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 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
  2. ncbi 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
  3. ncbi 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
  4. 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
  5. ncbi 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
  6. ncbi 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
  7. 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
  8. ncbi 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
  9. 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
  10. ncbi 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

Research Grants

  1. The Pharmacology of Dermal Fibrosis
    Bruce Cronstein; Fiscal Year: 2009
  2. Adenosine, Toll-Like Receptors and Angiogenesis
    Samuel Joseph Leibovich; Fiscal Year: 2010
  3. Adenosine, Toll-Like Receptors and Angiogenesis
    SAMUEL LEIBOVICH; Fiscal Year: 2009
  4. The Pharmacology of Dermal Fibrosis
    Bruce Neil Cronstein; Fiscal Year: 2010
  5. PHARMACOLOGY OF ANTIRHEUMATIC AGENTS
    Bruce Cronstein; Fiscal Year: 2002
  6. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    Raymond Koehler; Fiscal Year: 2009
  7. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    RAYMOND CHARLES KOEHLER; Fiscal Year: 2010
  8. Preconditioning Improves Coronary Patency
    Karin Przyklenk; Fiscal Year: 2009
  9. Preconditioning Improves Coronary Patency
    Karin Przyklenk; Fiscal Year: 2010
  10. Compartmentation of Myocyte Adenosine Receptor Signaling
    Robert D Lasley; Fiscal Year: 2010

Detail Information

Publications283 found, 100 shown here

  1. 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...
  2. ncbi 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...
  3. ncbi 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
    ....
  4. 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...
  5. ncbi 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 ..
  6. ncbi 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 ..
  7. 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
    ....
  8. ncbi 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...
  9. 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
    ....
  10. ncbi 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...
  11. ncbi 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...
  12. 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...
  13. 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...
  14. ncbi 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...
  15. ncbi 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...
  16. 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
    ....
  17. 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)...
  18. ncbi 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...
  19. ncbi 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 ..
  20. 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 ..
  21. ncbi 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...
  22. 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 ..
  23. 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...
  24. 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...
  25. 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...
  26. ncbi 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...
  27. 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
    ....
  28. 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...
  29. 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
    ....
  30. 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...
  31. 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
    ....
  32. ncbi 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...
  33. 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...
  34. 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...
  35. 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 ..
  36. 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...
  37. 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...
  38. 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...
  39. ncbi 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...
  40. 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...
  41. 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
    ....
  42. ncbi 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...
  43. 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...
  44. 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...
  45. ncbi 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 ..
  46. ncbi 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
    ....
  47. 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...
  48. ncbi 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...
  49. ncbi 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...
  50. ncbi 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...
  51. ncbi 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
    ....
  52. 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...
  53. ncbi 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...
  54. ncbi Down-regulation of adenosine A2A receptors upon NGF-induced differentiation of PC12 cells
    G Arslan
    Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden
    Neuropharmacology 36:1319-26. 1997
    PC12 cell differentiation was induced by one week of nerve growth factor (NGF) treatment and adenosine A2A receptor expression and activity were analysed...
  55. 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...
  56. ncbi The novel adenosine A2a receptor antagonist ST1535 potentiates the effects of a threshold dose of L-DOPA in MPTP treated common marmosets
    Sarah Rose
    Neurodegenerative Disease Research Centre, School of Health and Biomedical Sciences, King's College, London SE1 1UL UK
    Eur J Pharmacol 546:82-7. 2006
    ..The data suggests that ST1535 will be an effective anti-parkinsonian agent in combination with L-DOPA and allow a reduction in l-DOPA usage in the treatment of Parkinson's disease...
  57. 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...
  58. 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 ..
  59. ncbi 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...
  60. ncbi Attenuation of reperfusion lung injury and apoptosis by A2A adenosine receptor activation is associated with modulation of Bcl-2 and Bax expression and activation of extracellular signal-regulated kinases
    Julia Rivo
    Department of Anesthesiology and Critical Care Medicine, Hadassah University Medical Center, The Hebrew University of Jerusalem, Jerusalem, Israel
    Shock 27:266-73. 2007
    ..This protection is associated with decreased apoptosis and involves ERK1/2 activation and alterations in antiapoptotic Bcl-2 and proapoptotic Bax proteins...
  61. 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...
  62. 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
    ....
  63. 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...
  64. ncbi Medicinal chemistry of adenosine A2A receptor agonists
    Gloria Cristalli
    Dipartimento di Scienze Chimiche, Universita di Camerino, Italy
    Curr Top Med Chem 3:387-401. 2003
    ..This review is aimed at presenting a complete overview of the medicinal chemistry development of A(2A) adenosine receptor agonists and at stressing the strong need for more selective ligands at A(2A) human subtype...
