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adenosine a2a receptor

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https://www.readbyqxmd.com/read/28089906/adenosine-signaling-in-diabetes-mellitus-and-associated-cardiovascular-and-renal-complications
#1
REVIEW
Maria Peleli, Mattias Carlstrom
Diabetes mellitus is characterized by abnormal glucose and lipid metabolism, and subsequent hyperglycemia and dyslipidemia, which results from defects in pancreatic beta islets insulin secretion and/or decreased insulin sensitivity in metabolically active organs (i.e. liver, skeletal muscle and adipose tissue). Accumulating evidence highlights a critical role for the adenosine system in the regulation of insulin and glucose homeostasis and the pathophysiology of type 2 diabetes (T2D). Adenosine is a key diverse extracellular signaling molecule that regulates several aspects of tissue function by activating four G-protein-coupled receptors (i...
January 12, 2017: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/28077904/regadenoson-in-myocardial-perfusion-study-first-institutional-experiences-in-bosnia-and-herzegovina
#2
Nermina Beslic, Renata Milardovic, Amera Sadija, Sejla Ceric, Zeljka Raic
INTRODUCTION: Myocardial perfusion imaging (MPI) is widely used in the evaluation of known and suspected coronary artery disease (CAD). Imaging of heart in stress and rest enables the comparison of myocardial uptake of radiotracer in proportion to the needs and coronary flow, which is used for detection of perfusion defects. Exercise stress and pharmacologic agents are used for the stressing purpose. Novel pharmacologic stressor regadenoson is A2A selective adenosine agonist, which selectively binds to the adenosine receptors in coronary arteries causing coronary dilatation...
December 2016: Acta Informatica Medica: AIM
https://www.readbyqxmd.com/read/28075020/adenosine-receptors-regulate-gap-junction-coupling-of-the-human-cerebral-microvascular-endothelial-cells-hcmec-d3-by-ca-2-influx-through-cng-channels
#3
Almke Bader, Willem Bintig, Daniela Begandt, Anne Klett, Ina G Siller, Carola Gregor, Frank Schaarschmidt, Babette Weksler, Ignacio Romero, Pierre-Olivier Couraud, Stefan W Hell, Anaclet Ngezahayo
The human cerebral microvascular endothelial cell line hCMEC/D3 was used to characterize the physiological link between adenosine receptors and the gap junction coupling in endothelial cells of the blood-brain barrier. Expressed adenosine receptor subtypes and connexin (Cx) isoforms were identified by RT-PCR. Scrape loading/dye transfer was used to evaluate the impact of the A2A and A2B adenosine receptor subtype agonist 2-phenylaminoadenosine (2-PAA) on the gap junction coupling. We found that 2-PAA stimulated cAMP synthesis and enhanced gap junction coupling in a concentration-dependent manner...
January 11, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28071892/transient-adenosine-release-is-modulated-by-nmda-and-gabab-receptors
#4
Michael D Nguyen, Ying Wang, Mallikarjunarao Ganesana, B Jill Venton
Adenosine is a neuroprotective agent that modulates neurotransmission and is modulated by other neurotransmitters. Spontaneous, transient adenosine is a recently discovered mode of signaling where adenosine is released and cleared from the extracellular space quickly, in less than three seconds. Spontaneous adenosine release is regulated by adenosine A1 and A2a receptors, but regulation by other neurotransmitter receptors has not been studied. Here, we examined the effect of glutamate and GABA receptors on the concentration and frequency of spontaneous, transient adenosine release by measuring adenosine with fast-scan cyclic voltammetry in the rat caudate-putamen...
January 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28067172/fusing-docking-scoring-functions-improves-the-virtual-screening-performance-for-discovering-parkinson-s-disease-dual-target-ligands
#5
Yunierkis Perez-Castillo, Aliuska Morales Helguera, M Natália D S Cordeiro, Eduardo Tejera, Cesar Paz-Y-Miño, Aminael Sánchez-Rodríguez, Fernanda Borges, Maykel Cruz-Monteagudo
Virtual methodologies have become essential components of the drug discovery pipeline. Specifically, structure-based drug design methodologies exploit the 3D structure of molecular targets to discover new drug candidates through molecular docking. Recently, dual target ligands of the Adenosine A2A Receptor and Monoamine Oxidase B enzyme have been proposed as effective therapies for the treatment of Parkinson's disease. To the best of our knowledge, no theoretical study has been devoted to developing structure-based virtual screening methodologies for the discovery of dual A2AAR antagonists and MAO-B inhibitors...
