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https://www.readbyqxmd.com/read/27910870/antinociceptive-profile-of-levo-tetrahydropalmatine-in-acute-and-chronic-pain-mice-models-role-of-spinal-sigma-1-receptor
#1
Dong-Wook Kang, Ji-Young Moon, Jae-Gyun Choi, Suk-Yun Kang, Yeonhee Ryu, Jin Bong Park, Jang-Hern Lee, Hyun-Woo Kim
We have recently reported that repeated systemic treatments of extract from Corydalis yanhusuo alleviate neuropathic pain and levo-tetrahydropalmatine (l-THP) is one of active components from Corydalis. We designed this study to investigate antinociceptive effect of l-THP in acute and chronic pain models and related mechanism within the spinal cord. We found that intraperitoneal pretreatment with l-THP significantly inhibited the second phase of formalin-induced pain behavior. In addition, intrathecal as well as intraperitoneal pretreatment with l-THP reduced the mechanical allodynia (MA) induced by direct activation of sigma-1 receptor (Sig-1)...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27897342/catalytic-sp3-sp3-functionalisation-of-sulfonamides-late-stage-modification-of-drug-like-molecules
#2
Joseph B Sweeney, Othman Abdulla, Adam Clayton, Robert Faulkner, Duncan Gill, Craig Rice, Scarlett Walton
A new application of Pd-catalysed allylation is reported which enables the synthesis of a range of branched sp3-functionalised sulfonamides, a compound class for which few reported methods exist. By reacting benzyl sulfonamides with allylic acetates in the presence of Pd(0) catalysts and base at room temperature, direct allylation can be efficiently carried out, yielding products which are analogues of structural motifs seen in biologically active small molecules. The reaction is carried out under mild conditions and can be applied to nanomolar sigma-receptor binders, thus enabling a late-stage functionalisation and efficient expansion of drug-like chemical space...
November 29, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27886264/sigma-1-receptor-agonism-promotes-mechanical-allodynia-after-priming-the-nociceptive-system-with-capsaicin
#3
J M Entrena, C Sánchez-Fernández, F R Nieto, R González-Cano, S Yeste, E J Cobos, J M Baeyens
Sigma-1 receptor antagonists promote antinociception in several models of pain, but the effects of sigma-1 agonists on nociception (particularly when the nociceptive system is primed) are not so well characterized; therefore we evaluated the effects of sigma-1 agonists on pain under different experimental conditions. The systemic administration of the selective sigma-1 agonists (+)-pentazocine and PRE-084, as well as the nonselective sigma-1 agonist carbetapentane (used clinically as an antitussive drug), did not alter sensitivity to mechanical stimulation under baseline conditions...
November 25, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27885719/targeting-nanocarriers-with-anisamide-fact-or-artifact
#4
Athanasia Dasargyri, Carole D Kümin, Jean-Christophe Leroux
Encapsulating chemotherapeutics in nanoparticles can reduce the side effects of intravenous administration and improve their antitumor efficacy. Additionally, surface decoration of the nanocarriers with tumor-targeting ligands may enhance their specificity for cancer cells overexpressing the corresponding ligand-binding counterpart. The focus here is on anisamide, a low-molecular-weight benzamide derivative used as a tumor-directing moiety in functionalized nanosystems, based on its alleged interaction with Sigma receptors...
November 25, 2016: Advanced Materials
https://www.readbyqxmd.com/read/27857729/sigma-1-receptor-and-neuroprotection-current-outlook-and-potential-therapeutic-effects
#5
Giovanni Li Volti, Paolo Murabito
No abstract text is available yet for this article.
September 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/27851908/n-phenylpropyl-n-substituted-piperazines-occupy-sigma-receptors-and-alter-methamphetamine-induced-hyperactivity-in-mice
#6
Dennis K Miller, Eric S Park, Susan Z Lever, John R Lever
This study examined the effect of the N-phenylpropyl-N'-substituted piperazine ligands SA4503 (3.4-dimethoxyphenethyl), YZ-067 (4-methoxyphenethyl), YZ-185 (3-methoxyphenethyl) and Nahas-3h (4-methoxybenzyl) on methamphetamine-induced hyperactivity in mice. In a previous study in rats, SA4503 increased methamphetamine-induced hyperactivity at a lower ligand dose and enhanced it at a higher dose. The other ligands have not been investigated in this assay. Presently, mice were administered sigma ligands, and specific [(125)I]E-IA-DM-PE-PIPZE and [(125)I]RTI-121 binding was measured to determine σ1 sigma receptor and dopamine transporter occupancy, respectively...
