Genomes and Genes
adenosine a2a receptor
Summary: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
Publications312 found, 100 shown here
- Neuroprotection by adenosine A2A receptor blockade in experimental models of Parkinson's diseaseKen Ikeda
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co, Ltd, Nagaizumi, Sunto, Shizuoka, Japan
J Neurochem 80:262-70. 2002..We therefore conclude that the adenosine A2A receptor may provide a novel target for the long-term medication of Parkinson's disease, because blockade of this ..
- Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonistsMing Yang
Department of Pharmacology, CV Therapeutics, Inc, Palo Alto, CA 94304, USA
Naunyn Schmiedebergs Arch Pharmacol 375:133-44. 2007..Among the six A2A-antagonists, KW-6002 is the best for use in in vivo animal studies, particularly for a CNS target, based on its bioavailability, half life, and brain penetration...
- A(2A) adenosine receptor deficiency attenuates brain injury induced by transient focal ischemia in miceJ F Chen
Molecular Neurobiology Laboratory, Department of Neurology, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts 02114, USA
J Neurosci 19:9192-200. 1999....
- Dopamine D2 receptor dysfunction is rescued by adenosine A2A receptor antagonism in a model of DYT1 dystoniaFrancesco Napolitano
CEINGE Biotecnologie Avanzate, Naples, Italy
Neurobiol Dis 38:434-45. 2010....
- Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell deathLeonóra Himer
Department of Pharmacology, Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary
FASEB J 24:2631-40. 2010..The antiapoptotic effect of A(2A) receptor stimulation was mediated by protein kinase A. Together, these results demonstrate that A(2A) receptor activation suppresses the AICD of peripheral T cells...
- Receptor heteromerization in adenosine A2A receptor signaling: relevance for striatal function and Parkinson's diseaseK Fuxe
Department of Neuroscience, Karolinska Institute, Stockholm, Sweden
Neurology 61:S19-23. 2003....
- Adenosine A2A receptor blockade prevents synaptotoxicity and memory dysfunction caused by beta-amyloid peptides via p38 mitogen-activated protein kinase pathwayPaula M Canas
Center for Neuroscience of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
J Neurosci 29:14741-51. 2009....
- Receptors for purines and pyrimidinesV Ralevic
School of Biomedical Sciences, Queen s Medical Centre, University of Nottingham, Nottingham, England
Pharmacol Rev 50:413-92. 1998
- Local glutamate level dictates adenosine A2A receptor regulation of neuroinflammation and traumatic brain injuryShuang Shuang Dai
Molecular Biology Center, State Key Laboratory of Trauma, Burn, and Combined Injury, Research Institute of Surgery and Daping Hospital, Third Military Medical University, Chongqing 400042, China
J Neurosci 30:5802-10. 2010..These findings identify a novel role for glutamate in modulation of neuroinflammation and brain injury via the adenosine-A(2A)R system...
- Adenosine A2A receptor activation reduces proinflammatory events and decreases cell death following intracerebral hemorrhageM Mayne
Department of Pharmacology, University of Manitoba, Winnipeg, Canada
Ann Neurol 49:727-35. 2001..These results suggest that pharmacological strategies targeting A2A receptors may provide effective inhibition of acute neurotoxic proinflammatory events that occur following intracerebral hemorrhage...
- Synergistic up-regulation of vascular endothelial growth factor expression in murine macrophages by adenosine A(2A) receptor agonists and endotoxinSamuel Joseph Leibovich
Department of Cell Biology and Molecular Medicine, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, New Jersey 07103, USA
Am J Pathol 160:2231-44. 2002....
- Adenosine promotes wound healing and mediates angiogenesis in response to tissue injury via occupancy of A(2A) receptorsM Carmen Montesinos
Department of Medicine, New York University School of Medicine, New York, New York, USA
Am J Pathol 160:2009-18. 2002..Thus, targeting the adenosine A(2A) receptor is a novel approach to promoting wound healing and angiogenesis in normal individuals and those suffering from chronic wounds...
- Adenosine A2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson's disease: a double-blind, randomized, multicenter clinical trial (6002-US-005)Peter A LeWitt
Department of Neurology, Henry Ford Hospital, Southfield, MI 48034, USA
Ann Neurol 63:295-302. 2008..Based on new understanding of nondopaminergic pathways involved in Parkinson's disease (PD) pathophysiology, a selective adenosine A(2A) receptor antagonist, istradefylline, shows promise for the treatment of PD...
- Adenosine A2A receptor stimulation potentiates nitric oxide release by activated microgliaJosep Saura
Department of Pharmacology and Toxicology, IIBB, CSIC, IDIBAPS, Barcelona, Spain
J Neurochem 95:919-29. 2005....
- Adenosine A2A receptor activation limits graft-versus-host disease after allogenic hematopoietic stem cell transplantationCourtney M Lappas
Department of Biology, Lebanon Valley College, Annville, Pennsylvania, USA
J Leukoc Biol 87:345-54. 2010..We conclude that the selective activation of the A(2A)R has therapeutic potential in the prevention and treatment of acute GVHD...
- Adenosine A2A receptor agonists promote more rapid wound healing than recombinant human platelet-derived growth factor (Becaplermin gel)Cassandre Victor-Vega
Department of Medicine, New York University School of Medicine, NY 10016, USA
Inflammation 26:19-24. 2002Animal studies of the topical application of adenosine A2A receptor agonists show that it promotes wound closure...
- GPCR 3D homology models for ligand screening: lessons learned from blind predictions of adenosine A2a receptor complexVSEVOLOD KATRITCH
Molsoft LLC, 3366 N Torrey Pines Court, La Jolla, California 92037, USA
Proteins 78:197-211. 2010..A recently performed assessment of blind predictions of adenosine A2a receptor (AA2AR) structure in complex with ZM241385 (ZMA) antagonist provided a first example of unbiased ..
- Adenosine A2A receptor antagonism increases nNOS-immunoreactive neurons in the striatum of Huntington transgenic miceS Cipriani
Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50139 Firenze, Italy
Exp Neurol 213:163-70. 2008..We suggest that the protective effect of A(2A) antagonism in HD is related to the increase in striatal nNOS-IR neurons...
