adenosine a2a receptor

Summary

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.

Top Publications

  1. ncbi Neuroprotection by adenosine A2A receptor blockade in experimental models of Parkinson's disease
    Ken Ikeda
    Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co, Ltd, Nagaizumi, Sunto, Shizuoka, Japan
    J Neurochem 80:262-70. 2002
  2. ncbi Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists
    Ming Yang
    Department of Pharmacology, CV Therapeutics, Inc, Palo Alto, CA 94304, USA
    Naunyn Schmiedebergs Arch Pharmacol 375:133-44. 2007
  3. ncbi A(2A) adenosine receptor deficiency attenuates brain injury induced by transient focal ischemia in mice
    J 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
  4. pmc Dopamine D2 receptor dysfunction is rescued by adenosine A2A receptor antagonism in a model of DYT1 dystonia
    Francesco Napolitano
    CEINGE Biotecnologie Avanzate, Naples, Italy
    Neurobiol Dis 38:434-45. 2010
  5. pmc Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death
    Leonóra Himer
    Department of Pharmacology, Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary
    FASEB J 24:2631-40. 2010
  6. ncbi Receptor heteromerization in adenosine A2A receptor signaling: relevance for striatal function and Parkinson's disease
    K Fuxe
    Department of Neuroscience, Karolinska Institute, Stockholm, Sweden
    Neurology 61:S19-23. 2003
  7. ncbi Adenosine A2A receptor blockade prevents synaptotoxicity and memory dysfunction caused by beta-amyloid peptides via p38 mitogen-activated protein kinase pathway
    Paula 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
  8. ncbi Receptors for purines and pyrimidines
    V Ralevic
    School of Biomedical Sciences, Queen s Medical Centre, University of Nottingham, Nottingham, England
    Pharmacol Rev 50:413-92. 1998
  9. pmc Local glutamate level dictates adenosine A2A receptor regulation of neuroinflammation and traumatic brain injury
    Shuang 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
  10. ncbi Adenosine A2A receptor activation reduces proinflammatory events and decreases cell death following intracerebral hemorrhage
    M Mayne
    Department of Pharmacology, University of Manitoba, Winnipeg, Canada
    Ann Neurol 49:727-35. 2001

Research Grants

  1. The Pharmacology of Dermal Fibrosis
    Bruce Cronstein; Fiscal Year: 2009
  2. Pharmacological strategies to improve breathing after cervical spinal cord injury
    FRANCIS GOLDER; Fiscal Year: 2009
  3. Adenosine, Toll-Like Receptors and Angiogenesis
    Samuel Joseph Leibovich; Fiscal Year: 2010
  4. Adenosine, Toll-Like Receptors and Angiogenesis
    SAMUEL LEIBOVICH; Fiscal Year: 2009
  5. Adenosine, Toll-Like Receptors and Angiogenesis
    SAMUEL LEIBOVICH; Fiscal Year: 2009
  6. The Pharmacology of Dermal Fibrosis
    Bruce Neil Cronstein; Fiscal Year: 2010
  7. Pharmacological strategies to improve breathing after cervical spinal cord injury
    FRANCIS GOLDER; Fiscal Year: 2009
  8. Dopamine D2 and Adenosine A2A roles:Tremulous Movements
    John Salamone; Fiscal Year: 2004
  9. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce Cronstein; Fiscal Year: 2001
  10. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce Cronstein; Fiscal Year: 1999

Detail Information

Publications312 found, 100 shown here

  1. ncbi Neuroprotection by adenosine A2A receptor blockade in experimental models of Parkinson's disease
    Ken 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 ..
  2. ncbi Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists
    Ming 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...
  3. ncbi A(2A) adenosine receptor deficiency attenuates brain injury induced by transient focal ischemia in mice
    J 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
    ....
  4. pmc Dopamine D2 receptor dysfunction is rescued by adenosine A2A receptor antagonism in a model of DYT1 dystonia
    Francesco Napolitano
    CEINGE Biotecnologie Avanzate, Naples, Italy
    Neurobiol Dis 38:434-45. 2010
    ....
  5. pmc Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death
    Leonóra 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...
  6. ncbi Receptor heteromerization in adenosine A2A receptor signaling: relevance for striatal function and Parkinson's disease
    K Fuxe
    Department of Neuroscience, Karolinska Institute, Stockholm, Sweden
    Neurology 61:S19-23. 2003
    ....
  7. ncbi Adenosine A2A receptor blockade prevents synaptotoxicity and memory dysfunction caused by beta-amyloid peptides via p38 mitogen-activated protein kinase pathway
    Paula 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
    ....
  8. ncbi Receptors for purines and pyrimidines
    V Ralevic
    School of Biomedical Sciences, Queen s Medical Centre, University of Nottingham, Nottingham, England
    Pharmacol Rev 50:413-92. 1998
  9. pmc Local glutamate level dictates adenosine A2A receptor regulation of neuroinflammation and traumatic brain injury
    Shuang 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...
