, Sumitra Miriyala, Manikandan Panchatcharam, Christopher B Pattillo, Md Shenuarin Bhuiyan
C/EBP-homologous protein (CHOP) is a ubiquitously expressed stress-inducible transcription factor robustly induced by maladaptive endoplasmic reticulum (ER) stresses in a wide variety of cells. Here we examined a novel function of Sigma 1 receptor (Sigmar1) in regulating CHOP expression under ER-stress in cardiomyocytes. We also defined Sigmar1-dependent activation of the adaptive ER-stress pathway in regulating CHOP expression. We used adenovirus-mediated Sigmar1 overexpression as well as Sigmar1 knockdown by small interfering RNA (siRNA) in neonatal rat ventricular cardiomyocytes; to induce ER-stress cardiomyocytes were treated with tunicamycin...
June 30, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28654186/haloperidol-decreases-hyperalgesia-and-allodynia-induced-by-chronic-constriction-injury
#7
Josué Vidal Espinosa-Juárez, Osmar Antonio Jaramillo-Morales, Francisco Javier López-Muñoz
Neuropathic pain has proven to be a difficult condition to treat, so investigational therapy has been sought that may prove useful, such as the use of sigma-1 antagonists. Haloperidol (HAL) is a compound that shows a high affinity with these receptors, acting as an antagonist. Therefore, the objective of this study was to demonstrate its effect in an experimental model of neuropathic pain and corroborate its antagonistic action of the sigma-1 receptors under these conditions. BD-1063 was used as a sigma-1 antagonist control and gabapentin was used as a positive control...
June 27, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28648406/n-2-morpholin-4-yl-ethyl-2-1naphthyloxy-acetamide-inhibits-the-chronic-constriction-injury-generated-hyperalgesia-via-the-antagonism-of-sigma-1-receptors
#8
Josué Vidal Espinosa-Juárez, Osmar Antonio Jaramillo-Morales, Gabriel Navarrete-Vázquez, Luis Alberto Melo Hernández, Myrna Déciga-Campos, Francisco Javier López-Muñoz
The most used therapeutic treatment to relieve neuropathic pain is that of neuromodulators such as anti-epileptics or anti-depressants; however, there are alternatives that may be potentially useful. The sigma-1 receptor is a therapeutic target that has shown favorable results at preclinical levels. The aim of this study was to evaluate the anti-hyperalgesic effect of N-(2-morpholin-4-yl-ethyl)-2-(1-naphthyloxy) acetamide (NMIN) in a chronic constriction injury model (CCI) and compare it both a sigma-1 antagonist (BD-1063) and also Gabapentin, as well as determine its possible role as an antagonist of sigma-1 receptors...
June 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28644012/sigma-2-receptor-tmem97-agonists-produce-long-lasting-anti-neuropathic-pain-effects-in-mice
#9
James J Sahn, Galo L Mejia, Pradipta R Ray, Stephen F Martin, Theodore John Price
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1 receptor (σ1R) is a potential target for neuropathic pain therapeutics, and antagonists for this receptor are effective in preclinical models and are currently in phase II clinical trials. Relatively little is known about the σ2R, which has recently been identified as transmembrane protein 97 (Tmem97). We generated a series of σ1R and σ2R/Tmem97 agonists and antagonists and tested them for efficacy in the mouse spared nerve injury (SNI) model...
June 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28622300/the-als-linked-e102q-mutation-in-sigma-receptor-1-leads-to-er-stress-mediated-defects-in-protein-homeostasis-and-dysregulation-of-rna-binding-proteins
#10
Alice Dreser, Jan Tilmann Vollrath, Antonio Sechi, Sonja Johann, Andreas Roos, Alfred Yamoah, Istvan Katona, Saeed Bohlega, Dominik Wiemuth, Yuemin Tian, Axel Schmidt, Jörg Vervoorts, Marc Dohmen, Cordian Beyer, Jasper Anink, Eleonora Aronica, Dirk Troost, Joachim Weis, Anand Goswami
Amyotrophic lateral sclerosis (ALS) is characterized by the selective degeneration of motor neurons (MNs) and their target muscles. Misfolded proteins which often form intracellular aggregates are a pathological hallmark of ALS. Disruption of the functional interplay between protein degradation (ubiquitin proteasome system and autophagy) and RNA-binding protein homeostasis has recently been suggested as an integrated model that merges several ALS-associated proteins into a common pathophysiological pathway...