November 13, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/27829319/effect-of-different-concentrations-of-oxygen-on-expression-of-sigma-1-receptor-and-superoxide-dismutases-in-human-colon-adenocarcinoma-cell-lines
#7
Michał Skrzycki, Hanna Czeczot, Magdalena Mielczarek-Puta, Dagmara Otto-Ślusarczyk, Wojciech Graboń
CONTEXT: Tumor cells due to distance from capillary vessels exist in different oxygenation conditions (anoxia, hypoxia, normoxia). Changes in cell oxygenation lead to reactive oxygen species production and oxidative stress. Sigma 1 receptor (Sig1R) is postulated to be stress responding agent and superoxide dismutases (SOD1 and SOD2) are key antioxidant enzymes. It is possible that they participate in tumor cells adaptation to different concentrations of oxygen. OBJECTIVE: Evaluation of Sig1R, SOD1, and SOD2 expression in different concentrations of oxygen (1%, 10%, 21%) in colon adenocarcinoma cell lines...
November 9, 2016: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/27821430/mitochondria-associated-membrane-collapse-is-a-common-pathomechanism-in-sigmar1-and-sod1-linked-als
#8
Seiji Watanabe, Hristelina Ilieva, Hiromi Tamada, Hanae Nomura, Okiru Komine, Fumito Endo, Shijie Jin, Pedro Mancias, Hiroshi Kiyama, Koji Yamanaka
A homozygous mutation in the gene for sigma 1 receptor (Sig1R) is a cause of inherited juvenile amyotrophic lateral sclerosis (ALS16). Sig1R localizes to the mitochondria-associated membrane (MAM), which is an interface of mitochondria and endoplasmic reticulum. However, the role of the MAM in ALS is not fully elucidated. Here, we identified a homozygous p.L95fs mutation of Sig1R as a novel cause of ALS16. ALS-linked Sig1R variants were unstable and incapable of binding to inositol 1,4,5-triphosphate receptor type 3 (IP3R3)...
December 1, 2016: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/27818324/the-sigma-1-receptor-mediates-the-beneficial-effects-of-pridopidine-in-a-mouse-model-of-huntington-disease
#9
Daniel Ryskamp, Jun Wu, Michal Geva, Rebecca Kusko, Iris Grossman, Michael Hayden, Ilya Bezprozvanny
The tri-nucleotide repeat expansion underlying Huntington disease (HD) results in corticostriatal synaptic dysfunction and subsequent neurodegeneration of striatal medium spiny neurons (MSNs). HD is a devastating autosomal dominant disease with no disease-modifying treatments. Pridopidine, a postulated "dopamine stabilizer", has been shown to improve motor symptoms in clinical trials of HD. However, the target(s) and mechanism of action of pridopidine remain to be fully elucidated. As binding studies identified sigma-1 receptor (S1R) as a high-affinity receptor for pridopidine, we evaluated the relevance of S1R as a therapeutic target of pridopidine in HD...
November 3, 2016: Neurobiology of Disease
https://www.readbyqxmd.com/read/27785538/cholinergic-pet-imaging-in-infections-and-inflammation-using-11-c-donepezil-and-18-f-feobv
#10
Nis Pedersen Jørgensen, Aage K O Alstrup, Frank V Mortensen, Karoline Knudsen, Steen Jakobsen, Line Bille Madsen, Dirk Bender, Peter Breining, Mikkel Steen Petersen, Mariane Høgsberg Schleimann, Frederik Dagnæs-Hansen, Lars C Gormsen, Per Borghammer
INTRODUCTION: Immune cells utilize acetylcholine as a paracrine-signaling molecule. Many white blood cells express components of the cholinergic signaling pathway, and these are up-regulated when immune cells are activated. However, in vivo molecular imaging of cholinergic signaling in the context of inflammation has not previously been investigated. METHODS: We performed positron emission tomography (PET) using the glucose analogue 18F-FDG, and 11C-donepezil and 18F-FEOBV, markers of acetylcholinesterase and the vesicular acetylcholine transporter, respectively...