  10. ncbi Adenosine A2A receptor activation reduces proinflammatory events and decreases cell death following intracerebral hemorrhage
    M 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...
  11. pmc Synergistic up-regulation of vascular endothelial growth factor expression in murine macrophages by adenosine A(2A) receptor agonists and endotoxin
    Samuel 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
    ....
  12. pmc Adenosine promotes wound healing and mediates angiogenesis in response to tissue injury via occupancy of A(2A) receptors
    M 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...
  13. doi 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...
  14. ncbi Adenosine A2A receptor stimulation potentiates nitric oxide release by activated microglia
    Josep Saura
    Department of Pharmacology and Toxicology, IIBB, CSIC, IDIBAPS, Barcelona, Spain
    J Neurochem 95:919-29. 2005
    ....
  15. pmc Adenosine A2A receptor activation limits graft-versus-host disease after allogenic hematopoietic stem cell transplantation
    Courtney 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...
  16. ncbi 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. 2002
    Animal studies of the topical application of adenosine A2A receptor agonists show that it promotes wound closure...
  17. pmc GPCR 3D homology models for ligand screening: lessons learned from blind predictions of adenosine A2a receptor complex
    VSEVOLOD 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 ..
  18. ncbi Adenosine A2A receptor antagonism increases nNOS-immunoreactive neurons in the striatum of Huntington transgenic mice
    S 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...
  19. pmc Adenosine A(2A) receptor activation promotes wound neovascularization by stimulating angiogenesis and vasculogenesis
    M 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
    ....
  20. pmc Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists
    VSEVOLOD 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...
  21. doi Adenosine A2A receptor antagonists exert motor and neuroprotective effects by distinct cellular mechanisms
    Liqun 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...
  22. pmc Adenosine A2A receptor activation reduces infarct size in the isolated, perfused mouse heart by inhibiting resident cardiac mast cell degranulation
    Tyler 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...
  23. pmc Enhanced neuronal damage by co-administration of quinolinic acid and free radicals, and protection by adenosine A2A receptor antagonists
    W 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...
  24. ncbi 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 path
    Jiantu Che
    Department of Medicine, New York University School of Medicine, 550 First Avenue, New York, NY 10016, USA
    Mol Pharmacol 72:1626-36. 2007
    Prior 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)...
  25. ncbi Myocardial infarct-sparing effect of adenosine A2A receptor activation is due to its action on CD4+ T lymphocytes
    Zequan Yang
    Department of Biomedical Engineering, University of Virginia Health System, Box 800759, Charlottesville, VA 22903, USA
    Circulation 114:2056-64. 2006
    We 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...
  26. doi A differential role for the adenosine A2A receptor in opiate reinforcement vs opiate-seeking behavior
    Robyn 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...
  27. ncbi Differential expression of adenosine receptors in human endothelial cells: role of A2B receptors in angiogenic factor regulation
    Igor 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...
  28. doi Adenosine A2A receptor blockade or deletion diminishes fibrocyte accumulation in the skin in a murine model of scleroderma, bleomycin-induced fibrosis
    Majid 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...
  29. ncbi Adenosine A2A receptor antagonism increases striatal glutamate outflow in dopamine-denervated rats
    Claudia 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...
  30. pmc Adenosine A2A receptor antagonists: blockade of adenosinergic effects and T regulatory cells
    M 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...
  31. ncbi Genes for prostaglandin d synthase and receptor as well as adenosine A2A receptor are involved in the homeostatic regulation of nrem sleep
    O Hayaishi
    Department of Molecular Behavioral Biology, Osaka Bioscience Institute, 6 2 4 Furuedai, Suita, Osaka 5650874, Japan
    Arch Ital Biol 142:533-9. 2004
    ....
  32. doi Adenosine A2A receptor deficiency exacerbates white matter lesions and cognitive deficits induced by chronic cerebral hypoperfusion in mice
    Wei Duan
    Department of Neurology, Xinqiao Hospital, Third Military Medical University, 2 V Xinqiao Street, Chongqing 400037, PR China
    J Neurol Sci 285:39-45. 2009
    b>Adenosine A2A receptor inactivation consistently protects against acute ischemic brain injury; however, the role of the A2A receptor in chronic cerebral ischemia is unknown...
  33. pmc Genetic deletion of the adenosine A2A receptor confers postnatal development of relative myopia in mice
    Xiangtian Zhou
    School of Optometry and Ophthalmology and Eye Hospital, Wenzhou Medical College, Wenzhou, China
    Invest Ophthalmol Vis Sci 51:4362-70. 2010
    To critically evaluate whether the adenosine A2A receptor (A2AR) plays a role in postnatal refractive development in mice.