January 9, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28062599/in-vivo-evaluation-of-11c-preladenant-for-pet-imaging-of-adenosine-a2a-receptors-in-the-conscious-monkey
#6
Xiaoyun Zhou, Ronald Boellaard, Kiichi Ishiwata, Muneyuki Sakata, Rudi A Dierckx, Johan de Jong, Shingo Nishiyama, Hiroyuki Ohba, Hideo Tsukada, Erik F de Vries, Philip H Elsinga
: [(11)C]Preladenant was developed as a novel PET ligand for the adenosine A2A receptors (A2ARs). The present study aims to evaluate the suitability of [(11)C]preladenant-PET for the quantification of striatal A2ARs and the assessment of A2AR occupancy in the conscious monkey brain. METHODS: [(11)C]Preladenant was i.v. injected into conscious monkeys (n = 4, 18 PET scans) and a 91-min dynamic scan was started. Arterial blood samples in combination with metabolite analysis were obtained during the scan to provide the input function for kinetic modelling...
January 6, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28060732/prognostic-impact-of-cd73-and-a2a-adenosine-receptor-expression-in-non-small-cell-lung-cancer
#7
Yusuke Inoue, Katsuhiro Yoshimura, Nobuya Kurabe, Tomoaki Kahyo, Akikazu Kawase, Masayuki Tanahashi, Hiroshi Ogawa, Naoki Inui, Kazuhito Funai, Kazuya Shinmura, Hiroshi Niwa, Takafumi Suda, Haruhiko Sugimura
In immune cells, CD73 dephosphorylates and converts extracellular AMP into adenosine, which binds the A2A adenosine receptor (A2AR). Blockade of this interaction, which induces an immunosuppressed niche in the tumor microenvironment, represents a potential novel treatment strategy. The clinical significance of CD73 and A2AR expression in non-small-cell lung cancer (NSCLC), however, has yet to be thoroughly investigated. Here we evaluated CD73 and A2AR protein expression levels using immunohistochemistry in tissue microarrays containing 642 resected NSCLC specimens...
January 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28060378/cd73-regulates-anti-inflammatory-signaling-between-apoptotic-cells-and-endotoxin-conditioned-tissue-macrophages
#8
Patrick S Murphy, Jing Wang, Samir P Bhagwat, Joshua C Munger, William J Janssen, Terry W Wright, Michael R Elliott
The phagocytosis of apoptotic cells (efferocytosis) shifts macrophages to an anti-inflammatory state through a set of still poorly understood soluble and cell-bound signals. Apoptosis is a common feature of inflamed tissues, and efferocytosis by tissue macrophages is thought to promote the resolution of inflammation. However, it is not clear how the exposure of tissue macrophages to inflammatory cues (e.g., PAMPs, DAMPs) in the early stages of inflammation affects immune outcomes of macrophage-apoptotic cell interactions occurring at later stages of inflammation...
January 6, 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/28055204/design-synthesis-of-novel-potent-selective-orally-bio-available-adenosine-a2a-receptor-antagonists-and-their-biological-evaluation
#9
Sujay Basu, Dinesh A Barawkar, Sachin Thorat, Yogesh D Shejul, Meena Patel, Minakshi Naykodi, Vaibhav Jain, Yogesh Salve, Vandna Prasad, Sumit Chaudhary, Indraneel Ghosh, Ganesh Bhat, Azfar Quraishi, Harish Patil, Shariq Ansari, Suraj Menon, Vishal Unadkat, Rhishikesh Thakare, Madhav S Seervi, Ashwinkumar V Meru, Siddhartha De, Ravi K Bhamidipati, Sreekanth Rouduri, Venkata P Palle, Anita Chug, Kasim A Mookhtiar
Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the 2-position lead to identification of compound 25 as a potent and selective A2A adenosine receptor (A2AAdoR) antagonist with reasonable ADME and pharmacokinetic properties. However, poor intrinsic solubility and low to moderate oral bioavailability made this series unsuitable for further development. Further optimization using structure-based drug design approach resulted in discovery of potent and selective adenosine A2A receptor antagonists bearing substituted 1-methylcyclohexyl-carboxamide groups at position 2 of the benzothiazole scaffold and endowed with better solubility and oral bioavailability...
January 5, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28042771/oxidative-stress-pro-inflammatory-cytokines-and-antioxidants-regulate-expression-levels-of-micrornas-in-parkinson-s-disease
#10
Kedar N Prasad
Parkinson's disease (PD) is a slow progressive neurodegenerative disease associated with abnormal function of extrapyramidal system. Although several biochemical and genetic defects have been identified, increased oxidative stress and chronic inflammation are one of the earliest events that initiate and promote PD. Oxidative stress also participates in impaired non-motor symptoms.The levels of microRNAs that are evolutionarily conserved single-stranded non-coding RNAs of approximately 22 nucleotide in length are altered in PD...