- Adenosine A(2A) receptor activation promotes wound neovascularization by stimulating angiogenesis and vasculogenesisM Carmen Montesinos
Departments of Medicine and Surgery, The Veterans Administration New York Harbor Healthcare System, New York University Cancer Institute, New York University School of Medicine, New York, New York, USA
Am J Pathol 164:1887-92. 2004....
- Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonistsVSEVOLOD KATRITCH
Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
J Med Chem 53:1799-809. 2010..High success rate, novelty, and diversity of the chemical scaffolds and strong ligand efficiency of the A(2A)AR antagonists identified in this study suggest practical applicability of receptor-based VLS in GPCR drug discovery...
- Adenosine A2A receptor antagonists exert motor and neuroprotective effects by distinct cellular mechanismsLiqun Yu
Department of Neurology, Boston University School of Medicine, Boston, MA 02118, USA
Ann Neurol 63:338-46. 2008..To investigate whether the motor and neuroprotective effects of adenosine A(2A) receptor (A(2A)R) antagonists are mediated by distinct cell types in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) model of Parkinson's disease...
- Adenosine A2A receptor activation reduces infarct size in the isolated, perfused mouse heart by inhibiting resident cardiac mast cell degranulationTyler H Rork
Robert M Berne Cardiovascular Research Center, University of Virginia Health System, Charlottesville, VA, USA
Am J Physiol Heart Circ Physiol 295:H1825-33. 2008..In addition, our data suggest that A2AAR activation is cardioprotective in the isolated heart, at least in part by attenuating resident mast cell degranulation...
- Enhanced neuronal damage by co-administration of quinolinic acid and free radicals, and protection by adenosine A2A receptor antagonistsW M H Behan
Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, UK
Br J Pharmacol 135:1435-42. 2002..The site of interaction is probably distal to the NMDA receptor. Blockade of adenosine A(2A) receptors can protect against this combined damage, suggesting potential value in the prevention of brain damage...
- Adenosine A2A receptor occupancy stimulates collagen expression by hepatic stellate cells via pathways involving protein kinase A, Src, and extracellular signal-regulated kinases 1/2 signaling cascade or p38 mitogen-activated protein kinase signaling pathJiantu Che
Department of Medicine, New York University School of Medicine, 550 First Avenue, New York, NY 10016, USA
Mol Pharmacol 72:1626-36. 2007Prior studies indicate that adenosine and the adenosine A2A receptor play a role in hepatic fibrosis by a mechanism that has been proposed to involve direct stimulation of hepatic stellate cells (HSCs)...
- Myocardial infarct-sparing effect of adenosine A2A receptor activation is due to its action on CD4+ T lymphocytesZequan Yang
Department of Biomedical Engineering, University of Virginia Health System, Box 800759, Charlottesville, VA 22903, USA
Circulation 114:2056-64. 2006We previously used adenosine A2A receptor (A2AR) knockout (KO) mice and bone marrow transplantation to show that the infarct-sparing effect of A2AR activation at reperfusion is primarily due to effects on bone marrow-derived cells...
- A differential role for the adenosine A2A receptor in opiate reinforcement vs opiate-seeking behaviorRobyn Mary Brown
Brain Injury and Repair Group, Howard Florey Institute, University of Melbourne, Parkville, Vic, Australia
Neuropsychopharmacology 34:844-56. 2009..Collectively, these data suggest a differential role for adenosine A(2A) receptors in opiate reinforcement compared to opiate-seeking...
- Differential expression of adenosine receptors in human endothelial cells: role of A2B receptors in angiogenic factor regulationIgor Feoktistov
Division of Cardiology, Vanderbilt University, Nashville, Tenn 37232 6300, USA
Circ Res 90:531-8. 2002..A2B receptors, predominantly expressed in human microvascular cells, modulate expression of angiogenic factors via coupling to G(q), and possibly via G12/13...
- Adenosine A2A receptor blockade or deletion diminishes fibrocyte accumulation in the skin in a murine model of scleroderma, bleomycin-induced fibrosisMajid Katebi
Division of Clinical Pharmacology, Department of Medicine, New York University School of Medicine, 550 First Ave, New York, NY 10016, USA
Inflammation 31:299-303. 2008..Moreover, these results provide further evidence that adenosine A(2A) receptors may represent a new target for the treatment of such fibrosing diseases as scleroderma or nephrogenic fibrosing dermopathy...
- Adenosine A2A receptor antagonism increases striatal glutamate outflow in dopamine-denervated ratsClaudia Corsi
Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50139, Florence, Italy
Eur J Pharmacol 464:33-8. 2003..These results may be relevant to our understanding of the mechanism of action of adenosine A(2A) receptor antagonists in Parkinson's disease...
- Adenosine A2A receptor antagonists: blockade of adenosinergic effects and T regulatory cellsM Sitkovsky
New England Inflammation and Tissue Protection Institute, Consortium at Northeastern University, 113 Mugar Building, 360 Huntington Avenue, Boston, MA 02115, USA
Br J Pharmacol 153:S457-64. 2008..This review addresses several possible pharmacological modalities to block adenosinergic pathways and speculates on their future application together with impacts on human disease...
- Genes for prostaglandin d synthase and receptor as well as adenosine A2A receptor are involved in the homeostatic regulation of nrem sleepO Hayaishi
Department of Molecular Behavioral Biology, Osaka Bioscience Institute, 6 2 4 Furuedai, Suita, Osaka 5650874, Japan
Arch Ital Biol 142:533-9. 2004....
- Adenosine A2A receptor deficiency exacerbates white matter lesions and cognitive deficits induced by chronic cerebral hypoperfusion in miceWei Duan
Department of Neurology, Xinqiao Hospital, Third Military Medical University, 2 V Xinqiao Street, Chongqing 400037, PR China
J Neurol Sci 285:39-45. 2009b>Adenosine A2A receptor inactivation consistently protects against acute ischemic brain injury; however, the role of the A2A receptor in chronic cerebral ischemia is unknown...