June 16, 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/28603497/sigma-1-receptor-plays-a-negative-modulation-on-n-type-calcium-channel
#11
Kang Zhang, Zhe Zhao, Liting Lan, Xiaoli Wei, Liyun Wang, Xiaoyan Liu, Haitao Yan, Jianquan Zheng
The sigma-1 receptor is a 223 amino acids molecular chaperone with a single transmembrane domain. It is resident to eukaryotic mitochondrial-associated endoplasmic reticulum and plasma membranes. By chaperone-mediated interactions with ion channels, G-protein coupled receptors and cell-signaling molecules, the sigma-1 receptor performs broad physiological and pharmacological functions. Despite sigma-1 receptors have been confirmed to regulate various types of ion channels, the relationship between the sigma-1 receptor and N-type Ca(2+) channel is still unclear...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28572528/apex2-enhanced-electron-microscopy-distinguishes-sigma-1-receptor-localization-in-the-nucleoplasmic-reticulum
#12
Timur A Mavlyutov, Huan Yang, Miles L Epstein, Arnold E Ruoho, Jay Yang, Lian-Wang Guo
The sigma-1 receptor (Sig1R) is an endoplasmic reticulum chaperonin that is attracting tremendous interest as a potential anti-neurodegenerative target. While this membrane protein is known to reside in the inner nuclear envelope (NE) and influences transcription, apparent Sig1R presence in the nucleoplasm is often observed, seemingly contradicting its NE localization. We addressed this confounding issue by applying an antibody-free approach of electron microscopy (EM) to define Sig1R nuclear localization. We expressed APEX2 peroxidase fused to Sig1R-GFP in a Sig1R-null NSC34 neuronal cell line generated with CRISPR-Cas9...
May 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28572487/biodistribution-and-radiation-dosimetry-of-18-f-ftc-146-in-humans
#13
Trine Hjørnevik, Peter W Cipriano, Bin Shen, Jun Hyung Park, Praveen Gulaka, Dawn Holley, Harsh Gandhi, Daehyun Yoon, Erik S Mittra, Greg Zaharchuk, Sanjiv S Gambhir, Christopher R McCurdy, Frederick T Chin, Sandip Biswal
The purpose of this study is to assess safety, biodistribution and radiation dosimetry in humans for the highly selective sigma-1 receptor (S1R) positron emission tomography (PET) agent (18)F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[d]thiazol-2(3H)-one ((18)F-FTC-146). Methods: Ten healthy volunteers (HV; five female, five male; age: 34.3 ± 6.5 years) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/magnetic resonance imaging (PET/MRI) examinations were acquired for up to three hours after injection (357...
June 1, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28554311/the-role-of-sigma-1-receptor-an-intracellular-chaperone-in-neurodegenerative-diseases
#14
Botond Penke, Lívia Fülöp, Mária Szűcs, Ede Frecska
Widespread protein aggregation occurs in the living system under stress or during aging, owing to disturbance of endoplasmic reticulum (ER) proteostasis. Many neurodegenerative diseases may have a common mechanism: the failure of protein homeostasis. Perturbation of ER results in unfolded protein response (UPR). Prolonged chronical UPR may activate apoptotic pathways and cause cell death. ER is associated to mitochondria by the mitochondria-associated ER-membrane, MAM. The sigma-1 receptor (Sig-1R), a well-known ER-chaperone localizes in the MAM...
May 28, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28549890/-18-f-labeled-indole-based-analogs-as-highly-selective-radioligands-for-imaging-sigma-2-receptors-in-the-brain
#15
Liang Wang, Jiajun Ye, Yingfang He, Winnie Deuther-Conrad, Jinming Zhang, Xiaojun Zhang, Mengchao Cui, Jörg Steinbach, Yiyun Huang, Peter Brust, Hongmei Jia
We have designed and synthesized a series of indole-based σ2 receptor ligands containing 5,6-dimethoxyisoindoline or 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline as pharmacophore. In vitro competition binding assays showed that all ten ligands possessed low nanomolar affinity (Ki=1.79-5.23nM) for σ2 receptors and high subtype selectivity (Ki (σ2)/Ki (σ1)=56-708). Moreover, they showed high selectivity for σ2 receptor over the vesicular acetylcholine transporter (>1000-fold). The corresponding radiotracers [(18)F]16 and [(18)F]21 were prepared by an efficient one-pot, two-step reaction sequence with a home-made automated synthesis module, with 10-15% radiochemical yield and radiochemical purity of >99%...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549090/sigma-1-receptor-regulates-mitochondrial-function-in-glucose-and-oxygen-deprived-retinal-ganglion-cells
#16
Dorette Z Ellis, Linya Li, Yong Park, Shaoqing He, Brett Mueller, Thomas Yorio
Purpose: Understanding the role of mitochondria in retinal ganglion cells (RGCs) is relevant to human disease as studies have shown mitochondrial abnormalities in primary open-angle glaucoma patients. This study seeks to determine the effects of the sigma-1 receptor (σ-1r) and its agonists on mitochondrial function in oxygen- and glucose- deprived (OGD) purified neonatal RGCs. Methods: Retinal ganglion cells were isolated from rat pups and subjected to OGD in varying conditions in the presence or absence of σ-1r agonist and antagonist and following addition of an AAV2-σ-1r vector that was used to increase σ-1r expression...