  34. ncbi Adenosine A2A receptor stimulation increases angiogenesis by down-regulating production of the antiangiogenic matrix protein thrombospondin 1
    Avani Desai
    Department of Medicine, New York University School of Medicine, New York, New York 10016, USA
    Mol Pharmacol 67:1406-13. 2005
    Topical adenosine A2A receptor agonists promote wound healing by, among other effects, increasing microvessel formation...
  35. doi 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-outs
    Hai 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...
  36. ncbi Effect of the adenosine A2a receptor antagonist 3,7-dimethyl-propargylxanthine on anxiety-like and depression-like behavior and alcohol consumption in Wistar Rats
    Annika 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, ..
  37. doi Adenosine A2a receptor induced gliosis via Akt/NF-kappaB pathway in vitro
    Rong 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...
  38. doi Adenosine A2A receptor-selective stimulation reduces signaling pathways involved in the development of intestine ischemia and reperfusion injury
    Rosanna Di Paola
    IRCCS Centro Neurolesi Bonino Pulejo, School of Medicine, University of Messina, Messina, Italy
    Shock 33:541-51. 2010
    In 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 ..
  39. pmc Adenosine A2A receptor activation on CD4+ T lymphocytes and neutrophils attenuates lung ischemia-reperfusion injury
    Ashish 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...
  40. ncbi Protective effect of adenosine A2A receptor activation in small-for-size liver transplantation
    Li 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...
  41. ncbi Upregulation of striatal adenosine A2A receptor mRNA in 6-hydroxydopamine-lesioned rats intermittently treated with L-DOPA
    Masahiko Tomiyama
    Third Department of Medicine, Hirosaki University School of Medicine, Hirosaki 036 8216, Japan
    Synapse 52:218-22. 2004
    To 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 ..
  42. pmc Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis
    Gabriela 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...
  43. ncbi 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 receptor
    Lisa 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 ..
  44. doi Differential expression of adenosine A3 receptors controls adenosine A2A receptor-mediated inhibition of TLR responses in microglia
    Céline 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...
  45. ncbi Arachidonic acid activates phospholipase D in human neutrophils; essential role of endogenous leukotriene B4 and inhibition by adenosine A2A receptor engagement
    Sonya 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...
  46. pmc The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slices
    A 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...
  47. ncbi Modulation of orphan nuclear receptor NURR1 expression by methotrexate in human inflammatory joint disease involves adenosine A2A receptor-mediated responses
    Jennifer 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
    ....
  48. ncbi Adenosine A2A receptor antagonists improve deficits in initiation of movement and sensory motor integration in the unilateral 6-hydroxydopamine rat model of Parkinson's disease
    Annalisa Pinna
    Section of Cagliari, CNR Institute of Neuroscience, Cagliari, Italy
    Synapse 61:606-14. 2007
    ....
  49. ncbi Adenosine A2A receptor dysfunction correlates with age at onset anticipation in blood platelets of subjects with Huntington's disease
    V 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...
  50. pmc The adenosine A2A receptor agonist CGS 21680 fails to ameliorate the course of dextran sulphate-induced colitis in mice
    Z Selmeczy
    Department of Pharmacology, Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary
    Inflamm Res 56:204-9. 2007
    In 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.
  51. ncbi Adenosine A2A receptor activation: another potential therapy for trauma and hemorrhagic shock
    Rongqian Wu
    Crit Care Med 34:1273-5. 2006
  52. ncbi Monoamine oxidase B inhibition and neuroprotection: studies on selective adenosine A2A receptor antagonists
    Neal 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...
  53. ncbi Recent advances in the design and optimization of adenosine A2A receptor antagonists
    Chi B Vu
    Biogen Idec Inc, Department of Medicinal Chemistry, 14 Cambridge Center, Cambridge, MA 02142, USA
    Curr Opin Drug Discov Devel 8:458-68. 2005
    In recent years, the adenosine A2A receptor has gained interest as a potential therapeutic target for alleviating the symptoms of Parkinson's disease...
  54. ncbi Optimization of the human adenosine A2a receptor yields in Saccharomyces cerevisiae
    Alison 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...
  55. ncbi Adenosine A2A receptor activation decreases reperfusion injury associated with high-flow reperfusion
    Steven 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...
  56. ncbi Effect of the adenosine A2A receptor antagonist 8-(3-chlorostyryl)caffeine on L-DOPA biotransformation in rat striatum
    Krystyna Gołembiowska
    Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31 343 Krakow, Poland
    Brain Res 998:208-17. 2004
    In 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...
  57. ncbi Adenosine A2a receptor-mediated, normoxic induction of HIF-1 through PKC and PI-3K-dependent pathways in macrophages
    Cristina De Ponti
    Istituto di Patologia Generale, Universita di Milano, Italy
    J Leukoc Biol 82:392-402. 2007
    ....
  58. ncbi Inactivation of adenosine A2A receptor impairs long term potentiation in the accumbens nucleus without altering basal synaptic transmission
    P d'Alcantara
    Laboratory of Neurophysiology, Department of Neuroscience, Universite Libre de Bruxelles, Brussels, Begium
    Neuroscience 107:455-64. 2001
    ....
