keyword
MENU ▼
Read by QxMD icon Read
search

Sigma receptor

keyword
https://www.readbyqxmd.com/read/29786657/eukaryotic-translation-initiation-factor-4a-down-regulation-mediates-interleukin-24-induced-apoptosis-through-inhibition-of-translation
#1
Xuelin Zhong, Leah Persaud, Hilal Muharam, Ashleigh Francis, Dibash Das, Bertal Huseyin Aktas, Moira Sauane
Dysregulated activity of helicase eIF4A drives transformation to and maintenance of cancer cell phenotype by reprogramming cellular translation. Interleukin 24 (IL-24) is a tumor-suppressing protein, which has the ability to inhibit angiogenesis, sensitize cancer cells to chemotherapy, and induce cancer cell-specific apoptosis. In this study, we found that eIF4A is inhibited by IL-24. Consequently, selective reduction of translation was observed for mRNAs harboring strong secondary structures in their 5'-untranslated regions (5'UTRs)...
May 22, 2018: Cancers
https://www.readbyqxmd.com/read/29783994/large-scale-transcriptomic-analysis-reveals-that-pridopidine-reverses-aberrant-gene-expression-and-activates-neuroprotective-pathways-in-the-yac128-hd-mouse
#2
Rebecca Kusko, Jennifer Dreymann, Jermaine Ross, Yoonjeong Cha, Renan Escalante-Chong, Marta Garcia-Miralles, Liang Juin Tan, Michael E Burczynski, Ben Zeskind, Daphna Laifenfeld, Mahmoud Pouladi, Michal Geva, Iris Grossman, Michael R Hayden
BACKGROUND: Huntington Disease (HD) is an incurable autosomal dominant neurodegenerative disorder driven by an expansion repeat giving rise to the mutant huntingtin protein (mHtt), which is known to disrupt a multitude of transcriptional pathways. Pridopidine, a small molecule in development for treatment of HD, has been shown to improve motor symptoms in HD patients. In HD animal models, pridopidine exerts neuroprotective effects and improves behavioral and motor functions. Pridopidine binds primarily to the sigma-1 receptor, (IC50 ~ 100 nM), which mediates its neuroprotective properties, such as rescue of spine density and aberrant calcium signaling in HD neuronal cultures...
May 21, 2018: Molecular Neurodegeneration
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
#3
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/29760175/modulation-of-receptor-protein-tyrosine-phosphatase-sigma-increases-chondroitin-sulfate-proteoglycan-degradation-through-cathepsin-b-secretion-to-enhance-axon-outgrowth
#4
Amanda Phuong Tran, Sapna Sundar, Meigen Yu, Bradley T Lang, Jerry Silver
Severed axon tips reform growth cones following spinal cord injury that fail to regenerate, in part, because they become embedded within an inhibitory extracellular matrix. Chondroitin sulfate proteoglycans (CSPGs) are the major axon inhibitory matrix component that is increased within the lesion scar and in perineuronal nets around deafferented neurons. We have recently developed a novel peptide modulator (Intracellular Sigma Peptide or ISP) of the cognate receptor of CSPGs, protein tyrosine phosphatase sigma (RPTPσ), which has been shown to markedly improve sensorimotor function, micturition, and coordinated locomotor behavior in spinal cord contused rats...
May 14, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29749988/amelioration-of-pentylenetetrazole-induced-seizures-by-modulators-of-sigma-n-methyl-d-aspartate-and-ryanodine-receptors-in-mice
#5
Mojtaba Keshavarz, Behdad Yekzaman
Background: Sigma receptors, N-methyl-D-aspartate (NMDA) antagonist, and modulators of intracellular calcium may be useful for seizure control. Therefore, we aimed to evaluate the antiepileptic effects of opipramol, a sigma receptor agonist, against pentylenetetrazole (PTZ)-induced seizures in mice and assess ketamine and caffeine interaction with the antiepileptic effects of opipramol. Methods: PTZ (100 mg/kg) was used for the induction of seizure in 72 male albino Swiss strain of mice (n=8)...
March 2018: Iranian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29728649/small-molecule-modulators-of-%C3%AF-2r-tmem97-reduce-alcohol-withdrawal-induced-behaviors
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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/29577719/anisamide-anchored-lyotropic-nano-liquid-crystalline-particles-with-aie-effect-a-smart-optical-beacon-for-tumor-imaging-and-therapy
#18
Sandeep Urandur, Venkatesh Teja Banala, Ravi Prakash Shukla, Naresh Mittapelly, Gitu Pandey, Navodayam Kalleti, Kalyan Mitra, Srikanta Kumar Rath, Ritu Trivedi, Pratibha Ramarao, Prabhat Ranjan Mishra
The prospective design of nanocarriers for personalized oncotherapy should be an ensemble of targeting, imaging, and noninvasive therapeutic capabilities. Here in, we report the development of the inverse hexagonal nano liquid crystalline (NLC) particles able to host Formononetin (FMN), a phytoestrogen with known anticancer activity and Tetraphenylethene (TPE), an iconic optical beacon with aggregation-induced-emission (AIE) signature simultaneously. Ordered 3D mesoporous internal structure and high lipid volume fraction of NLC nanoparticles (NLC NPs) frame the outer compartment for the better settlement of payloads...
March 26, 2018: ACS Applied Materials & Interfaces
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
#19
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
#20
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
keyword
keyword
72082
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"