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Adenosine receptor

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https://www.readbyqxmd.com/read/28742222/disruption-of-the-atp-adenosine-balance-in-cd39-mice-is-associated-with-handling-induced-seizures
#1
Amanda J Lanser, Rafael M Rezende, Stephen Rubino, Paul J Lorello, Dustin J Donnelly, Huixin Xu, Lauren A Lau, Chris G Dulla, Barbara J Caldarone, Simon C Robson, Howard L Weiner
Seizures are due to excessive, synchronous neuronal firing in the brain and are characteristic of epilepsy, the fourth most prevalent neurologic disease. Herein, we report handling-induced and spontaneous seizures in mice deficient of CD39, a cell-surface ATPase highly expressed on microglial cells. CD39(-/-) mice with handling-induced seizures had normal input-output curves and paired-pulse ratio measured from hippocampal slices and lacked microgliosis, astrogliosis or overt cell loss in the hippocampus and cortex...
July 25, 2017: Immunology
https://www.readbyqxmd.com/read/28742108/fasting-metabolism-modulates-the-interleukin-12-interleukin-10-cytokine-axis
#2
Johannes J Kovarik, Elisabeth Kernbauer, Markus A Hölzl, Johannes Hofer, Guido A Gualdoni, Klaus G Schmetterer, Fitore Miftari, Yury Sobanov, Anastasia Meshcheryakova, Diana Mechtcheriakova, Nadine Witzeneder, Georg Greiner, Anna Ohradanova-Repic, Petra Waidhofer-Söllner, Marcus D Säemann, Thomas Decker, Gerhard J Zlabinger
A crucial role of cell metabolism in immune cell differentiation and function has been recently established. Growing evidence indicates that metabolic processes impact both, innate and adaptive immunity. Since a down-stream integrator of metabolic alterations, mammalian target of rapamycin (mTOR), is responsible for controlling the balance between pro-inflammatory interleukin (IL)-12 and anti-inflammatory IL-10, we investigated the effect of upstream interference using metabolic modulators on the production of pro- and anti-inflammatory cytokines...
2017: PloS One
https://www.readbyqxmd.com/read/28739086/a-preclinical-study-on-the-combined-effects-of-repeated-eltoprazine-and-preladenant-treatment-for-alleviating-l-dopa-induced-dyskinesia-in-parkinson-s-disease
#3
Wai Kin D Ko, Qin Li, Long Yun Cheng, Micaela Morelli, Manolo Carta, Erwan Bezard
Eltoprazine, a serotonergic (5-HT)1A/B receptor agonist, is a potential treatment for L-DOPA-induced dyskinesia (LID) in Parkinson's disease (PD) but notably compromises the anti-parkinsonian effects of L-DOPA, as seen in rodent and monkey models of PD. Preladenant, a selective adenosine A2a receptor antagonist, mediates modest anti-parkinsonian effects in parkinsonian monkeys. In a recent investigation, combined eltoprazine and preladenant treatment with a sub-threshold dose of L-DOPA acutely attenuated dyskinesia without exacerbating PD disability in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated macaques...
July 21, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28739056/supplementation-with-vitis-vinifera-l-skin-extract-improves-insulin-resistance-and-prevents-hepatic-lipid-accumulation-and-steatosis-in-high-fat-diet-fed-mice
#4
Izabelle Barcellos Santos, Graziele Freitas de Bem, Viviane Silva Cristino Cordeiro, Cristiane Aguiar da Costa, Lenize Costa Reis Marins de Carvalho, Ana Paula Machado da Rocha, Gisele França da Costa, Dayane Teixeira Ognibene, Roberto Soares de Moura, Angela Castro Resende
Nonalcoholic fatty liver disease is one of the most common complications of obesity. The Vitis vinifera L. grape skin extract (ACH09) is an important source of polyphenols, which are related to its antioxidant and antihyperglycemic activities. We hypothesized that ACH09 could also exert beneficial effects on metabolic disorders associated with obesity and evaluated ACH09's influence on high-fat (HF) diet-induced hepatic steatosis and insulin resistance in C57BL/6 mice. The animals were fed a standard diet (10% fat, control) or an HF diet (60% fat, HF) with or without ACH09 (200mg/[kg d]) for 12weeks...