- Genetic deletion of the adenosine A2A receptor confers postnatal development of relative myopia in miceXiangtian Zhou
School of Optometry and Ophthalmology and Eye Hospital, Wenzhou Medical College, Wenzhou, China
Invest Ophthalmol Vis Sci 51:4362-70. 2010To critically evaluate whether the adenosine A2A receptor (A2AR) plays a role in postnatal refractive development in mice.
- Adenosine A2A receptor stimulation increases angiogenesis by down-regulating production of the antiangiogenic matrix protein thrombospondin 1Avani Desai
Department of Medicine, New York University School of Medicine, New York, New York 10016, USA
Mol Pharmacol 67:1406-13. 2005Topical adenosine A2A receptor agonists promote wound healing by, among other effects, increasing microvessel formation...
- A critical role of the adenosine A2A receptor in extrastriatal neurons in modulating psychomotor activity as revealed by opposite phenotypes of striatum and forebrain A2A receptor knock-outsHai Ying Shen
Molecular Neuropharmacology Laboratory, Department of Neurology, Boston University School of Medicine, Boston, Massachusetts 02118, USA
J Neurosci 28:2970-5. 2008..These results indicate that A(2A)Rs in striatal and extrastriatal neurons exert an opposing modulation of psychostimulant effects and provide the first direct demonstration of a predominant facilitatory role of extrastriatal A(2A)Rs...
- Effect of the adenosine A2a receptor antagonist 3,7-dimethyl-propargylxanthine on anxiety-like and depression-like behavior and alcohol consumption in Wistar RatsAnnika Thorsell
Laboratory of Clinical and Translational Studies, NIAAA, NIH, Bethesda, Maryland 20892 1108, USA
Alcohol Clin Exp Res 31:1302-7. 2007..We therefore examined the effect of the adenosine A2a receptor antagonist 3,7-dimethylpropargylxanthine (DMPX, 3, and 10 mg/kg intraperitoneal) on alcohol reinforcement, ..
- Adenosine A2a receptor induced gliosis via Akt/NF-kappaB pathway in vitroRong Hu Ke
Department of Pathology, Shanghai Medical College, Fudan University, No 138, Yi Xue Yuan Road, Shanghai 200032, China
Neurosci Res 65:280-5. 2009..This study explores the role of the adenosine A2a receptor (A2aR) in gliosis after ischemia-like injury in a rat astrocyte cell line transfected with A2aR...
- Adenosine A2A receptor-selective stimulation reduces signaling pathways involved in the development of intestine ischemia and reperfusion injuryRosanna Di Paola
IRCCS Centro Neurolesi Bonino Pulejo, School of Medicine, University of Messina, Messina, Italy
Shock 33:541-51. 2010In the present study, we tested the efficacy of treatment with the selective adenosine A2A receptor agonist 2-[p-(2-carboxyethyl)phenylethylamino]-50-ethylcarboxamidoadenosine (CGS 21680) on ischemia and reperfusion injury of the ..
- Adenosine A2A receptor activation on CD4+ T lymphocytes and neutrophils attenuates lung ischemia-reperfusion injuryAshish K Sharma
Department of Surgery, University of Virginia Health System, Charlottesville, VA 22908, USA
J Thorac Cardiovasc Surg 139:474-82. 2010..This study tests the hypothesis that adenosine A(2A) receptor activation attenuates ischemia-reperfusion injury by inhibiting CD4+ T cell activation and subsequent neutrophil infiltration...
- Protective effect of adenosine A2A receptor activation in small-for-size liver transplantationLi Ming Tang
The Liver Transplantation Center of the First Affiliated Hospital, Nanjing Medical University, Nanjing, Jiangsu Province, China
Transpl Int 20:93-101. 2007..Our findings provide the rationale for a novel therapeutic approach using A(2A)R activation to maximize the availability of small-for-size liver grafts...
- Upregulation of striatal adenosine A2A receptor mRNA in 6-hydroxydopamine-lesioned rats intermittently treated with L-DOPAMasahiko Tomiyama
Third Department of Medicine, Hirosaki University School of Medicine, Hirosaki 036 8216, Japan
Synapse 52:218-22. 2004To determine whether the adenosine A2A receptor might play a role in L-DOPA-induced dyskinesia in Parkinson's disease, we analyzed changes in the expression of A2A receptor mRNA in response to intermittent treatment with L-DOPA in rats ..
- Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritisGabriela E Garcia
Department of Medicine, Nephrology Section, Alkek N520, One Baylor Plaza, Houston TX, 77030, USA
FASEB J 22:445-54. 2008..Accordingly, pharmacological activation of A(2A)R could be developed into a novel treatment for glomerulonephritis and other macrophage-related inflammatory diseases...
- Linear and nonlinear 3D-QSAR approaches in tandem with ligand-based homology modeling as a computational strategy to depict the pyrazolo-triazolo-pyrimidine antagonists binding site of the human adenosine A2A receptorLisa Michielan
Molecular Modeling Section, Dipartimento di Scienze Farmaceutiche, Universita di Padova, Via Marzolo 5, I 35131 Padova, Italy
J Chem Inf Model 48:350-63. 2008..computational techniques has been used to depict the hypothetical antagonist binding site of the human adenosine A2A receptor. In particular, a collection of 127 known human A2A antagonists has been utilized to derive two 3D-QSAR ..
- Differential expression of adenosine A3 receptors controls adenosine A2A receptor-mediated inhibition of TLR responses in microgliaCéline van der Putten
Alternatives Unit, Biomedical Primate Research Centre, Rijswijk, The Netherlands
J Immunol 182:7603-12. 2009..This would suggest exploration of combinations of A(2A)R agonists and A(3)R antagonists to dampen microglial activation during chronic neuroinflammatory conditions...
