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Sigma 1 receptor

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https://www.readbyqxmd.com/read/29297590/involvement-of-the-delayed-rectifier-outward-potassium-channel-kv2-1-in-methamphetamine-induced-neuronal-apoptosis-via-the-p38-mitogen-activated-protein-kinase-signaling-pathway
#1
Jingying Zhu, Songsong Zang, Xufeng Chen, Lei Jiang, Aihua Gu, Jie Cheng, Li Zhang, Jun Wang, Hang Xiao
Methamphetamine (Meth) is an illicit psychostimulant with high abuse potential and severe neurotoxicity. Recent studies have shown that dysfunctions in learning and memory induced by Meth may partially reveal the mechanisms of neuronal channelopathies. Kv2.1, the primary delayed rectifying potassium channel in neurons, is responsible for mediating apoptotic current surge. However, whether Kv2.1 is involved in Meth-mediated neural injury remains unknown. In the present study, the treatment of primary cultured hippocampal neurons with Meth indicated that Meth induced a time- and dose-dependent augmentation of Kv2...
January 3, 2018: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29291374/af710b-an-m1-sigma-1-receptor-agonist-with-long-lasting-disease-modifying-properties-in-a-transgenic-rat-model-of-alzheimer-s-disease
#2
Hélène Hall, M Florencia Iulita, Palma Gubert, Lisi Flores Aguilar, Adriana Ducatenzeiler, Abraham Fisher, A Claudio Cuello
INTRODUCTION: AF710B (aka ANAVEX 3-71) is a novel selective allosteric M1 muscarinic and sigma-1 receptor agonist. In 3×Tg-AD mice, AF710B attenuates cognitive deficits and decreases Alzheimer-like hallmarks. We now report on the long-lasting disease-modifying properties of AF710B in McGill-R-Thy1-APP transgenic (Tg) rats. METHODS: Chronic treatment with AF710B (10 μg/kg) was initiated in postplaque 13-month-old Tg rats. Drug or vehicle was administered orally daily for 4...
December 29, 2017: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
https://www.readbyqxmd.com/read/29289721/spinal-sigma-1-receptor-mediated-dephosphorylation-of-astrocytic-aromatase-plays-a-key-role-in-formalin-induced-inflammatory-nociception
#3
Hoon-Seong Choi, Mi-Ji Lee, Sheu-Ran Choi, Branden A Smeester, Alvin J Beitz, Jang-Hern Lee
Aromatase is a key enzyme responsible for the biosynthesis of estrogen from testosterone. Although recent evidence indicates that spinal cord aromatase participates in nociceptive processing, the mechanisms underlying its regulation and its involvement in nociception remain unclear. The present study focuses on the potential role of astrocyte aromatase in formalin-induced acute pain and begins to uncover one mechanism by which spinal aromatase activation is controlled. Following intraplantar formalin injection, nociceptive responses were quantified and immunohistochemistry/co-immunoprecipitation assays were used to investigate the changes in spinal Fos expression and the phospho-serine levels of spinal aromatase...
December 28, 2017: Neuroscience
https://www.readbyqxmd.com/read/29287249/multifunctional-thiosemicarbazones-and-deconstructed-analogues-as-a-strategy-to-study-the-involvement-of-metal-chelation-sigma-2-%C3%AF-2-receptor-and-p-gp-protein-in-the-cytotoxic-action-in%C3%A2-vitro-and-in%C3%A2-vivo-activity-in-pancreatic-tumors
#4
Maria Laura Pati, Mauro Niso, Dirk Spitzer, Francesco Berardi, Marialessandra Contino, Chiara Riganti, William G Hawkins, Carmen Abate
The aggressiveness of pancreatic cancer urgently requires more efficient treatment options. Because the sigma-2 (σ2) receptor was recently proposed as a promising target for pancreatic cancer therapy, we explored our previously developed multifunctional thiosemicarbazones, designed to synergistically impair cell energy levels, by targeting σ2 and P-gp proteins and chelating Iron. A deconstruction approach was herein applied by removing one function at a time from the potent multifunctional thiosemicarbazones 1 and 2, to investigate the contribution to cytotoxicity of each target involved...
December 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29273047/donepezil-suppresses-intracellular-ca2-mobilization-through-the-pi3k-pathway-in-rodent-microglia
#5
Yoshinori Haraguchi, Yoshito Mizoguchi, Masahiro Ohgidani, Yoshiomi Imamura, Toru Murakawa-Hirachi, Hiromi Nabeta, Hiroshi Tateishi, Takahiro A Kato, Akira Monji
BACKGROUND: Microglia are resident innate immune cells which release many factors including proinflammatory cytokines or nitric oxide (NO) when they are activated in response to immunological stimuli. Pathophysiology of Alzheimer's disease (AD) is related to the inflammatory responses mediated by microglia. Intracellular Ca2+ signaling is important for microglial functions such as release of NO and cytokines. In addition, alteration of intracellular Ca2+ signaling underlies the pathophysiology of AD, while it remains unclear how donepezil, an acetylcholinesterase inhibitor, affects intracellular Ca2+ mobilization in microglial cells...