January 2, 2017: Current Aging Science
https://www.readbyqxmd.com/read/28041708/expressions-of-adenosine-a2a-receptors-in-coronary-arteries-and-peripheral-blood-mononuclear-cells-are-correlated-in-coronary-artery-disease-patients
#11
Vlad Gariboldi, Donato Vairo, Régis Guieu, Marion Marlingue, Eléonore Ravis, David Lagier, Alissa Mari, Elsa Thery, Frédéric Collart, Marine Gaudry, Laurent Bonello, Franck Paganelli, Jocelyne Condo, Nathalie Kipson, Emmanuel Fenouillet, Jean Ruf, Giovanna Mottola
BACKGROUND: Altered coronary blood flow occurs in patients with coronary artery disease (CAD). Adenosine strongly impacts blood flow mostly via adenosine A2A receptor (A2AR) expressed in coronary tissues. As part of a systemic regulation of the adenosinergic system, we compared A2AR expression in situ, and on peripheral blood mononuclear cells (PBMC) in CAD patients. METHODS AND RESULTS: Aortic and coronary tissues, and PBMC were sampled in 20 CAD patients undergoing coronary artery bypass surgery and consecutively included...
December 21, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/28012971/effects-of-a-human-recombinant-alkaline-phosphatase-during-impaired-mitochondrial-function-in-human-renal-proximal-tubule-epithelial-cells
#12
Esther Peters, Tom Schirris, Alexander H van Asbeck, Jelle Gerretsen, Jennifer Eymael, Angel Ashikov, Merel J W Adjobo-Hermans, Frans Russel, Peter Pickkers, Rosalinde Masereeuw
Sepsis-associated acute kidney injury is a multifactorial syndrome in which inflammation and renal microcirculatory dysfunction play a profound role. Subsequently, renal tubule mitochondria reprioritize cellular functions to prevent further damage. Here, we investigated the putative protective effects of human recombinant alkaline phosphatase (recAP) during inhibition of mitochondrial respiration in conditionally immortalized human proximal tubule epithelial cells (ciPTEC). Full inhibition of mitochondrial oxygen consumption was obtained after 24h antimycin A treatment, which did not affect cell viability...
December 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28012867/chronic-oral-administration-of-mpep-an-antagonist-of-mglu5-receptor-during-gestation-and-lactation-alters-mglu5-and-a2a-receptors-in-maternal-and-neonatal-brain
#13
Antonio López-Zapata, David Agustín León-Navarro, María Crespo, José Luis Albasanz, Mairena Martín
Antidepressant and anxiolytic drugs are widely consumed even by pregnant and lactating women. The metabotropic glutamate receptor 5 (mGlu5) antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) exerts antidepressant- and anxiolytic-like actions. Given that treatment for anxiety and depression use to be prolonged in time, it is conceivable a possible modulation of metabotropic glutamate receptors (mGlu receptors) after prolonged MPEP exposure, which could also modify adenosine A2A receptors (A2AR) since functional cross-talk between them has been reported...
December 22, 2016: Neuroscience
https://www.readbyqxmd.com/read/28011152/adenosine-a2a-receptor-stimulation-blocks-development-of-nonalcoholic-steatohepatitis-in-mice-by-multilevel-inhibition-of-signals-that-cause-immunolipotoxicity
#14
Elisa Alchera, Simona Rolla, Chiara Imarisio, Valentina Bardina, Guido Valente, Francesco Novelli, Rita Carini
Lipotoxicity and immunoinflammation are associated with the evolution of steatosis toward nonalcoholic steatohepatitis (NASH). This study reports the ability of adenosine A2a receptor (A2aR) activation to inhibit NASH development by modulating the responses of CD4(+) T-helper (Th) cells to avoid an immuno-mediated potentiation of lipotoxicity. The effect of the A2aR agonist CGS21680 on immunoinflammatory signals, CD4(+)Th cell infiltration and immunolipotoxicity was analyzed in steatotic C57BL/6 mice fed with a methionine-choline-deficient (MCD) diet and in mouse hepatocytes exposed to palmitic acid (PA)...