  59. pmc Adenosine A2A receptor signaling and golf assembly show a specific requirement for the gamma7 subtype in the striatum
    William 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...
  60. doi DNA methylation and Yin Yang-1 repress adenosine A2A receptor levels in human brain
    Sandra 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
    ....
  61. ncbi Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in rats
    Elisabetta Tronci
    Department of Toxicology, University of Cagliari, Italy
    Eur J Pharmacol 566:94-102. 2007
    Antagonism of adenosine A2A receptor function has been proposed as an effective therapy in the treatment of Parkinson's disease...
  62. ncbi Behavioral and electrophysiological effects of the adenosine A2A receptor antagonist SCH 58261 in R6/2 Huntington's disease mice
    M R Domenici
    Department of Drug Research and Evaluation, Istituto Superiore di Sanita, Viale Regina Elena, 299, 00161, Rome, Italy
    Neurobiol Dis 28:197-205. 2007
    The 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 ..
  63. ncbi Adenosine A2A receptor antagonists as novel anti-Parkinsonian agents: a review of structure-activity relationships
    F Azam
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Seventh of October University, Misurata, Libya
    Pharmazie 64:771-95. 2009
    The adenosine A2A receptor (AA2AR) has emerged as an attractive target for the treatment of Parkinson's disease...
  64. ncbi Adenosine A2A receptor stimulation decreases GAT-1-mediated GABA uptake in the globus pallidus of the rat
    Brenda 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...
  65. doi Blocking adenosine A2A receptor reduces peritoneal fibrosis in two independent experimental models
    Sigal 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...
  66. doi The selective adenosine A2A receptor agonist CGS 21680 reduces JNK MAPK activation in oligodendrocytes in injured spinal cord
    Tiziana 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 ..
  67. ncbi New aspects of physiological and pathophysiological functions of adenosine A2A receptor in basal ganglia
    H 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...
  68. doi Selective adenosine A2a receptor antagonism reduces JNK activation in oligodendrocytes after cerebral ischaemia
    Alessia Melani
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini, 6, Florence, Italy
    Brain 132:1480-95. 2009
    ....
  69. ncbi Theophylline induces neutrophil apoptosis through adenosine A2A receptor antagonism
    K 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...
  70. ncbi Adenosine A2A receptor-mediated cell death of mouse thymocytes involves adenylate cyclase and Bim and is negatively regulated by Nur77
    Ildiko 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...
  71. ncbi PAP 9704, a Korean herbal medicine attenuates methamphetamine-induced hyperlocomotion via adenosine A2A receptor stimulation in mice
    Yong 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...
  72. ncbi Rapid modification of the glycocalyx caused by ischemia-reperfusion is inhibited by adenosine A2A receptor activation
    Steven 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...
  73. ncbi Adenosine A2A receptor occupancy stimulates expression of proteins involved in reverse cholesterol transport and inhibits foam cell formation in macrophages
    Allison 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...
  74. pmc Suppression of inflammation by low-dose methotrexate is mediated by adenosine A2A receptor but not A3 receptor activation in thioglycollate-induced peritonitis
    M 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...
  75. ncbi Spinal adenosine A2a receptor activation elicits long-lasting phrenic motor facilitation
    Francis J Golder
    Department of Comparative Biosciences, University of Wisconsin, Madison, Wisconsin 53706, USA
    J Neurosci 28:2033-42. 2008
    ....
  76. ncbi Genetic and pharmacological inactivation of the adenosine A2A receptor attenuates 3-nitropropionic acid-induced striatal damage
    J Stephen Fink
    Department of Neurology, Boston University School of Medicine, MA 02118, USA
    J Neurochem 88:538-44. 2004
    b>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...
  77. pmc 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 promoter
    Madhuri 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. 2007
    Macrophages 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...
  78. pmc Adenosine A2A receptor activation reduces hepatic ischemia reperfusion injury by inhibiting CD1d-dependent NKT cell activation
    Courtney 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...
  79. ncbi Cellular and behavioural effects of the adenosine A2a receptor antagonist KW-6002 in a rat model of l-DOPA-induced dyskinesia
    M 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 ..
  80. pmc Triggering neurotrophic factor actions through adenosine A2A receptor activation: implications for neuroprotection
    Ana 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 ..
  81. ncbi Adenosine inhibits IL-12 and TNF-[alpha] production via adenosine A2a receptor-dependent and independent mechanisms
    G 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...
  82. pmc Adenosine closes the K+ channel KCa3.1 in human lung mast cells and inhibits their migration via the adenosine A2A receptor
    S 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 ..
  83. pmc Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor
    Francesca 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...
  84. pmc Effects of adenosine A2A receptor stimulation on cocaine-seeking behavior in rats
    Ryan 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...