December 22, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29238093/circhipk2-mediated-%C3%AF-1r-promotes-endoplasmic-reticulum-stress-in-human-pulmonary-fibroblasts-exposed-to-silica
#6
Zhouli Cao, Qingling Xiao, Xiaoniu Dai, Zewei Zhou, Rong Jiang, Yusi Cheng, Xiyue Yang, Huifang Guo, Jing Wang, Zhaoqing Xi, Honghong Yao, Jie Chao
Silicosis is characterized by fibroblast accumulation and excessive deposition of extracellular matrix. Although the roles of SiO2-induced chemokines and cytokines released from alveolar macrophages have received significant attention, the direct effects of SiO2 on protein production and functional changes in pulmonary fibroblasts have been less extensively studied. Sigma-1 receptor, which has been associated with cell proliferation and migration in the central nervous system, is expressed in the lung, but its role in silicosis remains unknown...
December 13, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/29226684/quantum-dot-based-luminescent-nanoprobes-for-sigma-2-receptor-imaging
#7
Maria Laura Pati, Elisabetta Fanizza, Sonja Hager, Diana Groza, Petra Heffeter, Amelita Grazia Laurenza, Valentino Laquintana, Maria Lucia Curri, Nicoletta Depalo, Carmen Abate, Nunzio Denora
The increasing importance of sigma-2 receptor as target for the diagnosis and therapy of tumours paves the way for the development of innovative optically traceable fluorescent probes as tumour cell contrast and therapeutic agents. Here, a novel hybrid organic-inorganic nanostructure is developed by combining the superior fluorescent properties of inorganic quantum dots (QDs), coated with a hydrophilic silica shell (QD@SiO2 NPs), the versatility of the silica shell and the high selectivity for sigma-2 receptors of the two synthetic ligands, namely the 6-[(6-aminohexyl)oxy]-2-(3-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propyl)-3,4-dihydroisoquinolin-1(2H)-one (MLP66) and 6-[1-[3-(4-cyclohexylpiperazin-1-yl)propyl]-1,2,3,4-tetrahydronaphthalen-5-yloxy]hexylamine (TA6)...
December 11, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29220177/-methyl-1r-2s-2-4-4-chlorophenyl-4-hydroxypiperidin-1-yl-methyl-1-phenylcyclopropanecarboxylate-mr200-derivatives-as-potent-and-selective-sigma-receptor-ligands-stereochemistry-and-pharmacological-properties
#8
Emanuele Amata, Antonio Rescifina, Orazio Prezzavento, Emanuela Arena, Maria Dichiara, Valeria Pittalà, Ángeles Montilla-García, Francesco Punzo, Pedro Merino, Enrique J Cobos, Agostino Marrazzo
Methoxycarbonyl-1-phenyl-2-cyclopropylmethyl based derivatives cis-(+)-1a [cis-(+)-MR200], cis-(-)-1a [cis-(-)-MR201], and trans-(±)-1a [trans-(±)-MR204], have been identified as new potent sigma (σ) receptor ligands. In the present paper, novel enantiomerically pure analogues were synthesized and optimized for their σ receptor affinity and selectivity. Docking studies rationalized the results obtained in the radioligand binding assay. Absolute stereochemistry was unequivocally established by X-ray analysis of precursor trans-(+)-5a as camphorsulfonyl derivative 9...
December 8, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29212933/characterization-of-an-influenza-virus-pseudotyped-with-ebolavirus-glycoprotein
#9
Julie Xiao, Pramila Rijal, Lisa Schimanski, Arun Kumar Tharkeshwar, Edward Wright, Wim Annaert, Alain Townsend
We have produced a new Ebola virus pseudotype: E-S-FLU, which can be handled in biosafety level-1/2 containment for laboratory analysis. E-S-FLU is a single cycle influenza virus coated with Ebolavirus glycoprotein, and it encodes enhanced green fluorescence protein as a reporter that replaces the influenza haemagglutinin. MDCK-SIAT1 cells were transduced to express Ebolavirus glycoprotein as a stable transmembrane protein for E-S-FLU production. Infection of cells by E-S-FLU was dependent on Niemann-Pick C1 protein, which is the well-characterized receptor for Ebola virus entry at the late endosome/lysosome membrane...