December 6, 2016: Translational Research: the Journal of Laboratory and Clinical Medicine
https://www.readbyqxmd.com/read/28010756/deregulation-of-adenosine-receptors-in-psoriatic-epidermis-an-option-for-therapeutic-treatment
#15
Stefania Merighi, Pier Andrea Borea, Katia Varani, Stefania Gessi
Purinergic signaling is involved in psoriasis, a chronic skin disease characterized by increased epidermis cell growth. In particular, Andrés et al. focus on the keratinocyte biology modulated by adenosine receptors providing evidence that the A2B subtype plays a prominent role in the reduction of keratinocyte proliferation whereas A2A and A2B agonists have antiinflammatory effects independent of adenosine receptors. The authors report that psoriatic epidermis presents a deregulated adenosine receptor expression profile with reduced A2B and increased A2A...
January 2017: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/28007538/adenosine-a2a-receptor-deletion-affects-social-behaviors-and-anxiety-in-mice-involvement-of-anterior-cingulate-cortex-and-amygdala
#16
Laura López-Cruz, Maria Carbó-Gas, Marta Pardo, Pilar Bayarri, Olga Valverde, Catherine Ledent, John D Salamone, Mercè Correa
Blockade of adenosine A2A receptors can potentiate motivation to work for natural reinforcers such as food. Conspecific interaction is a potent natural reinforcer in social animals that can be manifested as preference for social exploration versus other sources of novel stimulation. Deficiencies in this type of motivated behavior (social withdrawal) have been seen in several pathologies such as autism and depression. However, the role of A2A receptors in motivation for social interaction has not been widely explored...
December 19, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27994068/resetting-microbiota-by-lactobacillus-reuteri-inhibits-t-reg-deficiency-induced-autoimmunity-via-adenosine-a2a-receptors
#17
Baokun He, Thomas K Hoang, Ting Wang, Michael Ferris, Christopher M Taylor, Xiangjun Tian, Meng Luo, Dat Q Tran, Jain Zhou, Nina Tatevian, Fayong Luo, Jose G Molina, Michael R Blackburn, Thomas H Gomez, Stefan Roos, J Marc Rhoads, Yuying Liu
Regulatory T (T reg) cell deficiency causes lethal, CD4(+) T cell-driven autoimmune diseases. Stem cell transplantation is used to treat these diseases, but this procedure is limited by the availability of a suitable donor. The intestinal microbiota drives host immune homeostasis by regulating the differentiation and expansion of T reg, Th1, and Th2 cells. It is currently unclear if T reg cell deficiency-mediated autoimmune disorders can be treated by targeting the enteric microbiota. Here, we demonstrate that Foxp3(+) T reg cell deficiency results in gut microbial dysbiosis and autoimmunity over the lifespan of scurfy (SF) mouse...
January 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/27986907/cutting-edge-adenosine-a2a-receptor-signals-inhibit-germinal-center-t-follicular-helper-cell-differentiation-during-the-primary-response-to-vaccination
#18
Shirdi E Schmiel, Jessica A Yang, Marc K Jenkins, Daniel L Mueller
Adenosine A2a receptor (A2aR) signaling acts as a barrier to autoimmunity by promoting anergy, inducing regulatory T cells, and inhibiting effector T cells. However, in vivo effects of A2aR signaling on polyclonal CD4 T cells during a primary response to foreign Ag has yet to be determined. To address this problem, we immunized mice with peptide Ag 2W1S coupled to PE in CFA and treated with the selective A2aR agonist CGS-21680 (CGS). 2W1S:I-A(b)-specific tetramer-binding CD4 T cells did not become anergic or differentiate into Foxp3(+) regulatory T cells...
January 15, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/27981581/dissecting-neurovascular-coupling-mechanisms-a-role-for-adenosine-a2a-receptor-an-editorial-highlight-for-correlation-of-transient-adenosine-release-and-oxygen-changes-in-the-caudate-putamen
#19
EDITORIAL
Nicholas Dale, Ana Maria Sebastião
Read the highlighted article 'Correlation of transient adenosine release and oxygen changes in the caudate-putamen' on page 13.
January 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/27974933/effects-of-caffeine-on-locomotor-activity-in-streptozotocin-induced-diabetic-rats
#20
Bădescu Sv, Tătaru Cp, Kobylinska L, Georgescu El, Zahiu Dm, Zăgrean Am, Zăgrean L
Diabetes mellitus modifies the expression of adenosine receptors in the brain. Caffeine acts as an antagonist of A1 and A2A adenosine receptors and was shown to have a dose-dependent biphasic effect on locomotion in mice. The present study investigated the link between diabetes and locomotor activity in an animal model of streptozotocin-induced diabetes, and the effects of a low-medium dose of caffeine in this relation. The locomotor activity was investigated by using Open Field Test at 6 weeks after diabetes induction and after 2 more weeks of chronic caffeine administration...
July 2016: Journal of Medicine and Life
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