- Arachidonic acid activates phospholipase D in human neutrophils; essential role of endogenous leukotriene B4 and inhibition by adenosine A2A receptor engagementSonya Grenier
Canadian Institutes for Health Research Group on the Molecular Mechanisms of Inflammation, Centre de Recherche en Rhumatologie et Immunologie, Quebec, Canada
J Leukoc Biol 73:530-9. 2003..These results provide evidence of a requirement for an autocrine-stimulatory loop involving LTB(4) and BLTR1 in the translocation of small GTPases to membranes and the activation of PMN PLD by AA...
- The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slicesA M Pugliese
Department of Preclinical and Clinical Pharmacology, University of Florence, Florence, Italy
Br J Pharmacol 157:818-30. 2009..Activation of adenosine A(2A) receptors in the CA1 region of rat hippocampal slices during oxygen-glucose deprivation (OGD), a model of cerebral ischaemia, was investigated...
- Modulation of orphan nuclear receptor NURR1 expression by methotrexate in human inflammatory joint disease involves adenosine A2A receptor-mediated responsesJennifer A Ralph
Department of Veterinary Biochemistry and Physiology, Conway Institute of Biomolecular and Biomedical Research, University College Dublin, Belfield, Ireland
J Immunol 175:555-65. 2005....
- Adenosine A2A receptor antagonists improve deficits in initiation of movement and sensory motor integration in the unilateral 6-hydroxydopamine rat model of Parkinson's diseaseAnnalisa Pinna
Section of Cagliari, CNR Institute of Neuroscience, Cagliari, Italy
Synapse 61:606-14. 2007....
- Adenosine A2A receptor dysfunction correlates with age at onset anticipation in blood platelets of subjects with Huntington's diseaseV Maglione
Neurogenetics Unit, IRCCS Neuromed, Pozzilli, Italy
Am J Med Genet B Neuropsychiatr Genet 139:101-5. 2005..48, P = 0.0001 by linear correlation analysis). An increased platelet A(2A) receptor B(max) may belong in a cascade of toxic events leading to earlier onset of HD: as such it could be a useful marker of onset anticipation...
- The adenosine A2A receptor agonist CGS 21680 fails to ameliorate the course of dextran sulphate-induced colitis in miceZ Selmeczy
Department of Pharmacology, Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary
Inflamm Res 56:204-9. 2007In this study we investigated the effect of CGS 21680 (2-p-(2-Carboxyethyl)phenethylamino-5-N-ethylcarboxamidoadenosine hydrochloride), an adenosine A2A receptor agonist, in a model of dextran sulphate sodium (DSS)-induced colitis.
- Adenosine A2A receptor activation: another potential therapy for trauma and hemorrhagic shockRongqian Wu
Crit Care Med 34:1273-5. 2006
- Monoamine oxidase B inhibition and neuroprotection: studies on selective adenosine A2A receptor antagonistsNeal Castagnoli
Department of Chemistry, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061 0212, USA
Neurology 61:S62-8. 2003..b>Adenosine A2A receptor antagonists (e.g...
- Recent advances in the design and optimization of adenosine A2A receptor antagonistsChi B Vu
Biogen Idec Inc, Department of Medicinal Chemistry, 14 Cambridge Center, Cambridge, MA 02142, USA
Curr Opin Drug Discov Devel 8:458-68. 2005In recent years, the adenosine A2A receptor has gained interest as a potential therapeutic target for alleviating the symptoms of Parkinson's disease...
- Optimization of the human adenosine A2a receptor yields in Saccharomyces cerevisiaeAlison Wedekind
Chemical Engineering Department, University of Delaware, Newark, Delaware 19716, USA
Biotechnol Prog 22:1249-55. 2006..When compared to other reports of GPCR expression in yeast it is clear that this system is among those producing the highest GPCR protein yields per culture both before and after optimization...
- Adenosine A2A receptor activation decreases reperfusion injury associated with high-flow reperfusionSteven M Fiser
Department of Thoracic and Cardiovascular Surgery, University of Virginia Health Sciences Center, Charlottesville, VA 22908, USA
J Thorac Cardiovasc Surg 124:973-8. 2002..Our hypothesis was that selective activation of the adenosine A(2A) receptor with a highly specific analog (ATL-146e) would inhibit leukocyte activation and decrease reperfusion injury after high-flow reperfusion...
- Effect of the adenosine A2A receptor antagonist 8-(3-chlorostyryl)caffeine on L-DOPA biotransformation in rat striatumKrystyna Gołembiowska
Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31 343 Krakow, Poland
Brain Res 998:208-17. 2004In the present study, we investigated effects of the new selective adenosine A2A receptor antagonist 8-(3-chlorostyryl)caffeine (CSC) on L-DOPA-induced dopamine (DA) release in the striatum of intact and reserpine-treated rats...
- Adenosine A2a receptor-mediated, normoxic induction of HIF-1 through PKC and PI-3K-dependent pathways in macrophagesCristina De Ponti
Istituto di Patologia Generale, Universita di Milano, Italy
J Leukoc Biol 82:392-402. 2007....
- Inactivation of adenosine A2A receptor impairs long term potentiation in the accumbens nucleus without altering basal synaptic transmissionP d'Alcantara
Laboratory of Neurophysiology, Department of Neuroscience, Universite Libre de Bruxelles, Brussels, Begium
Neuroscience 107:455-64. 2001....
- Adenosine A2A receptor signaling and golf assembly show a specific requirement for the gamma7 subtype in the striatumWilliam F Schwindinger
Weis Center for Research, Geisinger Clinic, Danville, Pennsylvania 17822, USA
J Biol Chem 285:29787-96. 2010..Collectively, these results further support the A(2A)R G-protein α(olf)β(2)γ(7) interface as a possible therapeutic target for Parkinson disease...
- DNA methylation and Yin Yang-1 repress adenosine A2A receptor levels in human brainSandra P Buira
Institut de Neuropatologia, Servei d Anatomia Patològica, IDIBELL Hospital Universitari de Bellvitge, L Hospitalet de Llobregat, Spain
J Neurochem 115:283-95. 2010....
- Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in ratsElisabetta Tronci
Department of Toxicology, University of Cagliari, Italy
Eur J Pharmacol 566:94-102. 2007Antagonism of adenosine A2A receptor function has been proposed as an effective therapy in the treatment of Parkinson's disease...