July 2017: Nutrition Research
https://www.readbyqxmd.com/read/28738113/estrogen-status-gates-effects-of-kappa-opioid-receptor-on-temporomandibular-joint-responsive-neurons-at-the-spinomedullary-junction-in-female-rats
#5
Akimasa Tashiro, David A Bereiter, Yasuhiro Nishida
AIMS: To determine whether estrogen status alters κ-opioid inhibition of nociceptive processing by affecting temporomandibular joint (TMJ) input to neurons in the trigeminal subnucleus caudalis [Vc]/C1-2 region at the spinomedullary junction in female rats. METHODS: TMJ-responsive neurons were recorded in laminae I-II of the Vc/C1-2 region at the spinomedullary junction of ovariectomized female rats treated for 2 days with low-dose estradiol (LE group; 2 mg/day) or high-dose estradiol (HE group; 20 mg/day)...
July 2017: Journal of Oral & Facial Pain and Headache
https://www.readbyqxmd.com/read/28736837/acute-effects-of-alcohol-on-sleep-are-mediated-by-components-of-homeostatic-sleep-regulatory-system-an-editorial-highlight-for-lesions-of-the-basal-forebrain-cholinergic-neurons-attenuates-sleepiness-and-adenosine-after-alcohol-consumption-on-doi-10-1111-jnc
#6
EDITORIAL
Md Noor Alam, Dennis McGinty
Alcohol causes adenosine buildup, which inhibits wake-active neurons via adenosine A1 receptors thus disinhibiting sleep active neurons and also stimulates sleep-active neurons via A2A receptors, causing sleep. This editorial highlights the study entitled, "Lesions of the basal forebrain cholinergic neurons attenuates sleepiness and adenosine after alcohol consumption" by Sharma and colleagues. They report that the wake-promoting basal forebrain (BF) cholinergic neurons play a crucial role in mediating acute alcohol-induced sleep via adenosinergic signaling...
July 24, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28734904/identifying-novel-members-of-the-wntless-interactome-through-genetic-and-candidate-gene-approaches
#7
Jessica Petko, Trevor Tranchina, Goral Patel, Robert Levenson, Stephanie Justice-Bitner
Wnt signaling is an important pathway that regulates several aspects of embryogenesis, stem cell maintenance, and neural connectivity. We have recently determined that opioids decrease Wnt secretion, presumably by inhibiting the recycling of the Wnt trafficking protein Wntless (Wls). This effect appears to be mediated by protein-protein interaction between Wls and the mu-opioid receptor (MOR), the primary cellular target of opioid drugs. The goal of this study was to identify novel protein interactors of Wls that are expressed in the brain and may also play a role in reward or addiction...
July 19, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28734869/p2x-receptors-up-regulate-the-cell-surface-expression-of-the-neuronal-glycine-transporter-glyt2
#8
Lucía Villarejo-López, Esperanza Jiménez, David Bartolomé-Martín, Francisco Zafra, Pablo Lapunzina, Carmen Aragón, Beatriz López-Corcuera
Glycinergic inhibitory neurons of the spinal dorsal horn exert critical control over the conduction of nociceptive signals to higher brain areas. The neuronal glycine transporter 2 (GlyT2) is involved in the recycling of synaptic glycine from the inhibitory synaptic cleft and its activity modulates intra and extracellular glycine concentrations. In this report we show that the stimulation of P2X purinergic receptors with βγ-methylene adenosine 5'-triphosphate induces the up-regulation of GlyT2 transport activity by increasing total and plasma membrane expression and reducing transporter ubiquitination...
July 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28734063/atp-and-astrocytes-play-a-prominent-role-in-the-control-of-the-respiratory-pattern-generator-in-the-lamprey
#9
Elenia Cinelli, Ludovica Iovino, Donatella Mutolo
The role of ATP and astrocytes in respiratory rhythm modulation has been recently investigated in neonatal rodents. However, no information on the role of ATP and astrocytes within the respiratory network of the lamprey is available, particularly within the paratrigeminal respiratory group (pTRG), the proposed respiratory central pattern generator. To address these issues, the present study was carried out on isolated brainstems of the adult lamprey. Bath application of ATP caused marked increases in respiratory frequency followed by decreases in the respiratory motor output, mediated by the ATP metabolite adenosine at the level of the pTRG...
July 22, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28734062/coumarins-and-adenosine-receptors-new-perceptions-in-structure-affinity-relationships
#10
André Fonseca, Maria João Matos, Santiago Vilar, Sonja Kachler, Karl-Norbert Klotz, Eugenio Uriarte, Fernanda Borges
Adenosine receptors (ARs) subtypes are involved in several physiological and pharmacological processes. Ligands able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective ARs ligands based on coumarin scaffold. Therefore, a series 3-phenylcarboxamidocoumarins were synthesised and their affinity for the human ARs subtypes was screened by radioligand binding assays for A1 , A2A and A3 receptors and for A2B by adenylyl cyclase assay...