  65. 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 ..
  66. ncbi 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 ..
  67. 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...
  68. ncbi 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...
  69. 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...
  70. ncbi Adenosine A2A receptor facilitates calcium-dependent protein secretion through the activation of protein kinase A and phosphatidylinositol-3 kinase in PC12 cells
    Yasunori Mori
    Institute of Molecular and Cellular Biosciences, University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan
    Cell Struct Funct 29:101-10. 2004
    ....
  71. ncbi 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...
  72. 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...
  73. 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
    ....
  74. 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...
  75. ncbi 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
    ....
  76. ncbi Adenosine triggers preconditioning through MEK/ERK1/2 signalling pathway during hypoxia/reoxygenation in neonatal rat cardiomyocytes
    R Germack
    Biomedical Research Centre, School of Biomedical and Natural Sciences, Nottingham Trent University, UK
    J Mol Cell Cardiol 39:429-42. 2005
    ..In addition, A(3)AR-induced preconditioning also involves a PI-3K dependent pathway...
  77. ncbi Role of adenosine A2A receptor in the regulation of gastric somatostatin release
    Linda Yip
    Department of Physiology, University of British Columbia, Vancouver, Canada
    J Pharmacol Exp Ther 309:804-15. 2004
    ..The lowest level was detected in the mucosa. In conclusion, adenosine may act on A(2A) receptors to augment SLI release and consequently control gastric acid secretion...
  78. ncbi Determination of adenosine effects and adenosine receptors in murine corpus cavernosum
    Rita C Tostes
    Department of Pharmacology, Institute of Biomedical Sciences, University of Sao Paulo, Sao Paulo, Brazil
    J Pharmacol Exp Ther 322:678-85. 2007
    ..In addition, adenosine negatively modulates sympathetic neurotransmission, by A1 receptor subtype activation, in murine corpora cavernosa. Adenosine may subserve dual roles in modulating the physiological mechanisms of erection in mice...
  79. ncbi Activation of adenosine receptors in the posterior cingulate cortex impairs memory retrieval in the rat
    Grace Schenatto Pereira
    Instituto de Pesquisas Biomédicas, Pontificia Universidade Catolica do Rio Grande do Sul, Porto Alegre, RS
    Neurobiol Learn Mem 83:217-23. 2005
    ..These findings provide behavioral evidence for the role of adenosinergic system in the memory retrieval into PCC...
  80. ncbi Binding of the prototypical adenosine A(2A) receptor agonist CGS 21680 to the cerebral cortex of adenosine A(1) and A(2A) receptor knockout mice
    Luisa V Lopes
    Laboratory of Neurosciences, Faculty of Medicine, University of Lisbon, Portugal
    Br J Pharmacol 141:1006-14. 2004
    ..Thus, CGS 21680 should be used with care in all preparations where adenosine A(1) receptors out-number A(2A) receptors...
  81. ncbi 1,2,4-Triazolo[1,5-a]quinoxaline derivatives: synthesis and biological evaluation as adenosine receptor antagonists
    Daniela Catarzi
    Dipartimento di Scienze Farmaceutiche, Polo Scientifico, Universita degli Studi di Firenze, Via U Schiff, 6, Sesto Fiorentino FZ, 50019, Italy
    Farmaco 59:71-81. 2004
    ....
  82. ncbi Adenosine receptor-mediated modulation of dopamine release in the nucleus accumbens depends on glutamate neurotransmission and N-methyl-D-aspartate receptor stimulation
    Davide Quarta
    Preclinical Pharmacology Section, Behavioral Neuroscience Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, Department of Health and Human Services, Baltimore, Maryland 21224, USA
    J Neurochem 91:873-80. 2004
    ..Furthermore, these results underscore the role of A(1) vs. A(2A) receptor antagonism in the central effects of caffeine...
  83. ncbi Caffeine inhibition of rat carotid body chemoreceptors is mediated by A2A and A2B adenosine receptors
    S V Conde
    , , Facultad de Medicina, Valladolid, Spain
    J Neurochem 98:616-28. 2006
    ..It is concluded that endogenous adenosine, via presynaptic A2B and postsynaptic A2A receptors, can exert excitatory effects on the overall output of the rat CB chemoreceptors...
  84. ncbi Co-localization and functional interaction between adenosine A(2A) and metabotropic group 5 receptors in glutamatergic nerve terminals of the rat striatum
    Ricardo J Rodrigues
    Centre for Neuroscience of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
    J Neurochem 92:433-41. 2005
    ..This emphasizes the role of the modulation of glutamate release as a likely mechanism of action of these receptors both in striatal neuroprotection and in Parkinson's disease...