- Behavioral and electrophysiological effects of the adenosine A2A receptor antagonist SCH 58261 in R6/2 Huntington's disease miceM R Domenici
Department of Drug Research and Evaluation, Istituto Superiore di Sanita, Viale Regina Elena, 299, 00161, Rome, Italy
Neurobiol Dis 28:197-205. 2007The effect of chronic treatment with the selective adenosine A2A receptor antagonist SCH 58261 on the behavioral and electrophysiological alterations typical of R6/2 mice (a transgenic mouse model of Huntington's disease, HD), has been ..
- Adenosine A2A receptor antagonists as novel anti-Parkinsonian agents: a review of structure-activity relationshipsF Azam
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Seventh of October University, Misurata, Libya
Pharmazie 64:771-95. 2009The adenosine A2A receptor (AA2AR) has emerged as an attractive target for the treatment of Parkinson's disease...
- Adenosine A2A receptor stimulation decreases GAT-1-mediated GABA uptake in the globus pallidus of the ratBrenda Gonzalez
Departamento de Fisiologia, Biofisica y Neurociencias, Centro de Investigacion y de Estudios Avanzados, Apartado Postal 14 740, 07000 Mexico DF, Mexico
Neuropharmacology 51:154-9. 2006..2microM) are within the range measured in the interstitial fluid under some physiological conditions. Thus, inhibition of uptake may be important in increasing interstitial GABA during endogenous adenosine release...
- Blocking adenosine A2A receptor reduces peritoneal fibrosis in two independent experimental modelsSigal Nakav
Department of Clinical Biochemistry, Soroka Medical Center and Ben Gurion University of the Negev, Beer Sheva, Israel
Nephrol Dial Transplant 24:2392-9. 2009..We have previously shown that adenosine is a potent regulator of inflammation in the peritoneum. In the current study, we explored the role of adenosine and the A(2A)R in two experimental models...
- The selective adenosine A2A receptor agonist CGS 21680 reduces JNK MAPK activation in oligodendrocytes in injured spinal cordTiziana Genovese
IRCCS Centro Neurolesi Bonino Pulejo, Messina, Italy
Shock 32:578-85. 2009..Although functional studies indicate a protective effect of adenosine A2A receptor agonists in SCI, the basic molecular mechanisms accounting for the their protective effects from SCI have ..
- New aspects of physiological and pathophysiological functions of adenosine A2A receptor in basal gangliaH Kase
Pharmaceutical Research and Development Division, Kyowa Hakko Kogyo Co Ltd, Tokyo, Japan
Biosci Biotechnol Biochem 65:1447-57. 2001..A2A receptor antagonists provide a novel therapeutic potential for the treatment of Parkinson's disease...
- Selective adenosine A2a receptor antagonism reduces JNK activation in oligodendrocytes after cerebral ischaemiaAlessia Melani
Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini, 6, Florence, Italy
Brain 132:1480-95. 2009....
- Theophylline induces neutrophil apoptosis through adenosine A2A receptor antagonismK Yasui
Department of Pediatrics, Shinshu University School of Medicine, Matsumoto, Japan
J Leukoc Biol 67:529-35. 2000..was designed to determine whether theophylline would augment granulocyte apoptosis via a mechanism of adenosine A2A receptor antagonism...
- Adenosine A2A receptor-mediated cell death of mouse thymocytes involves adenylate cyclase and Bim and is negatively regulated by Nur77Ildiko Kiss
Department of Biochemistry and Molecular Biology, Signaling and Apoptosis Research Group, Hungarian Academy of Sciences, Research Center of Molecular Medicine, University of Debrecen
Eur J Immunol 36:1559-71. 2006..Collectively our data demonstrate that adenosine-induced cell death involves signaling pathways originally found in negative selection of thymocytes and suggest a determining role of Bim and a regulatory role for Nur77...
- PAP 9704, a Korean herbal medicine attenuates methamphetamine-induced hyperlocomotion via adenosine A2A receptor stimulation in miceYong Soo Kwon
Neurotoxicology Program, College of Pharmacy, Kangwon National University, Chunchon, Korea
Biol Pharm Bull 27:906-9. 2004..5 or 3.0 mg/kg, i.p.) did not significantly affect this pharmacological action. Our results suggest that PAP 9704 prevents MA-induced hyperlocomotion, at least in part, via the stimulation of the adenosine A(2A) receptor...
- Rapid modification of the glycocalyx caused by ischemia-reperfusion is inhibited by adenosine A2A receptor activationSteven H Platts
Department of Molecular Physiology and Biological Physics, University of Virginia, Charlottesville 22908, USA
Am J Physiol Heart Circ Physiol 284:H2360-7. 2003..The modifications of the glycocalyx appear to be an early step in the inflammatory cascade typically associated with reperfusion injury, and adenosine A(2A) receptor activation may play a role in protection from this injury...
- Adenosine A2A receptor occupancy stimulates expression of proteins involved in reverse cholesterol transport and inhibits foam cell formation in macrophagesAllison B Reiss
Department of Medicine, New York University School of Medicine, New York, NY, USA
J Leukoc Biol 76:727-34. 2004..Prior studies have suggested occupancy of the anti-inflammatory adenosine A2A receptor (A2AR) minimizes early atherosclerotic changes in arteries following injury...
- Suppression of inflammation by low-dose methotrexate is mediated by adenosine A2A receptor but not A3 receptor activation in thioglycollate-induced peritonitisM Carmen Montesinos
Department of Pharmacology, Universidad de Valencia, Burjassot, Valencia, Spain
Arthritis Res Ther 8:R53. 2006..75 mg/kg/week) in a model of acute peritoneal inflammation in adenosine A2A receptor knockout mice and A3 receptor knockout mice and their wild-type littermates...
- Spinal adenosine A2a receptor activation elicits long-lasting phrenic motor facilitationFrancis J Golder
Department of Comparative Biosciences, University of Wisconsin, Madison, Wisconsin 53706, USA
J Neurosci 28:2033-42. 2008....
