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Sigma 1 receptor

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https://www.readbyqxmd.com/read/29767748/glial-activation-and-central-synapse-loss-but-not-motoneuron-degeneration-are-prevented-by-the-sigma-1-receptor-agonist-pre-084-in-the-smn2b-mouse-model-of-spinal-muscular-atrophy
#1
Clàudia Cerveró, Alba Blasco, Olga Tarabal, Anna Casanovas, Lídia Piedrafita, Xavier Navarro, Josep E Esquerda, Jordi Calderó
Spinal muscular atrophy (SMA) is characterized by the loss of α-motoneurons (MNs) with concomitant muscle denervation. MN excitability and vulnerability to disease are particularly regulated by cholinergic synaptic afferents (C-boutons), in which Sigma-1 receptor (Sig1R) is concentrated. Alterations in Sig1R have been associated with MN degeneration. Here, we investigated whether a chronic treatment with the Sig1R agonist PRE-084 was able to exert beneficial effects on SMA. We used a model of intermediate SMA, the Smn2B/- mouse, in which we performed a detailed characterization of the histopathological changes that occur throughout the disease...
May 14, 2018: Journal of Neuropathology and Experimental Neurology
https://www.readbyqxmd.com/read/29728649/small-molecule-modulators-of-%C3%AF-2r-tmem97-reduce-alcohol-withdrawal-induced-behaviors
#2
Luisa L Scott, James J Sahn, Antonio Ferragud, Rachel C Yen, Praveen N Satarasinghe, Michael D Wood, Timothy R Hodges, Ted Shi, Brooke A Prakash, Kaitlyn M Friese, Angela Shen, Valentina Sabino, Jonathan T Pierce, Stephen F Martin
Repeated cycles of intoxication and withdrawal enhance the negative reinforcing properties of alcohol and lead to neuroadaptations that underlie withdrawal symptoms driving alcohol dependence. Pharmacotherapies that target these neuroadaptations may help break the cycle of dependence. The sigma-1 receptor (σ1R) subtype has attracted interest as a possible modulator of the rewarding and reinforcing effects of alcohol. However, whether the sigma-2 receptor, recently cloned and identified as transmembrane protein 97 (σ2R/TMEM97), plays a role in alcohol-related behaviors is currently unknown...
April 20, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29704822/development-of-a-novel-radiobromine-labeled-sigma-1-receptor-imaging-probe
#3
Kazuma Ogawa, Ryohei Masuda, Yoshiaki Mizuno, Akira Makino, Takashi Kozaka, Yoji Kitamura, Yasushi Kiyono, Kazuhiro Shiba, Akira Odani
INTRODUCTION: Sigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 receptor, and synthesized radiobrominated (+)-pBrV. This radiobrominated (+)-pBrV showed high tumor uptake in tumor-bearing mice; however, radioactivity accumulation in normal tissues, such as the liver, was high. We assumed that the accumulation of (+)-pBrV in the non-target tissues was partially derived from its high lipophilicity; therefore, we synthesized and evaluated (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-bromophenol [(+)-BrV-OH], which is a more hydrophilic compound...
April 6, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29692729/pridopidine-reverses-phencyclidine-induced-memory-impairment
#4
Kristoffer Sahlholm, Marta Valle-León, Víctor Fernández-Dueñas, Francisco Ciruela
Pridopidine is in clinical trials for Huntington's disease treatment. Originally developed as a dopamine D2 receptor (D2 R) ligand, pridopidine displays about 100-fold higher affinity for the sigma-1 receptor (sigma-1R). Interestingly, pridopidine slows disease progression and improves motor function in Huntington's disease model mice and, in preliminarily reports, Huntington's disease patients. The present study examined the anti-amnesic potential of pridopidine. Thus, memory impairment was produced in mice by administration of phencyclidine (PCP, 10 mg/kg/day) for 10 days, followed by 14 days' treatment with pridopidine (6 mg/kg/day), or saline...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29682701/selective-effects-of-5-ht2c-receptor-modulation-on-performance-of-a-novel-valence-probe-visual-discrimination-task-and-probabilistic-reversal-learning-in-mice
#5
Benjamin U Phillips, Sigma Dewan, Simon R O Nilsson, Trevor W Robbins, Christopher J Heath, Lisa M Saksida, Timothy J Bussey, Johan Alsiö
RATIONALE: Dysregulation of the serotonin (5-HT) system is a pathophysiological component in major depressive disorder (MDD), a condition closely associated with abnormal emotional responsivity to positive and negative feedback. However, the precise mechanism through which 5-HT tone biases feedback responsivity remains unclear. 5-HT2C receptors (5-HT2CRs) are closely linked with aspects of depressive symptomatology, including abnormalities in reinforcement processes and response to stress...