May 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28544475/thiazole-based-%C3%AF-1-receptor-ligands-diversity-by-late-stage-c-h-arylation-of-thiazoles-structure-affinity-and-selectivity-relationships-and-molecular-interactions
#17
Artur K Kokornaczyk, Dirk Schepmann, Junichiro Yamaguchi, Kenichiro Itami, Erik Laurini, Maurizio Fermeglia, Sabrina Pricl, Bernhard Wünsch
Spirocyclic thiophene derivatives represent promising σ1 ligands with high σ1 affinity and selectivity over the σ2 subtype. To increase ligand efficiency, the thiophene ring was replaced bioisosterically by a thiazole ring, and the pyran ring was opened. Late-stage diversification by regioselective C-H arylation of thiazoles 9 a-c resulted in a set of 53 compounds with high diversity. This set of compounds was analyzed with respect to σ1 affinity, σ1 /σ2 selectivity, lipophilicity (logD7.4 ), lipophilicity-corrected ligand efficiency (LELP), and molecular target interactions...
May 24, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28525360/role-of-sigma-1-receptor-in-high-fat-diet-induced-peripheral-neuropathy
#18
Tieying Song, Jianhui Zhao, Xiaojing Ma, Zaiwang Zhang, Bo Jiang, Yunliang Yang
The neurobiological mechanisms of obesity-induced peripheral neuropathy are poorly understood. We evaluated the role of Sigma-1 receptor (Sig-1R) and NMDA receptor (NMDARs) in the spinal cord in peripheral neuropathy using an animal model of high fat diet-induced diabetes. We examined the expression of Sig-1R and NMDAR subunits GluN2A and GluN2B along with postsynaptic density protein 95 (PSD-95) in the spinal cord after 24-week HFD treatment in both wild-type and Sig-1R-/- mice. Finally, we examined the effects of repeated intrathecal administrations of selective Sig-1R antagonists BD1047 in HFD-fed wild-type mice on peripheral neuropathy...
June 14, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28495886/the-sigma-1-receptor-modulates-dopamine-transporter-conformation-and-cocaine-binding-and-may-thereby-potentiate-cocaine-self-administration-in-rats
#19
Weimin Conrad Hong, Hideaki Yano, Takato Hiranita, Frederick T Chin, Christopher R McCurdy, Tsung-Ping Su, Susan G Amara, Jonathan L Katz
The dopamine transporter (DAT) regulates dopamine (DA) neurotransmission by recapturing DA into the presynaptic terminals and is a principal target of the psychostimulant cocaine. The sigma-1 receptor (σ1R) is a molecular chaperone, and its ligands have been shown to modulate DA neuronal signaling, although their effects on DAT activity are unclear. Here, we report that the prototypical σ1R agonist (+)-pentazocine potentiated the dose response of cocaine self-administration in rats, consistent with the effects of the σR agonists PRE-084 and DTG (1,3-di-o-tolylguanidine) reported previously...
July 7, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28476021/association-of-body-mass-index-with-er-pr-and-14-3-3%C3%AF-expression-in-tumor-and-stroma-of-type-i-and-type-ii-endometrial-carcinoma
#20
Joseph F Peevey, Brandon-Luke L Seagle, Kruti P Maniar, J Julie Kim
Obesity is a prominent risk factor for endometrial cancer (EC) and can impede on surgical and hormonal treatments. Markers of EC, estrogen receptor (ER), progesterone receptor (PR), phospho(Ser473)-AKT (pAKT) and 14-3-3 sigma (14-3-3σ) were measured in EC tissues in both the tumor and stroma and grouped by body mass index (BMI). Immunohistochemical scoring of 82 cases of Type 1 and Type II EC tissues revealed a significantly increased tumor expression of ER, PR and 14-3-3σ in women with Type I (BMI < 40) as compared to Type II (BMI < 30) EC...
June 27, 2017: Oncotarget
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