  85. ncbi Differential coronary microvascular exchange responses to adenosine: roles of receptor and microvessel subtypes
    JianJie Wang
    Department of Physiology and Pharmacology, School of Medicine, University of Missouri, Columbia, Missouri, USA
    Microcirculation 12:313-26. 2005
    ..To assess the role of adenosine receptors in the regulation of coronary microvascular permeability to porcine serum albumin (P(s)(PSA))...
  86. ncbi Adenosine A1 receptors modulate the anxiolytic-like effect of ethanol in the elevated plus-maze in mice
    Rui D S Prediger
    Departamento de Farmacologia, , Universidade Federal de Santa Catarina, UFSC, Rua Ferreira Lima 82, , SC 88015-420, Brazil
    Eur J Pharmacol 499:147-54. 2004
    ..6 g/kg). These results reinforce the involvement of adenosine in anxiety and suggest that the activation of adenosine A1 receptors, but not adenosine A(2A) receptors, mediate the anxiolytic-like effect induced by ethanol in mice...
  87. ncbi Adenosine A2A receptor modulation of juvenile female rat skeletal muscle microvessel permeability
    JianJie Wang
    Dept of Medical Pharmacology and Physiology, University of Missouri, Columbia, MO 65212, USA
    Am J Physiol Heart Circ Physiol 291:H3094-105. 2006
    ....
  88. ncbi Animal models for the study of adenosine receptor function
    R Yaar
    Department of Biochemistry, Whitaker Cardiovascular Institute, Boston University School of Medicine, Boston, Massachusetts, USA
    J Cell Physiol 202:9-20. 2005
    ..Furthermore, it illustrates the need for multiple adenosine receptor subtype deficiency studies in mice and the deletion of the A2b subtype...
  89. ncbi Upregulation of A2A adenosine receptor expression by TNF-alpha in PBMC of patients with CHF: a regulatory mechanism of inflammation
    Pier Leopoldo Capecchi
    Department of Clinical Medicine and Immunological Sciences, Section of Clinical Immunology, University of Siena, Siena, Italy
    J Card Fail 11:67-73. 2005
    ..The study is aimed at determining the role of the A(2A)R in the modulation of TNF-alpha production, and the ex vivo effect of TNF-alpha on A(2A)R in peripheral blood mononuclear cells (PBMC) from CHF patients...
  90. ncbi Adenosine is upregulated during peritonitis and is involved in downregulation of inflammation
    B Rogachev
    Department of Nephrology, Soroka Medical Center and Ben Gurion University of the Negev, Beer Sheva, Israel
    Kidney Int 70:675-81. 2006
    ..Future treatment with adenosine agonists should be considered for attenuating the damage to mesothelium during the course of acute peritonitis...
  91. ncbi Tonic adenosine A1 and A2A receptor activation is required for the excitatory action of VIP on synaptic transmission in the CA1 area of the hippocampus
    D Cunha-Reis
    Institute of Pharmacology and Neurosciences, Faculty of Medicine and Institute of Molecular Medicine, University of Lisbon, Av Prof Egas Moniz, 1649 028 Lisbon, Portugal
    Neuropharmacology 52:313-20. 2007
    ..This differential sensitivity to adenosine modulation might be due to the different VIP circuits contributing to VIP effects on pyramidal cell dendrites and pyramidal cell bodies...
  92. ncbi Modulation of short-term social memory in rats by adenosine A1 and A(2A) receptors
    Rui D S Prediger
    Departamento de Farmacologia, , Universidade Federal de Santa Catarina, UFSC, , SC 88049-900, Brazil
    Neurosci Lett 376:160-5. 2005
    ..These results indicate that adenosine modulates the short-term social memory in rats by acting on both A1 and A(2A) receptors, with adenosine receptor agonists and antagonists, respectively, disrupting and enhancing the social memory...
  93. ncbi Progress in the pursuit of therapeutic adenosine receptor antagonists
    Stefano Moro
    Molecular Modeling Section, Dipartimento di Scienze Farmaceutiche, Universita di Padova, Via Marzolo 5, I 35131 Padova, Italy
    Med Res Rev 26:131-59. 2006
    ..In this review, we will summarize the most relevant progress in developing new therapeutic adenosine receptor antagonists...
  94. ncbi Role of adenosine A1 receptors in the modulation of dopamine D1 and adenosine A2A receptor signaling in the neostriatum
    K Yabuuchi
    Oita University Faculty of Medicine, Yufu, Oita 879-5593, Japan
    Neuroscience 141:19-25. 2006
    ..In conclusion, A(1) receptors play a major modulatory role in dopamine and adenosine receptor signaling...