- Genetic and pharmacological inactivation of the adenosine A2A receptor attenuates 3-nitropropionic acid-induced striatal damageJ Stephen Fink
Department of Neurology, Boston University School of Medicine, MA 02118, USA
J Neurochem 88:538-44. 2004b>Adenosine A2A receptor (A2AR) antagonism attenuates 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced dopaminergic neurodegeneration and quinolinic acid-induced excitotoxicity in the neostriatum...
- Synergistic up-regulation of vascular endothelial growth factor (VEGF) expression in macrophages by adenosine A2A receptor agonists and endotoxin involves transcriptional regulation via the hypoxia response element in the VEGF promoterMadhuri Ramanathan
Department of Cell Biology and Molecular Medicine, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, NJ 07103, USA
Mol Biol Cell 18:14-23. 2007Macrophages are an important source of vascular endothelial growth factor (VEGF). Adenosine A2A receptor (A2AR) agonists with Toll-like receptor (TLR) 2, 4, 7, and 9 agonists synergistically induce macrophage VEGF expression...
- Adenosine A2A receptor activation reduces hepatic ischemia reperfusion injury by inhibiting CD1d-dependent NKT cell activationCourtney M Lappas
Department of Pharmacology, University of Virginia, Charlottesville, VA 2290, USA
J Exp Med 203:2639-48. 2006..These findings suggest that hepatic reperfusion injury is initiated by the CD1d-dependent activation of NKT cells, and the activation of these cells is inhibited by A2AR activation...
- Cellular and behavioural effects of the adenosine A2a receptor antagonist KW-6002 in a rat model of l-DOPA-induced dyskinesiaM Lundblad
Department of Physiological Sciences, Wallenberg Neuroscience Centre, Neurobiology Division, Lund, Sweden
J Neurochem 84:1398-410. 2003..These results show that monotreatment with an adenosine A2a receptor antagonist can relieve motor disability without inducing behavioural and cellular signs of dyskinesia in ..
- Triggering neurotrophic factor actions through adenosine A2A receptor activation: implications for neuroprotectionAna M Sebastião
Institute of Pharmacology and Neurosciences, Faculty of Medicine, University of Lisbon, Lisbon, Portugal
Br J Pharmacol 158:15-22. 2009..Evidence has, however, accumulated showing that tonic adenosine A2A receptor activity is a required step to allow synaptic actions of neurotrophic factors, namely upon synaptic ..
- Adenosine inhibits IL-12 and TNF-[alpha] production via adenosine A2a receptor-dependent and independent mechanismsG Hasko
Inotek Corp, Beverly, Massachusetts 01915, USA
FASEB J 14:2065-74. 2000..In summary, adenosine inhibits IL-12 production via various adenosine receptors. These results support the notion that adenosine-based therapies might be useful in certain autoimmune and/or inflammatory diseases...
- Adenosine closes the K+ channel KCa3.1 in human lung mast cells and inhibits their migration via the adenosine A2A receptorS Mark Duffy
Department of Infection, Immunity and Inflammation, Institute for Lung Health, University of Leicester, and Glenfield Hospital, Leicester, UK
Eur J Immunol 37:1653-62. 2007..KCa3.1 suppression by adenosine was reversed partially by the selective adenosine A2A receptor antagonist ZM241385 but not by the A2B receptor antagonist MRS1754, and the effects of adenosine were ..
- Co-evolving stability and conformational homogeneity of the human adenosine A2a receptorFrancesca Magnani
Medical Research Council, Laboratory of Molecular Biology, Hills Road, Cambridge CB2 0QH, United Kingdom
Proc Natl Acad Sci U S A 105:10744-9. 2008..The mutant receptors both showed markedly improved stability in short-chain alkyl-glucoside detergents compared with the wild-type receptor, which will facilitate their structural analysis...
- Effects of adenosine A2A receptor stimulation on cocaine-seeking behavior in ratsRyan K Bachtell
Department of Psychology and Neuroscience, University of Colorado, UCB 345, Boulder, CO 80309 0345, USA
Psychopharmacology (Berl) 206:469-78. 2009..Adenosine receptors antagonize the effects of DA receptor stimulation on intracellular signaling, neuronal output, and behavior...
- Adenosine A2A receptor blockade differentially influences excitotoxic mechanisms at pre- and postsynaptic sites in the rat striatumMaria Teresa Tebano
Department of Pharmacology, Istituto Superiore di Sanita, Rome, Italy
J Neurosci Res 77:100-7. 2004..This indicates that the neuroprotective potential of A(2A) antagonists may be evident mainly in models of neurodegeneration in which presynaptic mechanisms play a major role...
- Cross-regulation of carbon monoxide and the adenosine A2a receptor in macrophagesArvand Haschemi
Transplant and Immunobiology Research Centers, Department of Surgery, Beth Israel Deaconess Medical Center, Harvard Medical School, 99 Brookline Avenue, Boston, MA 02215, USA
J Immunol 178:5921-9. 2007..Taken together, these data suggest the existence of a positive feedback loop among adenosine, HO-1, CO, and the A2aR in the chronological resolution of the inflammatory response...
- The protective effect of adenosine A2A receptor antagonism in cerebral ischemiaF Pedata
Department of Preclinical and Clinical Pharmacology, University of Florence, V le Pieraccini 6, 50139 Florence, Italy
Neurol Res 27:169-74. 2005..We reviewed our most recent work on the protective effect of adenosine A(2A)antagonism in cerebral ischemia...
- Infarct-sparing effect of A2A-adenosine receptor activation is due primarily to its action on lymphocytesZequan Yang
Department of Biomedical Engineering, of Virginia Health System, Charlottesville 22903, USA
Circulation 111:2190-7. 2005..A2A-adenosine receptor (A2AAR) activation on reperfusion after ischemia reduces the size of myocardial infarction, but the mechanism of action has not been fully defined...