October 26, 2016: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/27767041/silencing-microrna-143-protects-the-integrity-of-the-blood-brain-barrier-implications-for-methamphetamine-abuse
#11
Ying Bai, Yuan Zhang, Jun Hua, Xiangyu Yang, Xiaotian Zhang, Ming Duan, Xinjian Zhu, Wenhui Huang, Jie Chao, Rongbin Zhou, Gang Hu, Honghong Yao
MicroRNA-143 (miR-143) plays a critical role in various cellular processes; however, the role of miR-143 in the maintenance of blood-brain barrier (BBB) integrity remains poorly defined. Silencing miR-143 in a genetic animal model or via an anti-miR-143 lentivirus prevented the BBB damage induced by methamphetamine. miR-143, which targets p53 unregulated modulator of apoptosis (PUMA), increased the permeability of human brain endothelial cells and concomitantly decreased the expression of tight junction proteins (TJPs)...
October 21, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27761593/creb-decreases-astrocytic-excitability-by-modifying-subcellular-calcium-fluxes-via-the-sigma-1-receptor
#12
A Eraso-Pichot, R Larramona-Arcas, E Vicario-Orri, R Villalonga, L Pardo, E Galea, R Masgrau
Astrocytic excitability relies on cytosolic calcium increases as a key mechanism, whereby astrocytes contribute to synaptic transmission and hence learning and memory. While it is a cornerstone of neurosciences that experiences are remembered, because transmitters activate gene expression in neurons, long-term adaptive astrocyte plasticity has not been described. Here, we investigated whether the transcription factor CREB mediates adaptive plasticity-like phenomena in astrocytes. We found that activation of CREB-dependent transcription reduced the calcium responses induced by ATP, noradrenaline, or endothelin-1...
October 19, 2016: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/27755986/tactics-for-preclinical-validation-of-receptor-binding-radiotracers
#13
Susan Z Lever, Kuo-Hsien Fan, John R Lever
INTRODUCTION: Aspects of radiopharmaceutical development are illustrated through preclinical studies of [(125)I]-(E)-1-(2-(2,3-dihydrobenzofuran-5-yl)ethyl)-4-(iodoallyl)piperazine ([(125)I]-E-IA-BF-PE-PIPZE), a radioligand for sigma-1 (σ1) receptors, coupled with examples from the recent literature. Findings are compared to those previously observed for [(125)I]-(E)-1-(2-(2,3-dimethoxy-5-yl)ethyl)-4-(iodoallyl)piperazine ([(125)I]-E-IA-DM-PE-PIPZE). METHODS: Syntheses of E-IA-BF-PE-PIPZE and [(125)I]-E-IA-BF-PE-PIPZE were accomplished by standard methods...
September 3, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27738380/treatment-resistant-depression-with-loss-of-antidepressant-response-rapid-acting-antidepressant-action-of-dextromethorphan-a-possible-treatment-bridging-molecule
#14
Edward C Lauterbach
Dextromethorphan (DM) may have ketamine-like rapid-acting, treatment-resistant, and conventional antidepressant effects.(1,2) This reports our initial experience with DM in unipolar Major Depressive Disorder (MDD). A patient with treatment-resistant MDD (failing adequate trials of citalopram and vortioxetine) with loss of antidepressant response (to fluoxetine and bupropion) twice experienced a rapid-acting antidepressant effect within 48 hours of DM administration and lasting 7 days, sustained up to 20 days with daily administration, then gradually developing labile loss of antidepressant response over the ensuing 7 days...
August 15, 2016: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/27735948/transactivation-of-trkb-by-sigma-1-receptor-mediates-cocaine-induced-changes-in-dendritic-spine-density-and-morphology-in-hippocampal-and-cortical-neurons
#15
Minhan Ka, Yeon-Hee Kook, Ke Liao, Shilpa Buch, Woo-Yang Kim
Cocaine is a highly addictive narcotic associated with dendritic spine plasticity in the striatum. However, it remains elusive whether cocaine modifies spines in a cell type-specific or region-specific manner or whether it alters different types of synapses in the brain. In addition, there is a paucity of data on the regulatory mechanism(s) involved in cocaine-induced modification of spine density. In the current study, we report that cocaine exposure differentially alters spine density, spine morphology, and the types of synapses in hippocampal and cortical neurons...