April 22, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29674970/hypothesis-the-psychedelic-ayahuasca-heals-traumatic-memories-via-a-sigma-1-receptor-mediated-epigenetic-mnemonic-process
#6
Antonio Inserra
Ayahuasca ingestion modulates brain activity, neurotransmission, gene expression and epigenetic regulation. N,N -Dimethyltryptamine (DMT, one of the alkaloids in Ayahuasca) activates sigma 1 receptor (SIGMAR1) and others. SIGMAR1 is a multi-faceted stress-responsive receptor which promotes cell survival, neuroprotection, neuroplasticity, and neuroimmunomodulation. Simultaneously, monoamine oxidase inhibitors (MAOIs) also present in Ayahuasca prevent the degradation of DMT. One peculiarity of SIGMAR1 activation and MAOI activity is the reversal of mnemonic deficits in pre-clinical models...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29671217/cyproheptadine-regulates-pyramidal-neuron-excitability-in-mouse-medial-prefrontal-cortex
#7
Yan-Lin He, Kai Wang, Qian-Ru Zhao, Yan-Ai Mei
Cyproheptadine (CPH), a first-generation antihistamine, enhances the delayed rectifier outward K+ current (IK ) in mouse cortical neurons through a sigma-1 receptor-mediated protein kinase A pathway. In this study, we aimed to determine the effects of CPH on neuronal excitability in current-clamped pyramidal neurons in mouse medial prefrontal cortex slices. CPH (10 µmol/L) significantly reduced the current density required to generate action potentials (APs) and increased the instantaneous frequency evoked by a depolarizing current...
April 18, 2018: Neuroscience Bulletin
https://www.readbyqxmd.com/read/29660915/hemorheological-and-metabolic-consequences-of-renal-ischemia-reperfusion-and-their-modulation-by-n-n-dimethyl-tryptamine-on-a-rat-model
#8
Katalin Peto, Norbert Nemeth, Anita Mester, Zsuzsanna Magyar, Souleiman Ghanem, Viktoria Somogyi, Bence Tanczos, Adam Deak, Laszlo Bidiga, Ede Frecska, Balazs Nemes
BACKGROUND: Micro-rheological relations of renal ischemia-reperfusion (I/R) have not been completely elucidated yet. Concerning anti-inflammatory agents, it is supposed that sigma-1 receptor agonist N,N-dimethyl-tryptamin (DMT) can be useful to reduce I/R injury. OBJECTIVE: To investigate the micro-rheological and metabolic parameters, and the effects of DMT in renal I/R in rats. METHODS: In anesthetized rats from median laparotomy both kidneys were exposed...
April 13, 2018: Clinical Hemorheology and Microcirculation
https://www.readbyqxmd.com/read/29656199/investigating-isoindoline-tetrahydroisoquinoline-and-tetrahydrobenzazepine-scaffolds-for-their-sigma-receptor-binding-properties
#9
Kathryn Linkens, Hayden R Schmidt, James J Sahn, Andrew C Kruse, Stephen F Martin
Substituted norbenzomorphans are known to display high affinity and selectivity for the two sigma receptor (σR) subtypes. In order to study the effects of simplifying the structures of these compounds, a scaffold hopping strategy was used to design several novel sets of substituted isoindolines, tetrahydroisoquinolines and tetrahydro-2-benzazepines. The binding affinities of these new compounds for the sigma 1 (σ1R) and sigma 2 (σ2R) receptors were determined, and some analogs were identified that exhibit high affinity (Ki  ≤ 25 nM) and significant selectivity (>10-fold) for σ1R or σ2R...
March 29, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29624527/dezocine-alleviates-morphine-induced-dependence-in-rats
#10
Fei-Xiang Wu, Hasan Babazada, Hao Gao, Xi-Ping Huang, Chun-Hua Xi, Chun-Hua Chen, Jin Xi, Wei-Feng Yu, Renyu Liu
BACKGROUND: Opioid dependence is a major public health issue without optimal therapeutics. This study investigates the potential therapeutic effect of dezocine, a nonaddictive opioid, in opioid dependence in rat models. METHODS: Dezocine was administered intraperitoneally to a morphine-dependent rat model to investigate its effect on withdrawal and conditioned place preference (CPP). Effect of dezocine on morphine withdrawal syndrome and CPP was analyzed using 2-way analysis of variance (ANOVA) followed by Tukey's post hoc test...