- Effects of CGS 21680, a selective adenosine A2A receptor agonist, on allergic airways inflammation in the ratJohn R Fozard
Research Department, Novartis Pharma AG, WSJ 386 510, CH 4002, Basel, Switzerland
Eur J Pharmacol 438:183-8. 2002..anti-inflammatory and hypotensive responses to CGS 21680 were blocked by pretreatment with the selective adenosine A2A receptor antagonist, 4-(2-(7-amino-2-(2-furyl)(1,2,4)triazolo(2,3-a(1,3,5)triazin-5-yl amino)ethyl)phenol (ZM ..
- Adenosine A2A receptor antagonists and Parkinson's disease: state of the art and future directionsN Simola
Department of Toxicology and Centre of Excellence for Neurobiology of Dependence, University of Cagliari, Via Ospedale, 72, 09124 Cagliari, Italy
Curr Pharm Des 14:1475-89. 2008....
- Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout miceM El Yacoubi
UMR 6036 CNRS, IFRMP 23, , 22 Boulevard Gambetta, 76183 Rouen Cedex, France
Br J Pharmacol 134:68-77. 2001..2. We have designed studies to assess whether adenosine A2A receptor antagonists, or genetic inactivation of the receptor would be effective in established screening ..
- Cyclic AMP-dependent inhibition of human neutrophil oxidative activity by substituted 2-propynylcyclohexyl adenosine A(2A) receptor agonistsG W Sullivan
Department of Medicine, University of Virginia, Charlottesville, VA 22908
Br J Pharmacol 132:1017-26. 2001..The data indicate that activation of A(2A)ARs inhibits neutrophil oxidative activity by activating [cyclic AMP](i)/PKA...
- Design, synthesis, and evaluation of novel A2A adenosine receptor agonistsJ M Rieger
Department of Chemistry, University of Virginia, McCormick Road, P.O. Box 400319, Charlottesville, Virginia 22904-4319, USA
J Med Chem 44:531-9. 2001..891) that provides for enhanced A2A selectivity and predictability. Synthesis, pharmacological evaluation, and modeling of four novel ligands further validate the utility and predictive power (r2 = 0.626) of the CoMFA model...
- Effects of an adenosine A2A receptor blockade in the nucleus accumbens on locomotion, feeding, and prepulse inhibition in ratsJens Nagel
Department of Animal Physiology, University of Stuttgart, Pfaffenwaldring 57, D 70550 Stuttgart, Germany
Synapse 49:279-86. 2003..The data add further support to the view that adenosine is a tonically active modulator of striatal function through actions on A(2A) receptors...
- Additive protection against lung ischemia-reperfusion injury by adenosine A2A receptor activation before procurement and during reperfusionLeo M Gazoni
Department of Surgery, University of Virginia, Charlottesville 22908, USA
J Thorac Cardiovasc Surg 135:156-65. 2008b>Adenosine A2A receptor activation during reperfusion improves lung ischemia-reperfusion injury...
- Association studies of the adenosine A2a receptor (1976T > C) genetic polymorphism in Parkinson's disease and schizophreniaC J Hong
Department of Psychiatry, Taipei Veterans General Hospital, Taipei, Taiwan, ROC
J Neural Transm 112:1503-10. 2005..in schizophrenia and Parkinson's disease (PD), as well as the reciprocal antagonistic interactions between adenosine A2a receptor (A2aAR) and the dopamine D2 receptors, A2aAR may be a candidate gene conferring susceptibility to PD or ..
- Caffeine and a selective adenosine A2A receptor antagonist induce reward and sensitization behavior associated with increased phospho-Thr75-DARPP-32 in miceChih W Hsu
Department of Emergency Medicine, Tzu Chi General Hospital, Hualien 970, Taiwan
Psychopharmacology (Berl) 204:313-25. 2009....
- Caffeine attenuates the duration of coronary vasodilation and changes in hemodynamics induced by regadenoson (CVT-3146), a novel adenosine A2A receptor agonistGong Zhao
Department of Pharmacology and Preclinical Development, CV Therapeutics, Inc, Palo Alto, California, USA
J Cardiovasc Pharmacol 49:369-75. 2007..The results indicate that 1 to 10 mg/kg caffeine dose-dependently reduced the duration, but not the peak increase of CBF caused by 5 microg/kg regadenoson...
- Reduction of infarct size and postischemic inflammation from ATL-146e, a highly selective adenosine A2A receptor agonist, in reperfused canine myocardiumDavid K Glover
Department of Internal Medicine, Division of Cardiology, University of Virginia, PO Box 800500, UVA Health System, Cobb Hall, Rm 1010, Hospital Drive, Charlottesville, VA 22908 0500, USA
Am J Physiol Heart Circ Physiol 288:H1851-8. 2005..Such combination therapy may be beneficial clinically by potentiating cardioprotection after coronary reperfusion at doses far below those producing vasodilatation or side effects...
- Up-regulation of A(2A) adenosine receptors by proinflammatory cytokines in rat PC12 cellsMaria L Trincavelli
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, Italy
Biochem Pharmacol 64:625-31. 2002..The biological significance of this regulation might be associated with modulating cellular activity in response to tissue damage associated with inflammatory mediator production...
- Enhanced adenosine A2A receptor facilitation of synaptic transmission in the hippocampus of aged ratsNelson Rebola
Center for Neurosciences of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, Portugal
J Neurophysiol 90:1295-303. 2003....
- The Pharmacology of Dermal FibrosisBruce Cronstein; Fiscal Year: 2009..We have recently demonstrated that the purine nucleoside adenosine, acting through the adenosine A2A receptor, plays a central role in the fibrosis that develops in experimental models of hepatic cirrhosis and ..
- Adenosine, Toll-Like Receptors and AngiogenesisSamuel Joseph Leibovich; Fiscal Year: 2010..This pathway involves a synergistic interaction of TLR 2, 4, 7 or 9 and adenosine A2A receptor (A2AR) signaling. TLR agonists up-regulate A2AR expression. A2AR agonists then up-regulate HIF11-I...