  85. ncbi Adenosine A2A receptor blockade differentially influences excitotoxic mechanisms at pre- and postsynaptic sites in the rat striatum
    Maria 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...
  86. ncbi Cross-regulation of carbon monoxide and the adenosine A2a receptor in macrophages
    Arvand 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...
  87. ncbi The protective effect of adenosine A2A receptor antagonism in cerebral ischemia
    F 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...
  88. ncbi Infarct-sparing effect of A2A-adenosine receptor activation is due primarily to its action on lymphocytes
    Zequan 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...
  89. ncbi Effects of CGS 21680, a selective adenosine A2A receptor agonist, on allergic airways inflammation in the rat
    John 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 ..
  90. ncbi Adenosine A2A receptor antagonists and Parkinson's disease: state of the art and future directions
    N 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
    ....
  91. pmc Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice
    M 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 ..
  92. pmc Cyclic AMP-dependent inhibition of human neutrophil oxidative activity by substituted 2-propynylcyclohexyl adenosine A(2A) receptor agonists
    G 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...
  93. ncbi Design, synthesis, and evaluation of novel A2A adenosine receptor agonists
    J 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...
  94. ncbi Effects of an adenosine A2A receptor blockade in the nucleus accumbens on locomotion, feeding, and prepulse inhibition in rats
    Jens 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...
  95. doi Additive protection against lung ischemia-reperfusion injury by adenosine A2A receptor activation before procurement and during reperfusion
    Leo M Gazoni
    Department of Surgery, University of Virginia, Charlottesville 22908, USA
    J Thorac Cardiovasc Surg 135:156-65. 2008
    b>Adenosine A2A receptor activation during reperfusion improves lung ischemia-reperfusion injury...
  96. ncbi Association studies of the adenosine A2a receptor (1976T > C) genetic polymorphism in Parkinson's disease and schizophrenia
    C 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 ..
  97. doi Caffeine and a selective adenosine A2A receptor antagonist induce reward and sensitization behavior associated with increased phospho-Thr75-DARPP-32 in mice
    Chih W Hsu
    Department of Emergency Medicine, Tzu Chi General Hospital, Hualien 970, Taiwan
    Psychopharmacology (Berl) 204:313-25. 2009
    ....
  98. ncbi Caffeine attenuates the duration of coronary vasodilation and changes in hemodynamics induced by regadenoson (CVT-3146), a novel adenosine A2A receptor agonist
    Gong 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...
  99. ncbi Reduction of infarct size and postischemic inflammation from ATL-146e, a highly selective adenosine A2A receptor agonist, in reperfused canine myocardium
    David 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...
  100. ncbi Up-regulation of A(2A) adenosine receptors by proinflammatory cytokines in rat PC12 cells
    Maria 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...
  101. ncbi Enhanced adenosine A2A receptor facilitation of synaptic transmission in the hippocampus of aged rats
    Nelson Rebola
    Center for Neurosciences of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, Portugal
    J Neurophysiol 90:1295-303. 2003
    ....

Research Grants87

  1. The Pharmacology of Dermal Fibrosis
    Bruce 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 ..
  2. Pharmacological strategies to improve breathing after cervical spinal cord injury
    FRANCIS GOLDER; Fiscal Year: 2009
    ..Our approach uses small, highly permeable molecules (adenosine A2a receptor agonists) that mimic the effects of brain- derived neurotrophic factor (BDNF) on phrenic motoneuron ..
  3. Adenosine, Toll-Like Receptors and Angiogenesis
    Samuel 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...
  4. Adenosine, Toll-Like Receptors and Angiogenesis
    SAMUEL 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...
  5. Adenosine, Toll-Like Receptors and Angiogenesis
    SAMUEL 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...
  6. The Pharmacology of Dermal Fibrosis
    Bruce 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 ..
  7. Pharmacological strategies to improve breathing after cervical spinal cord injury
    FRANCIS GOLDER; Fiscal Year: 2009
    ..Our approach uses small, highly permeable molecules (adenosine A2a receptor agonists) that mimic the effects of brain- derived neurotrophic factor (BDNF) on phrenic motoneuron ..
  8. Dopamine D2 and Adenosine A2A roles:Tremulous Movements
    John Salamone; Fiscal Year: 2004
    ..abstract_text> ..
  9. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce Cronstein; Fiscal Year: 2001
    ..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...
  10. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce Cronstein; Fiscal Year: 1999
    ..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...
  11. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce 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...
  12. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce Cronstein; Fiscal Year: 2000
    ..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...
  13. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    Raymond Koehler; Fiscal Year: 2009
    ....
  14. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    RAYMOND CHARLES KOEHLER; Fiscal Year: 2010
    ....
  15. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    Raymond Koehler; Fiscal Year: 2009
    ....
  16. Compartmentation of Myocyte Adenosine Receptor Signaling
    Robert 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. ..