April 5, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29597271/peg-400-cerium-ammonium-nitrate-combined-with-microwave-assisted-synthesis-for-rapid-access-to-beta-amino-ketones-an-easy-to-use-protocol-for-discovering-new-hit-compounds
#11
Giacomo Rossino, Maria Valeria Raimondi, Marta Rui, Marcello Di Giacomo, Daniela Rossi, Simona Collina
Compound libraries are important requirement in target-based drug discovery. In the present work, a small focused compound library based on β-aminoketone scaffold has been prepared combining microwave-assisted organic synthesis (MAOS) with polymer-assisted solution phase synthesis (PASPS) and replacing reaction workup standard purification procedures with solid phase extraction (SPE). Specifically, the effects of solvent, such as dioxane, dimethylformamide (DMF), polyethylene glycol 400 (PEG 400), temperature, irradiation time, stoichiometric ratio of reagents, and catalysts (HCl, acetic acid, cerium ammonium nitrate (CAN)) were investigated to maximize both conversion and yield...
March 28, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29589276/dipentylammonium-binds-to-the-sigma-1-receptor-and-protects-against-glutamate-toxicity-attenuates-dopamine-toxicity-and-potentiates-neurite-outgrowth-in-various-cultured-cell-lines
#12
James M Brimson, Stephen T Safrany, Heider Qassam, Tewin Tencomnao
Alzheimer's disease is a neurodegenerative disease that affects 44 million people worldwide, costing the world $605 billion to care for those affected not taking into account the physical and psychological costs for those who care for Alzheimer's patients. Dipentylammonium is a simple amine, which is structurally similar to a number of other identified sigma-1 receptor ligands with high affinities such as (2R-trans)-2butyl-5-heptylpyrrolidine, stearylamine and dodecylamine. This study investigates whether dipentylammonium is able to provide neuroprotective effects similar to those of sigma-1 receptor agonists such as PRE-084...
March 27, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29580951/modality-specific-peripheral-antinociceptive-effects-of-%C3%AE-opioid-agonists-on-heat-and-mechanical-stimuli-contribution-of-sigma-1-receptors
#13
Ángeles Montilla-García, Gloria Perazzoli, Miguel Á Tejada, Rafael González-Cano, Cristina Sánchez-Fernández, Enrique J Cobos, José M Baeyens
Morphine induces peripherally μ-opioid-mediated antinociception to heat but not to mechanical stimulation. Peripheral sigma-1 receptors tonically inhibit μ-opioid antinociception to mechanical stimuli, but it is unknown whether they modulate μ-opioid heat antinociception. We hypothesized that sigma-1 receptors might play a role in the modality-specific peripheral antinociceptive effects of morphine and other clinically relevant μ-opioid agonists. Mechanical nociception was assessed in mice with the paw pressure test (450 g), and heat nociception with the unilateral hot plate (55 °C) test...
March 23, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29558941/perturbing-chondroitin-sulfate-proteoglycan-signaling-through-lar-and-ptp%C3%AF-receptors-promotes-a-beneficial-inflammatory-response-following-spinal-cord-injury
#14
Scott Dyck, Hardeep Kataria, Arsalan Alizadeh, Kallivalappil T Santhosh, Bradley Lang, Jerry Silver, Soheila Karimi-Abdolrezaee
BACKGROUND: Traumatic spinal cord injury (SCI) results in upregulation of chondroitin sulfate proteoglycans (CSPGs) by reactive glia that impedes repair and regeneration in the spinal cord. Degradation of CSPGs is known to be beneficial in promoting endogenous repair mechanisms including axonal sprouting/regeneration, oligodendrocyte replacement, and remyelination, and is associated with improvements in functional outcomes after SCI. Recent evidence suggests that CSPGs may regulate secondary injury mechanisms by modulating neuroinflammation after SCI...
March 20, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29558382/bridging-from-brain-to-tumor-imaging-s-and-r-18-f-fluspidine-for-investigation-of-sigma-1-receptors-in-tumor-bearing-mice
#15
Mathias Kranz, Ralf Bergmann, Torsten Kniess, Birgit Belter, Christin Neuber, Zhengxin Cai, Gang Deng, Steffen Fischer, Jiangbing Zhou, Yiyun Huang, Peter Brust, Winnie Deuther-Conrad, Jens Pietzsch
Sigma-1 receptors (Sig1R) are highly expressed in various human cancer cells and hence imaging of this target with positron emission tomography (PET) can contribute to a better understanding of tumor pathophysiology and support the development of antineoplastic drugs. Two Sig1R-specific radiolabeled enantiomers ( S )-(-)- and ( R )-(+)-[18 F]fluspidine were investigated in several tumor cell lines including melanoma, squamous cell/epidermoid carcinoma, prostate carcinoma, and glioblastoma. Dynamic PET scans were performed in mice to investigate the suitability of both radiotracers for tumor imaging...