- Adenosine, Toll-Like Receptors and AngiogenesisSAMUEL LEIBOVICH; Fiscal Year: 2009..This pathway involves a synergistic interaction of TLR 2, 4, 7 or 9 and adenosine A2A receptor (A2AR) signaling. TLR agonists up-regulate A2AR expression. A2AR agonists then up-regulate HIF11-I...
- The Pharmacology of Dermal FibrosisBruce Neil Cronstein; Fiscal Year: 2010..We have recently demonstrated that the purine nucleoside adenosine, acting through the adenosine A2A receptor, plays a central role in the fibrosis that develops in experimental models of hepatic cirrhosis and ..
- PHARMACOLOGY OF ANTIRHEUMATIC AGENTSBruce Cronstein; Fiscal Year: 2002..regulate mRNA stability (nuclear run-off assays) or transcription (transfection of promoter constructs) of adenosine A2A receptor mRNA. III. Adenosine-mediated mechanisms of methotrexate toxicity...
- Therapeutic Strategies for Neonatal Hypoxic-Ischemic EncephalopathyRaymond Koehler; Fiscal Year: 2009....
- Therapeutic Strategies for Neonatal Hypoxic-Ischemic EncephalopathyRAYMOND CHARLES KOEHLER; Fiscal Year: 2010....
- Compartmentation of Myocyte Adenosine Receptor SignalingRobert D Lasley; Fiscal Year: 2010..The results of these in-depth studies of GPCRs and their interactions on subcellular protein kinase signaling in normal and ischemic myocardium may facilitate the development of new therapies for the treatment of the ischemic heart. ..
- Preconditioning Improves Coronary PatencyKarin Przyklenk; Fiscal Year: 2010..e., identification of the mechanisms by which brief episodes of preconditioning ischemia and adenosine A2A receptor stimulation improve vessel patency - may, in future, be exploited in the design of novel anti-platelet ..
- Nitric Oxide and Compensatory Coronary VasodilationDavid Stepp; Fiscal Year: 2004..2) We hypothesize that adenosine A2a receptor mediated coronary vasodilation is augmented by chronic impairment of NO production...
- Sepsis syndrome and adenosine A2A receptor activationWILLIAM SCHELD; Fiscal Year: 2007..abstract_text> ..
- Preconditioning Improves Coronary PatencyKarin Przyklenk; Fiscal Year: 2009..e., identification of the mechanisms by which brief episodes of preconditioning ischemia and adenosine A2A receptor stimulation improve vessel patency - may, in future, be exploited in the design of novel anti-platelet ..
- PHARMACOLOGIC PROMOTION OF WOUND HEALINGBruce Cronstein; Fiscal Year: 2007We have previously demonstrated that topical application of adenosine A2A receptor agonists promotes more rapid wound healing both in diabetic and normal animals...
- Pathogenesis and Treatment of Alcohol-Induced CirrhosisBruce Cronstein; Fiscal Year: 2007..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
- Regulation of the Endothelial Cell GlycocalyxBrian Duling; Fiscal Year: 2007..1. Can the effects of ischemia/reperfusion on the glycocalyx be reduced by activation of the adenosine A2A receptor? 2. Can the effects of I/R be mimicked by activation of A3 receptors? 3...
- DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSESRichard Martin; Fiscal Year: 2006..abstract_text> ..
- DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSESRichard Martin; Fiscal Year: 2005..abstract_text> ..
- Astrocytes and neurovascular couplingDALE ALAN PELLIGRINO; Fiscal Year: 2010..The central hypothesis is that astrocytes and the glia limitans represent a vital signaling conduit in the pial arteriolar dilation arising from neural activation. ..
- Astrocytes and neurovascular couplingDale Pelligrino; Fiscal Year: 2009..The central hypothesis is that astrocytes and the glia limitans represent a vital signaling conduit in the pial arteriolar dilation arising from neural activation. ..
- Ethanol regulation of signaling: from cells to behaviorIvan Diamond; Fiscal Year: 2009..The experiments in this proposal will identify and validate novel targets for the development of new therapeutic agents to treat alcoholism and alcohol abuse. ..
- Tailoring Novel Therapeutics for Emerging Drug-Resistant C. Difficile ColitisRichard Guerrant; Fiscal Year: 2007..We propose to investigate three types of anti-inflammatory agents alone and in combination: adenosine A2A receptor agonists that block leukocyte activation; A2B antagonists that block cytokine production by epithelial and ..
- Adenosine 2A Receptor Agonist in Diabetic NephropathyKambiz Kalantarinia; Fiscal Year: 2007..This project combines the strengths of the University of Virginia as a leader in both the study of adenosine A2A receptor agonist and diabetes...
- Resident Leukocytes in Lung Ischemia-Reperfusion InjuryVICTOR LAUBACH; Fiscal Year: 2007..The proposed studies will directly address the causes IR injury with the hopes of initiating further studies focusing on therapeutic strategies aimed at preventing or ameliorating acute lung IR injury. ..
- Prostaglandins: Kinins and Angiotensin InteractionsJOHN MC GIFF; Fiscal Year: 2007..3) Heme oxygenase activity and suppression of EET and 20-HETE synthesis. 4) Activation of peroxisome-proliferator-activated receptor alpha by Fibrates with stimulation of EET synthesis. ..
- Lymphocyte Activation in Sickle Cell Lung DiseaseJoel M Linden; Fiscal Year: 2010..We propose to investigate how this cells produces lung injury, and the effects of inhibiting its function on lung injury. We also will study iNKT cells in the blood of SCD patients. ..
- Prostaglandins: Kinins and Angiotensin InteractionsJOHN MC GIFF; Fiscal Year: 2009..3) Heme oxygenase activity and suppression of EET and 20-HETE synthesis. 4) Activation of peroxisome-proliferator-activated receptor alpha by Fibrates with stimulation of EET synthesis. ..
- Mechanisms of Chronic Dysfunction after Brain TraumaC Dixon; Fiscal Year: 2007Numerous studies have demonstrated an antagonistic interaction between specific adenosine A2A receptor (A2AR) and dopamine (DA) D2 receptor (D2R) subtypes...