October 13, 2016: Cell Death & Disease
https://www.readbyqxmd.com/read/27714195/a-systematic-exploration-of-the-effects-of-flexibility-and-basicity-on-sigma-%C3%AF-receptor-binding-in-a-series-of-substituted-diamines
#16
Trent Conroy, Madhura Manohar, Yu Gong, Shane M Wilkinson, Michael Webster, Brian P Lieberman, Samuel D Banister, Tristan A Reekie, Robert H Mach, Louis M Rendina, Michael Kassiou
The sigma-1 receptor (S1R) has attracted a great deal of attention as a prospective drug target due to its involvement in numerous neurological disorders and, more recently, for its therapeutic potential in neuropathic pain. As there was no crystal structure of this membrane-bound protein reported until 2016, ligand generation was driven by pharmacophore refinements to the general model suggested by Glennon and co-workers. The generalised S1R pharmacophore comprises a central region where a basic amino group is preferred, flanked by two hydrophobic groups...
October 4, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27697534/emerging-roles-of-the-neurotrophin-receptor-trkc-in-synapse-organization
#17
Yusuke Naito, Alfred Kihoon Lee, Hideto Takahashi
Tropomyosin-receptor-kinase (Trk) receptors have been extensively studied for their roles in kinase-dependent signaling cascades in nervous system development. Synapse organization is coordinated by trans-synaptic interactions of various cell adhesion proteins, a representative example of which is the neurexin-neuroligin complex. Recently, a novel role for TrkC as a synapse organizing protein has been established. Post-synaptic TrkC binds to pre-synaptic type-IIa receptor-type protein tyrosine phosphatase sigma (PTPσ)...
September 30, 2016: Neuroscience Research
https://www.readbyqxmd.com/read/27683542/the-endogenous-hallucinogen-and-trace-amine-n-n-dimethyltryptamine-dmt-displays-potent-protective-effects-against-hypoxia-via-sigma-1-receptor-activation-in-human-primary-ipsc-derived-cortical-neurons-and-microglia-like-immune-cells
#18
Attila Szabo, Attila Kovacs, Jordi Riba, Srdjan Djurovic, Eva Rajnavolgyi, Ede Frecska
N,N-dimethyltryptamine (DMT) is a potent endogenous hallucinogen present in the brain of humans and other mammals. Despite extensive research, its physiological role remains largely unknown. Recently, DMT has been found to activate the sigma-1 receptor (Sig-1R), an intracellular chaperone fulfilling an interface role between the endoplasmic reticulum (ER) and mitochondria. It ensures the correct transmission of ER stress into the nucleus resulting in the enhanced production of antistress and antioxidant proteins...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27673755/evaluation-of-pancreatic-vmat2-binding-with-active-and-inactive-enantiomers-of-18-f-fp-dtbz-in-baboons
#19
Mika Naganawa, Shu-Fei Lin, Keunpoong Lim, David Labaree, Jim Ropchan, Paul Harris, Yiyun Huang, Masanori Ichise, Richard E Carson, Gary W Cline
INTRODUCTION: (18)F-Fluoropropyl-(+)-dihydrotetrabenazine ((18)F-FP-(+)-DTBZ) is a vesicular monoamine transporter type 2 (VMAT2) radiotracer for positron emission tomography (PET) imaging to quantify human β-cell mass. Renal cortex and spleen have been suggested as reference regions, however, little is known about (18)F-FP-(+)-DTBZ binding in these regions including the fraction of radiometabolite. We compared the kinetics of (18)F-FP-(+)-DTBZ and its inactive enantiomer (18)F-FP-(-)-DTBZ in baboons, estimated the non-displaceable binding (VND) of the tracers, and used ex vivo studies to measure radiometabolite fractions...
December 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27671118/hb-gam-pleiotrophin-reverses-inhibition-of-neural-regeneration-by-the-cns-extracellular-matrix
#20
Mikhail Paveliev, Keith K Fenrich, Mikhail Kislin, Juha Kuja-Panula, Evgeny Kulesskiy, Markku Varjosalo, Tommi Kajander, Ekaterina Mugantseva, Anni Ahonen-Bishopp, Leonard Khiroug, Natalia Kulesskaya, Geneviève Rougon, Heikki Rauvala
Chondroitin sulfate (CS) glycosaminoglycans inhibit regeneration in the adult central nervous system (CNS). We report here that HB-GAM (heparin-binding growth-associated molecule; also known as pleiotrophin), a CS-binding protein expressed at high levels in the developing CNS, reverses the role of the CS chains in neurite growth of CNS neurons in vitro from inhibition to activation. The CS-bound HB-GAM promotes neurite growth through binding to the cell surface proteoglycan glypican-2; furthermore, HB-GAM abrogates the CS ligand binding to the inhibitory receptor PTPσ (protein tyrosine phosphatase sigma)...
September 27, 2016: Scientific Reports
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