March 20, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29531859/synthesis-radiolabelling-and-evaluation-of-11-c-pb212-as-a-radioligand-for-imaging-sigma-1-receptors-using-pet
#16
Francesco Spinelli, Ahmed Haider, Annamaria Toscano, Maria Laura Pati, Claudia Keller, Francesco Berardi, Nicola Antonio Colabufo, Carmen Abate, Simon M Ametamey
The Sigma-1 receptor (Sig-1R) has been described as a pluripotent modulator of distinct physiological functions and its involvement in various central and peripheral pathological disorders has been demonstrated. However, further investigations are required to understand the complex role of the Sig-1R as a molecular chaperon. A specific PET radioligand would provide a powerful tool in Sig-1R related studies. As part of our efforts to develop a Sig-1R PET radioligand that shows antagonistic properties, we investigated the suitability of 1-(4-(6-methoxynaphthalen-1-yl)butyl)-4-methylpiperidine (designated PB212) for imaging Sig-1R...
2018: American Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/29497125/critical-role-of-sigma-1-receptors-in-central-neuropathic-pain-related-behaviours-after-mild-spinal-cord-injury-in-mice
#17
Sílvia Castany, Georgia Gris, José Miguel Vela, Enrique Verdú, Pere Boadas-Vaello
Sigma-1 receptor (σ1 R) knockout (KO) CD1 mice, generated by homologous recombination, and separate pharmacological studies in wild type (WT) mice were done to investigate the role of this receptor in the development of pain-related behaviours (thermal hyperalgesia and mechanical allodynia) in mice after spinal cord contusion injury (SCI) - a model of central neuropathic pain. The modulatory effect of σ1 R KO on extracellular mediators and signalling pathways in the spinal cord was also investigated. In particular, changes in the expression of inflammatory cytokines (tumour necrosis factor TNF-α, interleukin IL-1β) and both the expression and activation (phosphorylation) of the N-methyl-D-aspartate receptor subunit 2B (NR2B-NMDA) and extracellular signal-regulated kinases (ERK1/2) were analysed...
March 1, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29484723/multi-modal-imaging-of-long-term-recovery-post-stroke-by-positron-emission-tomography-and-matrix-assisted-laser-desorption-ionisation-mass-spectrometry
#18
Fiona Henderson, Philippa J Hart, Jesus M Pradillo, Michael Kassiou, Lidan Christie, Kaye J Williams, Herve Boutin, Adam McMahon
RATIONALE: Stroke is a leading cause of disability worldwide. Understanding the recovery process post-stroke is essential; however, longer-term recovery studies are lacking. In vivo positron emission tomography (PET) can image biological recovery processes, but is limited by spatial resolution and its targeted nature. Untargeted mass spectrometry imaging offers high spatial resolution, providing an ideal ex vivo tool for brain recovery imaging. METHODS: Magnetic resonance imaging (MRI) was used to image a rat brain 48 h after ischaemic stroke to locate the infarcted regions of the brain...
May 15, 2018: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29483862/cocaine-effects-on-dopaminergic-transmission-depend-on-a-balance-between-sigma-1-and-sigma-2-receptor-expression
#19
David Aguinaga, Mireia Medrano, Ignacio Vega-Quiroga, Katia Gysling, Enric I Canela, Gemma Navarro, Rafael Franco
Sigma σ1 and σ2 receptors are targets of cocaine. Despite sharing a similar name, the two receptors are structurally unrelated and their physiological role is unknown. Cocaine increases the level of dopamine, a key neurotransmitter in CNS motor control and reward areas. While the drug also affects dopaminergic signaling by allosteric modulations exerted by σ1 R interacting with dopamine D1 and D2 receptors, the potential regulation of dopaminergic transmission by σ2 R is also unknown. We here demonstrate that σ2 R may form heteroreceptor complexes with D1 but not with D2 receptors...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29483387/sigma-1-receptor-stimulation-with-pre-084-ameliorates-myocardial-ischemia-reperfusion-injury-in-rats
#20
Qi-Jun Gao, Bo Yang, Jing Chen, Shao-Bo Shi, Hong-Jie Yang, Xin Liu
Background: The sigma receptors are a relatively novel receptor group with respect to knowledge of their effect on health. Although the sigma-1 receptor agonist PRE-084 exhibits a cardioprotective effect in some studies, the benefits in cases of myocardial ischemia/reperfusion (I/R) are not clear. The aim of this study was to explore the mechanism of action and assess the effect of PRE-084 on myocardial I/R injury in rats. Methods: In this study, rats were assigned randomly to three groups with computer (n = 14 for each group): a sham group, an I/R group, and a PRE-084 group...
March 5, 2018: Chinese Medical Journal
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