July 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28734058/evaluation-of-2-benzylidene-1-tetralone-derivatives-as-antagonists-of-a1-and-a2a-adenosine-receptors
#11
Lesetja J Legoabe, Mietha M Van der Walt, Gisella Terre'Blanche
Antagonists of the adenosine receptors (A1 and A2A ) are thought to be beneficial in neurological disorders, such as Alzheimer's and Parkinson's disease. The aim of this study was to explore 2-benzylidene-1-tetralone derivatives as antagonists of A1 and/or A2A adenosine receptors. In general, the test compounds were found to be selective for the A1 adenosine receptor, with only three test compounds possessing affinity for both the A1 and A2A adenosine receptor. The 2-benzylidene-1-tetralones bearing a hydroxyl substituent at either position C5, C6 or C7 of ring A displayed favorable adenosine A1 receptor binding, while C5 hydroxy substitution led to favorable A2A adenosine receptor affinity...
July 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28733470/dendritic-cell-targeted-lentiviral-vector-immunization-uses-pseudotransduction-and-dna-mediated-sting-and-cgas-activation
#12
Jocelyn T Kim, Yarong Liu, Rajan P Kulkarni, Kevin K Lee, Bingbing Dai, Geoffrey Lovely, Yong Ouyang, Pin Wang, Lili Yang, David Baltimore
Dendritic cell (DC) activation and antigen presentation are critical for efficient priming of T cell responses. Here, we study how lentiviral vectors (LVs) deliver antigen and activate DCs to generate T cell immunization in vivo. We report that antigenic proteins delivered in vector particles via pseudotransduction were sufficient to stimulate an antigen-specific immune response. The delivery of the viral genome encoding the antigen increased the magnitude of this response in vivo but was irrelevant in vitro...
July 21, 2017: Science Immunology
https://www.readbyqxmd.com/read/28731188/hispidin-rescues-palmitate%C3%A2-induced-insulin-resistance-in-c2c12-myotubes
#13
Jong Seok Lee, Jun Myoung Park, Sarah Lee, Hye Jin Lee, Hee-Sun Yang, Joohong Yeo, Ki Rim Lee, Byung Hyun Choi, Eock Kee Hong
Skeletal muscle serves an important role in the utilization of glucose during insulin‑stimulated conditions. Excessive saturated fatty acids are considered to be a major contributing factor to insulin resistance in skeletal muscle cells. The present study investigated the effects of hispidin on palmitate‑induced insulin resistance in C2C12 skeletal muscle myotubes via an MTT assay, glucose uptake assay, Oil‑Red‑O staining and western blot analysis. Hispidin reversed the palmitate‑induced inhibition of glucose uptake, and inhibited palmitate‑induced intracellular lipid accumulation...
July 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28730102/anti-scarring-effects-of-butaprost-on-human-subconjunctival-tenon-s-fibroblasts
#14
Jong Hoon Shin, Je Hyun Seo, Jae Ho Jung, Tae Woo Kim
AIM: To investigate the toxicity of the E-prostanoid 2 (EP2) receptor agonist, butaprost against human subconjunctival (Tenon's capsule) fibroblasts, and to determine the underlying mechanism. METHODS: We isolated Tenon's fibroblasts from the subconjunctival area of healthy subjects and evaluated the types of EP receptors expressed using quantitative real-time reverse transcription polymerase chain reaction (RT-PCR). The toxicity of butaprost against the fibroblasts was evaluated using methyl thiazolyl tetrazolium and lactic dehydrogenase assays...
2017: International Journal of Ophthalmology
https://www.readbyqxmd.com/read/28729619/effects-of-4-1h-quinolinone-derivative-a-novel-non-nucleotide-allosteric-purinergic-p2y-2-agonist-on-cardiomyocytes-in-neonatal-rats
#15
Kensuke Sakuma, Hideyuki Nakagawa, Tatsuo Oikawa, Masakuni Noda, Shota Ikeda
Purinergic P2Y 2 receptors, G-protein coupled receptors that primarily couple with Gαq/11-proteins, are activated equipotently by adenosine-5'-triphosphate (ATP) and uridine-5'-triphosphate. Evidence suggests that P2Y 2 agonists make potential drug candidates for the treatment of cardiovascular diseases. However, selective non-nucleotide, small-molecule P2Y 2 agonists have yet to be developed. In this report, we discuss Compound 89, a novel non-nucleotide allosteric P2Y 2 agonist that was active in signal transduction and gene induction, and in our in vitro cardiac hypertrophy model...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28728819/regulation-of-piezo-channels-by-cellular-signaling-pathways
#16
I Borbiro, T Rohacs
The recently identified mechanically activated Piezo1 and Piezo2 channels play major roles in various aspects of mechanosensation in mammals, and their mutations are associated with human diseases. Recent reports show that activation of cell surface receptors coupled to heterotrimeric Gq proteins increase the sensitivity of Piezo2 channels to mechanical stimuli. Activation of the cyclic adenosine monophosphate pathway was also shown to potentiate Piezo2 channel activity. This phenomenon may play a role in mechanical allodynia or hyperalgesia during inflammation...