  17. Compartmentation of Myocyte Adenosine Receptor Signaling
    ROBERT LASLEY; Fiscal Year: 2009
    ..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. ..
  18. Preconditioning Improves Coronary Patency
    Karin 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 ..
  19. Nitric Oxide and Compensatory Coronary Vasodilation
    David Stepp; Fiscal Year: 2002
    ..2) We hypothesize that adenosine A2a receptor mediated coronary vasodilation is augmented by chronic impairment of NO production...
  20. Nitric Oxide and Compensatory Coronary Vasodilation
    David Stepp; Fiscal Year: 2004
    ..2) We hypothesize that adenosine A2a receptor mediated coronary vasodilation is augmented by chronic impairment of NO production...
  21. Nitric Oxide and Compensatory Coronary Vasodilation
    David Stepp; Fiscal Year: 2001
    ..2) We hypothesize that adenosine A2a receptor mediated coronary vasodilation is augmented by chronic impairment of NO production...
  22. Nitric Oxide and Compensatory Coronary Vasodilation
    David Stepp; Fiscal Year: 2003
    ..2) We hypothesize that adenosine A2a receptor mediated coronary vasodilation is augmented by chronic impairment of NO production...
  23. Nitric Oxide and Compensatory Coronary Vasodilation
    David Stepp; Fiscal Year: 2001
    ..2) We hypothesize that adenosine A2a receptor mediated coronary vasodilation is augmented by chronic impairment of NO production...
  24. DEVELOPING METHODS FOR CRYSTALLIZING FAMILY C GPCRS
    Dan Feng; Fiscal Year: 2010
    ..This technology has been applied to the high-resolution structures of two Family A GPCRs (the 22AR and Adenosine A2a receptor), opening new opportunities for structure-based design of drugs...
  25. Sepsis syndrome and adenosine A2A receptor activation
    WILLIAM SCHELD; Fiscal Year: 2007
    ..abstract_text> ..
  26. Preconditioning Improves Coronary Patency
    Karin 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 ..
  27. PHARMACOLOGIC PROMOTION OF WOUND HEALING
    Bruce Cronstein; Fiscal Year: 2004
    We have previously demonstrated that topical application of adenosine A2A receptor agonists promotes more rapid wound healing both in diabetic and normal animals...
  28. PHARMACOLOGIC PROMOTION OF WOUND HEALING
    Bruce Cronstein; Fiscal Year: 2006
    We have previously demonstrated that topical application of adenosine A2A receptor agonists promotes more rapid wound healing both in diabetic and normal animals...
  29. PHARMACOLOGIC PROMOTION OF WOUND HEALING
    Bruce Cronstein; Fiscal Year: 2005
    We have previously demonstrated that topical application of adenosine A2A receptor agonists promotes more rapid wound healing both in diabetic and normal animals...
  30. PHARMACOLOGIC PROMOTION OF WOUND HEALING
    Bruce Cronstein; Fiscal Year: 2007
    We have previously demonstrated that topical application of adenosine A2A receptor agonists promotes more rapid wound healing both in diabetic and normal animals...
  31. Pathogenesis and Treatment of Alcohol-Induced Cirrhosis
    Bruce Cronstein; Fiscal Year: 2006
    ..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
  32. Pathogenesis and Treatment of Alcohol-Induced Cirrhosis
    Bruce Cronstein; Fiscal Year: 2007
    ..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
  33. Pathogenesis and Treatment of Alcohol-Induced Cirrhosis
    Bruce Cronstein; Fiscal Year: 2005
    ..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
  34. Pathogenesis and Treatment of Alcohol-Induced Cirrhosis
    Bruce Cronstein; Fiscal Year: 2004
    ..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
  35. Pathogenesis and Treatment of Alcohol-Induced Cirrhosis
    Bruce Cronstein; Fiscal Year: 2003
    ..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
  36. Pathogenesis and Treatment of Alcohol-Induced Cirrhosis
    Bruce Cronstein; Fiscal Year: 2004
    ..This adenosine-stimulated collagen production by HSC is blocked by an adenosine A2A receptor antagonist...
  37. Regulation of the Endothelial Cell Glycocalyx
    Brian Duling; Fiscal Year: 2004
    ..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...
  38. Regulation of the Endothelial Cell Glycocalyx
    Brian Duling; Fiscal Year: 2006
    ..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...
  39. Regulation of the Endothelial Cell Glycocalyx
    Brian Duling; Fiscal Year: 2005
    ..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...
  40. Regulation of the Endothelial Cell Glycocalyx
    Brian 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...
  41. DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSES
    Richard Martin; Fiscal Year: 2003
    ..abstract_text> ..
  42. DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSES
    Richard Martin; Fiscal Year: 2004
    ..abstract_text> ..
  43. DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSES
    Richard Martin; Fiscal Year: 2006
    ..abstract_text> ..
  44. DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSES
    Richard Martin; Fiscal Year: 2005
    ..abstract_text> ..