December 6, 2017: Journal of Virology
https://www.readbyqxmd.com/read/29207628/sigma-1-and-sigma-2-receptor-ligands-induce-apoptosis-and-autophagy-but-have-opposite-effect-on-cell-proliferation-in-uveal-melanoma
#10
Lucia Longhitano, Carlo Castruccio Castracani, Daniele Tibullo, Roberto Avola, Maria Viola, Giuliano Russo, Orazio Prezzavento, Agostino Marrazzo, Emanuele Amata, Michele Reibaldi, Antonio Longo, Andrea Russo, Nunziatina Laura Parrinello, Giovanni Li Volti
Uveal melanoma is the most common primary intraocular tumor in adults, with about 1200-1500 new cases occurring per year in the United States. Metastasis is a frequent occurrence in uveal melanoma, and outcomes are poor once distant spread occurs and no clinically significant chemotherapeutic protocol is so far available. The aim of the present study was to test the effect of various σ1 and σ2 receptor ligands as a possible pharmacological strategy for this rare tumor. Human uveal melanoma cells (92.1) were treated with various concentrations of different σ2 ligands (haloperidol and haloperidol metabolite II) and σ1 ligand ((+)-pentazocine) at various concentrations (1, 10 and 25 μM) and time points (0, 4 h, 8 h, 24 h and 48 h)...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29202454/fentanyl-related-designer-drugs-w-18-and-w-15-lack-appreciable-opioid-activity-in-vitro-and-in-vivo
#11
Xi-Ping Huang, Tao Che, Thomas J Mangano, Valerie Le Rouzic, Ying-Xian Pan, Michael D Cameron, Michael H Baumann, Gavril W Pasternak, Bryan L Roth
W-18 (4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide) and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide). Here, we describe the comprehensive pharmacological profiles of W-18 and W-15, as examination of their structural features predicted that they might lack opioid activity. We found W-18 and W-15 to be without detectible activity at μ, δ, κ, and nociception opioid receptors in a variety of assays...
November 16, 2017: JCI Insight
https://www.readbyqxmd.com/read/29191857/evaluation-of-11c-me-nb1-as-a-potential-pet-radioligand-for-measuring-glun2b-containing-nmda-receptors-drug-occupancy-and-receptor-crosstalk
#12
Stefanie D Krämer, Thomas Betzel, Linjing Mu, Ahmed Haider, Adrienne Herde Müller, Anna K Boninsegni, Claudia Keller, Marina Szermerski, Roger Schibli, Bernhard Wünsch, Simon M Ametamey
Clinical and preclinical research with modulators binding to the NMDA receptor GluN2B N-terminal domain (NTD) aim for the treatment of various neurological diseases. However, the interpretation of the results is hampered by the lack of a suitable NMDA PET tracer for assessing the receptor occupancy of candidate drugs. We have developed [11C]Me-NB1 as a PET tracer for imaging GluN1/GluN2B-containing NMDA receptors and used it to investigate in rats the dose-dependent receptor occupancy of eliprodil, a GluN2B NTD modulator...
November 30, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29185346/novel-sigma-1-receptor-antagonists-from-opioids-to-small-molecules-what-is-new
#13
Emanuela Arena, Maria Dichiara, Giuseppe Floresta, Carmela Parenti, Agostino Marrazzo, Valeria Pittalà, Emanuele Amata, Orazio Prezzavento
Sigma-1 (σ1) receptor has been identified as a chaperone protein that interacts with other proteins, such as N-methyl-D-aspartate (NMDA) and opioid receptors, modulating their activity. σ1 receptor antagonists have been developed to obtain useful compounds for the treatment of psychoses, pain, drug abuse and cancer. Some interesting compounds such as E-5842 (5) and MS-377 (24), haloperidol and piperazine derivatives, respectively, were endowed with high affinity for σ1 receptors (Ki σ1 = 4 and 73 nM; Ki σ2 = 220 and 6900, respectively)...
November 29, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29172248/differential-involvement-of-ipsilateral-and-contralateral-spinal-cord-astrocyte-d-serine-in-carrageenan-induced-mirror-image-pain-role-of-sigma-1-receptors-and-astrocyte-gap-junctions
#14
Hoon-Seong Choi, Dae-Hyun Roh, Seo-Yeon Yoon, Sheu-Ran Choi, Soon-Gu Kwon, Suk-Yun Kang, Ji-Young Moon, Ho-Jae Han, Alvin J Beitz, Jang-Hern Lee
BACKGROUND AND PURPOSE: Although we have recently demonstrated that spinal astrocyte gap junctions mediate the development of mirror-image pain (MIP), it is still unclear which astrocyte-derived factor is responsible for the development of MIP and how its production is controlled. In the present study, we focused on the role of ipsilateral versus contralateral D-serine in the development of MIP and investigated the possible involvement of sigma-1 receptors and gap junctions in astrocyte D-serine production...