2017: Current Topics in Membranes
https://www.readbyqxmd.com/read/28728462/increased-binding-potential-of-brain-adenosine-a-sub-1-sub-receptor-in-chronic-stages-of-patients-with-diffuse-axonal-injury-measured-with-1-methyl-sup-11-sup-c-8-dicyclopropylmethyl-1-methyl-3-propylxanthine-pet-imaging
#17
Shihori Hayashi, Motoki Inaji, Tadashi Nariai, Keiichi Oda, Muneyuki Sakata, Jun Toyohara, Kenji Ishii, Kiichi Ishiwata, Taketoshi Maehara
The positron emission tomography (PET) radioligand for adenosine A <sub>1</sub> receptor (A1R) [1-methyl- <sup>11</sup>C] 8-dicyclopropylmethyl-1-methyl-3-propylxanthine (MPDX) has recently been developed for human brain imaging. In the present study, we evaluated the alteration of the A1R in patients with diffuse axonal injury (DAI) in chronic stage <i>in vivo</i>. Ten patients with DAI (7 men and 3 women) were included in this study. Three PET examinations were sequentially performed to measure A1R binding with <sup>11</sup>C-MPDX, glucose metabolism with <sup>18</sup>F-fluorodeoxyglucose (FDG), and central benzodiazepine receptor binding with <sup>11</sup>C-flumazenil (FMZ), decreases of <sup>11</sup>C-FMZ uptake indicate neuronal loss...
July 20, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/28728042/pharmacological-relationships-and-ligand-discovery-of-g-protein-coupled-receptors-revealed-by-simultaneous-ligand-and-receptor-clustering
#18
Cheng Zhang, Yi-Ming Shao, Xiaohua Ma, Siew Lee Cheong, Chu Qin, Lin Tao, Peng Zhang, Shangying Chen, Xian Zeng, Hongxia Liu, Giorgia Pastorin, Yuyang Jiang, Yu Zong Chen
Conventional ligand and receptor similarity methods have been extensively used for exposing pharmacological relationships and drug lead discovery. They may in some cases neglect minor relationships useful for target hopping particularly against the remote family members. To complement the conventional methods for capturing these minor relationships, we developed a new method that uses a SLARC (Simultaneous Ligand And Receptor Clustering) 2D map to simultaneously characterize the ligand structural and receptor binding-site sequence relationships of a receptor family...
July 11, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28726742/special-issue-adenosine-receptors
#19
EDITORIAL
Francisco Ciruela, Eddy Sotelo
Nearly 90 years ago, Drury and Szent-Györgyi revealed that adenosine produced profound hypotension and bradycardia, and it affected kidney function in mammals [1]. [...].
July 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28725182/canonical-and-novel-non-canonical-cholinergic-agonists-inhibit-atp-induced-release-of-monocytic-interleukin-1%C3%AE-via-different-combinations-of-nicotinic-acetylcholine-receptor-subunits-%C3%AE-7-%C3%AE-9-and-%C3%AE-10
#20
Anna Zakrzewicz, Katrin Richter, Alisa Agné, Sigrid Wilker, Kathrin Siebers, Bijan Fink, Gabriela Krasteva-Christ, Mike Althaus, Winfried Padberg, Arik J Hone, J Michael McIntosh, Veronika Grau
Recently, we discovered a cholinergic mechanism that inhibits the adenosine triphosphate (ATP)-dependent release of interleukin-1β (IL-1β) by human monocytes via nicotinic acetylcholine receptors (nAChRs) composed of α7, α9 and/or α10 subunits. Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that elicit metabotropic activity at monocytic nAChR. Interestingly, PC does not provoke ion channel responses at conventional nAChRs composed of subunits α9 and α10...
2017: Frontiers in Cellular Neuroscience
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