  45. Astrocytes and neurovascular coupling
    DALE 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. ..
  46. Astrocytes and neurovascular coupling
    Dale 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. ..
  47. ADENOSINE A1 AND A2 RECEPTORS IN THE MYOCARDIUM
    James Dobson; Fiscal Year: 2002
    ..Recently we reported that adenosine A2a receptor stimulation also limits the antiadrenergic actions of adenosine...
  48. ADENOSINE A1 AND A2 RECEPTORS IN THE MYOCARDIUM
    James Dobson; Fiscal Year: 2001
    ..Recently we reported that adenosine A2a receptor stimulation also limits the antiadrenergic actions of adenosine...
  49. ADENOSINE A1 AND A2 RECEPTORS IN THE MYOCARDIUM
    James Dobson; Fiscal Year: 2003
    ..Recently we reported that adenosine A2a receptor stimulation also limits the antiadrenergic actions of adenosine...
  50. Purinergic Modulation of Dermal Fibrosis
    Edwin Sl Chan; Fiscal Year: 2010
    Dermal fibrosis is a hallmark of systemic sclerosis. We have previously demonstrated that stimulation of adenosine A2A receptor promotes collagen production in vitro while blockade of the adenosine A2A receptor attenuates development of ..
  51. Purinergic Modulation of Dermal Fibrosis
    Edwin Chan; Fiscal Year: 2009
    Dermal fibrosis is a hallmark of systemic sclerosis. We have previously demonstrated that stimulation of adenosine A2A receptor promotes collagen production in vitro while blockade of the adenosine A2A receptor attenuates development of ..
  52. Ethanol regulation of signaling: from cells to behavior
    Ivan 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. ..
  53. A2AR/mGluR5 Antagonist Combination Antiparkinsonian Therapy in MPTP Monkeys
    James Bogenpohl; Fiscal Year: 2009
    ..Another potential non-dopaminergic anti-PD drug target is the adenosine A2A receptor (A2AR). A2AR is expressed almost exclusively in striatal medium spiny neurons of the indirect pathway...
  54. Ethanol regulation of signaling: from cells to behavior
    Ivan Diamond; Fiscal Year: 2007
    ..The experiments in this proposal will identify and validate novel targets for the development of new therapeutic agents to treat alcoholism and alcohol abuse. ..
  55. Ethanol regulation of signaling: from cells to behavior
    Ivan Diamond; Fiscal Year: 2005
    ..The experiments in this proposal will identify and validate novel targets for the development of new therapeutic agents to treat alcoholism and alcohol abuse. ..
  56. Tailoring Novel Therapeutics for Emerging Drug-Resistant C. Difficile Colitis
    Richard L Guerrant; Fiscal Year: 2010
    ..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 ..
  57. Tailoring Novel Therapeutics for Emerging Drug-Resistant C. Difficile Colitis
    Richard 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 ..
  58. A2AR/mGluR5 Antagonist Combination Antiparkinsonian Therapy in MPTP Monkeys
    James Bogenpohl; Fiscal Year: 2010
    ..Another potential non-dopaminergic anti-PD drug target is the adenosine A2A receptor (A2AR). A2AR is expressed almost exclusively in striatal medium spiny neurons of the indirect pathway...
  59. Ethanol regulation of signaling: from cells to behavior
    Ivan Diamond; Fiscal Year: 2006
    ..The experiments in this proposal will identify and validate novel targets for the development of new therapeutic agents to treat alcoholism and alcohol abuse. ..
  60. Tailoring Novel Therapeutics for Emerging Drug-Resistant C. Difficile Colitis
    Richard Guerrant; Fiscal Year: 2009
    ..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 ..
  61. GPCR Network
    Raymond C Stevens; Fiscal Year: 2010
    ..Structural studies are necessary to understand the exquisite molecular recognition and signal transduction properties of this important protein family for both basic and applied biomedical research. ..
  62. Adenosine 2A Receptor Agonist in Diabetic Nephropathy
    Kambiz Kalantarinia; Fiscal Year: 2010
    ..This project combines the strengths of the University of Virginia as a leader in both the study of adenosine A2A receptor agonist and diabetes...
  63. Adenosine 2A Receptor Agonist in Diabetic Nephropathy
    Kambiz Kalantarinia; Fiscal Year: 2010
    ..This project combines the strengths of the University of Virginia as a leader in both the study of adenosine A2A receptor agonist and diabetes...
  64. Adenosine 2A Receptor Agonist in Diabetic Nephropathy
    Kambiz Kalantarinia; Fiscal Year: 2009
    ..This project combines the strengths of the University of Virginia as a leader in both the study of adenosine A2A receptor agonist and diabetes...
  65. IMPROVED VASODILATORS FOR PHARMACOLOGICAL STRESS IMAGING
    George Beller; Fiscal Year: 2000
    ..The desired coronary vasodilatation is mediated by the stimulation of the adenosine A2A receptor by adenosine, most of the side effects are caused by stimulation of the other 3 adenosine receptor ..