  95. ncbi 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors
    Zhan-Guo Gao
    Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
    Biochem Pharmacol 68:1985-93. 2004
    ..4 microM) and 2-[2-(2-thienyl)-ethyloxy]adenosine (EC(50) = 1.8 microM) were found to be relatively potent A(2B) agonists, although less potent than NECA (EC(50) = 140 nM)...
  96. ncbi Stimulation of adenosine A1 and A2A receptors by AMP in the submucosal plexus of guinea pig small intestine
    Na Gao
    Dept of Physiology and Cell Biology, Columbus, OH 43210 1218, USA
    Am J Physiol Gastrointest Liver Physiol 292:G492-500. 2007
    ....
  97. ncbi Adenosine administration produces an antidepressant-like effect in mice: evidence for the involvement of A1 and A2A receptors
    Manuella P Kaster
    , , Universidade Federal de Santa Catarina, , SC 88040-900, Brazil
    Neurosci Lett 355:21-4. 2004
    ..p.) and DPMA (1-5 mg/kg, i.p.) also produced an antidepressant-like effect in the FST. This is the first report of an antidepressant-like effect of adenosine in mice, apparently mediated through an interaction with A1 and A2A receptors...
  98. ncbi Potentiation of cytokine induction of group IIA phospholipase A(2) in rat mesangial cells by ATP and adenosine via the A2A adenosine receptor
    K Scholz-Pedretti
    Pharmazentrum Frankfurt, , Theodor-Stern-Kai-7, D-60590 Frankfurt am Main, Germany
    Br J Pharmacol 132:37-46. 2001
    ..7. These data indicate that ATP mediates proinflammatory long-term effects in rat mesangial cells via its degradation product adenosine through the A2A receptor resulting in potentiation of sPLA(2)-IIA induction...
  99. ncbi Adenosine A2A receptor-mediated facilitation of noradrenaline release involves protein kinase C activation and attenuation of presynaptic inhibitory receptor-mediated effects in the rat vas deferens
    Gloria Queiroz
    Laboratorio de Farmacologia, Faculdade de Farmacia, Universidade do Porto, Porto, Portugal
    J Neurochem 85:740-8. 2003
    ..The adenosine A2A receptor-mediated facilitation was not changed by inhibitors of protein kinase A, protein kinase G or calmodulin ..
  100. ncbi Adenosine promotes neuronal recovery from reactive oxygen species induced lesion in rat hippocampal slices
    Claudia G Almeida
    Laboratory of Neurosciences, Faculty of Medicine of Lisbon, Avenue Prof Egas Moniz, 1649 028 Lisbon, Portugal
    Neurosci Lett 339:127-30. 2003
    ..7+/-5.8% of control (n=5). The blockade of A(2A) receptors was devoid of effect (n=4). Adenosine is released by ROS-generating systems, and attenuates the deleterious cellular consequences of ROS through A(1) receptor activation...
  101. ncbi Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors
    Zhan-Guo Gao
    Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK/National Institutes of Health, Bldg. 8A, Rm. B1A-19, Bethesda, MD 20892-0810, USA
    Biochem Pharmacol 65:525-34. 2003
    ..Both binding and functional assays support the allosteric interactions of amiloride analogues with A(3) receptors...

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. 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...
  3. 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...
  4. 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 ..
  5. 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...
  6. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    Raymond Koehler; Fiscal Year: 2009
    ....
  7. Therapeutic Strategies for Neonatal Hypoxic-Ischemic Encephalopathy
    RAYMOND CHARLES KOEHLER; Fiscal Year: 2010
    ....
  8. 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 ..
  9. 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 ..
  10. 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. ..
  11. 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...
  12. Sepsis syndrome and adenosine A2A receptor activation
    WILLIAM SCHELD; Fiscal Year: 2007
    ..abstract_text> ..
  13. 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...
  14. 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...
  15. 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...
  16. DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSES
    Richard Martin; Fiscal Year: 2006
    ..abstract_text> ..
  17. DEVELOPMENTAL REGULATION OF HYPERCAPNIC RESPONSES
    Richard Martin; Fiscal Year: 2005
    ..abstract_text> ..
  18. 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. ..
  19. 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. ..
  20. 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. ..
  21. 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 ..
  22. 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...
  23. 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. ..
  24. 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. ..
  25. 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. ..
  26. 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. ..
  27. Mechanisms of Chronic Dysfunction after Brain Trauma
    C Dixon; Fiscal Year: 2007
    Numerous studies have demonstrated an antagonistic interaction between specific adenosine A2A receptor (A2AR) and dopamine (DA) D2 receptor (D2R) subtypes...