November 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29129596/amyloid-toxicity-is-enhanced-after-pharmacological-or-genetic-invalidation-of-the-%C3%AF-1-receptor
#15
Tangui Maurice, Manon Strehaiano, Fanny Duhr, Nathalie Chevallier
The sigma-1 receptor (S1R) is a molecular chaperone which activity modulates several intracellular signals including calcium mobilization at mitochondria-associated endoplasmic reticulum membranes. S1R agonists are potent neuroprotectants against neurodegenerative insults and particularly in rodent models of Alzheimer's disease (AD). We here analyzed whether S1R inactivation modifies vulnerability to amyloid toxicity in AD models. Two strategies were used: (1) amyloid β[25-35] (Aβ25-35) peptide (1, 3, 9nmol) was injected intracerebroventricularly in mice treated repeatedly with the S1R antagonist NE-100 or in S1RKO mice, and (2) WT, APPSweInd, S1RKO, and APPSweInd/S1RKO mice were created and female littermates analyzed at 8 months of age...
November 9, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29127580/sigma-1-receptor-agonists-induce-oxidative-stress-in-mitochondria-and-enhance-complex-i-activity-in-physiological-condition-but-protect-against-pathological-oxidative-stress
#16
Nino Goguadze, Elene Zhuravliova, Didier Morin, Davit Mikeladze, Tangui Maurice
The sigma1 receptor (σ1R) is a chaperone protein residing at mitochondria-associated endoplasmic reticulum (ER) membranes (MAMs), where it modulates Ca(2+) exchange between the ER and mitochondria by interacting with inositol-1,4,5 trisphosphate receptors (IP3Rs). The σ1R is highly expressed in the central nervous system and its activation stimulates neuromodulation and neuroprotection, for instance in Alzheimer's disease (AD) models in vitro and in vivo. σ1R effects on mitochondria pathophysiology and the downstream signaling are still not fully understood...
November 10, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29117944/small-molecule-sigma1-modulator-induces-autophagic-degradation-of-pd-l1
#17
Christina M Maher, Jeffrey D Thomas, Derick A Haas, Charles G Longen, Halley M Oyer, Jane Y Tong, Felix J Kim
Emerging evidence suggests that Sigma1 (SIGMAR1, also known as sigma-1 receptor) is a unique ligand-regulated integral membrane scaffolding protein that contributes to cellular protein and lipid homeostasis. Previously, we demonstrated that some small molecule modulators of Sigma1 alter endoplasmic reticulum (ER) associated protein homeostasis pathways in cancer cells, including the unfolded protein response and autophagy. Programmed death-ligand 1 (PD-L1) is a type 1 integral membrane glycoprotein that is co-translationally inserted into the ER and is processed and transported through the secretory pathway...
November 8, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/29115704/recessive-distal-motor-neuropathy-with-pyramidal-signs-in-an-omani-kindred-underlying-novel-mutation-in-the-sigmar1-gene
#18
Ramachandiran Nandhagopal, Douja Meftah, Sami Al-Kalbani, Patrick Scott
BACKGROUND: Distal hereditary motor neuropathy (dHMN) due to sigma nonopiod intracellular receptor 1 gene (SIGMAR1) mutation (OMIM 601978.0003) is a rare neuromuscular disorder characterized by prominent amyotrophic distal limb weakness and co-existing pyramidal signs initially described in a Chinese family in the recent year. We report an extended consanguineous Omani family segregating dHMN with pyramidal signs in an autosomal recessive pattern and describe a novel mutation in the SIGMAR1 gene underlying this motor phenotype...
November 8, 2017: European Journal of Neurology: the Official Journal of the European Federation of Neurological Societies
https://www.readbyqxmd.com/read/29110212/selective-blockade-of-the-sigma-1-receptor-has-beneficial-effects-on-both-acute-and-chronic-oxaliplatin-induced-peripheral-neuropathy
#19
EDITORIAL
Susan G Dorsey
No abstract text is available yet for this article.
November 6, 2017: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/29097161/a-behavioral-and-pharmacological-characterization-of-palatable-diet-alternation-in-mice
#20
Catherine F Moore, Gabrielle S Schlain, Samantha Mancino, Valentina Sabino, Pietro Cottone
Obesity and eating disorders are widespread in Western societies. Both the increased availability of highly palatable foods and dieting are major risk factors contributing to the epidemic of disorders of feeding. The purpose of this study was to characterize an animal model of maladaptive feeding induced by intermittent access to a palatable diet alternation in mice. In this study, mice were either continuously provided with standard chow food (Chow/Chow), or provided with standard chow for 2days and a high-sucrose, palatable food for 1day (Chow/Palatable)...
October 31, 2017: Pharmacology, Biochemistry, and Behavior
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