  66. Adenosine 2A Receptor Agonist in Diabetic Nephropathy
    Kambiz 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...
  67. Resident Leukocytes in Lung Ischemia-Reperfusion Injury
    VICTOR LAUBACH; Fiscal Year: 2006
    ..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. ..
  68. Resident Leukocytes in Lung Ischemia-Reperfusion Injury
    VICTOR LAUBACH; Fiscal Year: 2005
    ..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. ..
  69. Resident Leukocytes in Lung Ischemia-Reperfusion Injury
    VICTOR 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. ..
  70. Neutrophil Trafficking to Normal and Inflamed Lung
    Brian Duling; Fiscal Year: 2005
    ..abstract_text> ..
  71. Neutrophil Trafficking to Normal and Inflamed Lung
    Brian Duling; Fiscal Year: 2004
    ..abstract_text> ..
  72. Dopamine D2 receptor overexpression, adenosine A2A receptors, and motivation
    RYAN DAVID WARD; Fiscal Year: 2010
    ..preliminary assessment of brain changes that result from striatal D2 overexpression indicate that the adenosine A2A receptor is significantly downregulated in the D2OE mice...
  73. Neutrophil Trafficking to Normal and Inflamed Lung
    Brian Duling; Fiscal Year: 2006
    ..abstract_text> ..
  74. Neutrophil Trafficking to Normal and Inflamed Lung
    Brian Duling; Fiscal Year: 2007
    ..abstract_text> ..
  75. CTRIP: Treatment of Sickle Cell Crisis with inhibitors of NKT cell activation
    DAVID G contact NATHAN; Fiscal Year: 2010
    ..It causes short life span, pain and multi-organ failure. We have discovered a new anti-inflammatory approach to effectively treat SCD in mice and we plan to evaluate this new therapy in patients with SCD. ..
  76. ADENOSINE /DOPAMINE INTERACTIONS IN A2A RECEPTOR KO MICE
    Jiang Fan Chen; Fiscal Year: 1999
    DESCRIPTION (from applicant's abstract): The adenosine A2a receptor (A2aR) is co-expressed with the dopamine D2 receptor (D2R) in striatopallidal neurons and exerts an antagonistic influence on postsynaptic D2R function in brain...
  77. ADENOSINE /DOPAMINE INTERACTIONS IN A2A RECEPTOR KO MICE
    Jiang Fan Chen; Fiscal Year: 2000
    DESCRIPTION (from applicant's abstract): The adenosine A2a receptor (A2aR) is co-expressed with the dopamine D2 receptor (D2R) in striatopallidal neurons and exerts an antagonistic influence on postsynaptic D2R function in brain...
  78. Prostaglandins: Kinins and Angiotensin Interactions
    JOHN MC GIFF; Fiscal Year: 2005
    ..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. ..
  79. Prostaglandins: Kinins and Angiotensin Interactions
    JOHN MC GIFF; Fiscal Year: 2006
    ..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. ..
  80. CTRIP: Treatment of Sickle Cell Crisis with inhibitors of NKT cell activation
    David Nathan; Fiscal Year: 2009
    ..It causes short life span, pain and multi-organ failure. We have discovered a new anti-inflammatory approach to effectively treat SCD in mice and we plan to evaluate this new therapy in patients with SCD. ..
  81. Prostaglandins: Kinins and Angiotensin Interactions
    JOHN 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. ..
  82. Lymphocyte Activation in Sickle Cell Lung Disease
    Joel 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. ..
  83. Prostaglandins: Kinins and Angiotensin Interactions
    JOHN 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. ..
  84. Regulatory T Cells as a Novel Therapeutic Agent/Target for Acute Kidney Injury
    Gilbert R Kinsey; Fiscal Year: 2010
    ..expert in immune mechanisms of kidney injury and the anti-inflammatory properties and potential of adenosine A2A receptor agonists in kidney disease...
  85. Mechanisms of Chronic Dysfunction after Brain Trauma
    C Dixon; Fiscal Year: 2006
    ..provided by applicant): Numerous studies have demonstrated an antagonistic interaction between specific adenosine A2A receptor (A2AR) and dopamine (DA) D2 receptor (D2R) subtypes...
  86. Mechanisms of Chronic Dysfunction after Brain Trauma
    C Dixon; Fiscal Year: 2007
    ..provided by applicant): Numerous studies have demonstrated an antagonistic interaction between specific adenosine A2A receptor (A2AR) and dopamine (DA) D2 receptor (D2R) subtypes...
  87. Adenosine 2A Receptor Signaling in Lung Transplant Injury and Rejection
    Christine Lau; Fiscal Year: 2009
    ..Agonists of the anti-inflammatory Gs-coupled adenosine A2A receptor (A2AR) have been shown to inhibit the activity of most inflammatory cells, and extensive preclinical ..