adenosine a1 receptor

Summary

Summary: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.

Top Publications

  1. ncbi Sleep and its homeostatic regulation in mice lacking the adenosine A1 receptor
    Dag Stenberg
    Institute of Biomedicine Physiology, University of Helsinki, Helsinki, Finland
    J Sleep Res 12:283-90. 2003
  2. pmc Adenosine A1 receptor activation as a brake on the microglial response after experimental traumatic brain injury in mice
    M Lee Haselkorn
    Safar Center for Resuscitation Research, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania 15260, USA
    J Neurotrauma 27:901-10. 2010
  3. pmc Prostatic acid phosphatase is an ectonucleotidase and suppresses pain by generating adenosine
    Mark J Zylka
    Department of Cell and Molecular Physiology, UNC Neuroscience Center, University of North Carolina, CB 7545, Chapel Hill, NC 27599, USA
    Neuron 60:111-22. 2008
  4. pmc Autophagy is required for preconditioning by the adenosine A1 receptor-selective agonist CCPA
    Smadar Yitzhaki
    BioScience Center, San Diego State University, San Diego, CA 92182 4650, USA
    Basic Res Cardiol 104:157-67. 2009
  5. ncbi G16-mediated activation of nuclear factor kappaB by the adenosine A1 receptor involves c-Src, protein kinase C, and ERK signaling
    Andrew M F Liu
    Department of Biochemistry, Molecular Neuroscience Center, and Biotechnology Research Institute, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China
    J Biol Chem 279:53196-204. 2004
  6. ncbi Up-regulation of adenosine A1 receptor binding in pentylenetetrazol kindling in mice: effects of angiotensin IV
    Jana Tchekalarova
    Laboratory of Experimental Psychopharmacology, Institute of Physiology, Acad G Bonchev Str, bl 23, Bulgarian Academy of Sciences, Sofia 1113, Bulgaria
    Brain Res 1032:94-103. 2005
  7. ncbi 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists
    Lisa C W Chang
    Division of Medicinal Chemistry, Leiden Amsterdam Center for Drug Research, P O Box 9502, 2300 RA Leiden, The Netherlands
    J Med Chem 47:6529-40. 2004
  8. ncbi Modification of adenosine A1 and A2A receptor density in the hippocampus of streptozotocin-induced diabetic rats
    Joao M N Duarte
    Center for Neuroscience of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
    Neurochem Int 48:144-50. 2006
  9. ncbi Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones
    Stefanie Weyler
    University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, Kreuzbergweg 26, 53115 Bonn, Germany
    ChemMedChem 1:891-902. 2006
  10. ncbi Activation of the adenosine A1 receptor inhibits HIV-1 tat-induced apoptosis by reducing nuclear factor-kappaB activation and inducible nitric-oxide synthase
    Sandeep C Pingle
    Department of Pharmacology, Southern Illinois University School of Medicine, PO Box 19629, Springfield, IL 62794 9629, USA
    Mol Pharmacol 72:856-67. 2007

Research Grants

Detail Information

Publications227 found, 100 shown here

  1. ncbi Sleep and its homeostatic regulation in mice lacking the adenosine A1 receptor
    Dag Stenberg
    Institute of Biomedicine Physiology, University of Helsinki, Helsinki, Finland
    J Sleep Res 12:283-90. 2003
    ..We conclude that constitutional lack of adenosine A1R does not prevent the homeostatic regulation of sleep...
  2. pmc Adenosine A1 receptor activation as a brake on the microglial response after experimental traumatic brain injury in mice
    M Lee Haselkorn
    Safar Center for Resuscitation Research, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania 15260, USA
    J Neurotrauma 27:901-10. 2010
    ..A(1)AR activation is an endogenous inhibitor of the microglial response to TBI, likely via inhibition of proliferation, and this may represent a therapeutic avenue to modulate microglia after TBI...
  3. pmc Prostatic acid phosphatase is an ectonucleotidase and suppresses pain by generating adenosine
    Mark J Zylka
    Department of Cell and Molecular Physiology, UNC Neuroscience Center, University of North Carolina, CB 7545, Chapel Hill, NC 27599, USA
    Neuron 60:111-22. 2008
    ..Our studies reveal molecular and physiological functions for PAP in purine nucleotide metabolism and nociception and suggest a novel use for PAP in the treatment of chronic pain...
  4. pmc Autophagy is required for preconditioning by the adenosine A1 receptor-selective agonist CCPA
    Smadar Yitzhaki
    BioScience Center, San Diego State University, San Diego, CA 92182 4650, USA
    Basic Res Cardiol 104:157-67. 2009
    ..Taken together, these results indicate that autophagy plays an important role in mediating the cardioprotective effects conferred by adenosine pretreatment...
  5. ncbi G16-mediated activation of nuclear factor kappaB by the adenosine A1 receptor involves c-Src, protein kinase C, and ERK signaling
    Andrew M F Liu
    Department of Biochemistry, Molecular Neuroscience Center, and Biotechnology Research Institute, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China
    J Biol Chem 279:53196-204. 2004
    The G(i)-linked adenosine A1 receptor has been shown to mediate anti-inflammatory actions, possibly via modulation of the transcription factor nuclear factor-kappaB (NFkappaB)...
  6. ncbi Up-regulation of adenosine A1 receptor binding in pentylenetetrazol kindling in mice: effects of angiotensin IV
    Jana Tchekalarova
    Laboratory of Experimental Psychopharmacology, Institute of Physiology, Acad G Bonchev Str, bl 23, Bulgarian Academy of Sciences, Sofia 1113, Bulgaria
    Brain Res 1032:94-103. 2005
    ..The antiepileptogenic effect of ANG IV could be realized partly through an adenosine-dependent mechanism...
  7. ncbi 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists
    Lisa C W Chang
    Division of Medicinal Chemistry, Leiden Amsterdam Center for Drug Research, P O Box 9502, 2300 RA Leiden, The Netherlands
    J Med Chem 47:6529-40. 2004
    ..Taking into account molecular modeling results from a series of potent adenosine A1 receptor antagonists, a pharmacophore was derived from which we show that a monocyclic core can be equally ..
  8. ncbi Modification of adenosine A1 and A2A receptor density in the hippocampus of streptozotocin-induced diabetic rats
    Joao M N Duarte
    Center for Neuroscience of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
    Neurochem Int 48:144-50. 2006
    ....
  9. ncbi Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones
    Stefanie Weyler
    University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, Kreuzbergweg 26, 53115 Bonn, Germany
    ChemMedChem 1:891-902. 2006
    ..Their efficacy was generally lower than that of the full inverse agonist DPCPX, and depended on subtle structural changes. Some of the new compounds belong to the most potent and selective A(1) antagonists described to date...
  10. ncbi Activation of the adenosine A1 receptor inhibits HIV-1 tat-induced apoptosis by reducing nuclear factor-kappaB activation and inducible nitric-oxide synthase
    Sandeep C Pingle
    Department of Pharmacology, Southern Illinois University School of Medicine, PO Box 19629, Springfield, IL 62794 9629, USA
    Mol Pharmacol 72:856-67. 2007
    ..Taken together, our results demonstrate that the A(1)AR protects against HIV-1 toxicity by inhibiting NF-kappaB, thereby reducing the expression of iNOS and NO radicals and neuronal apoptosis...
  11. ncbi Blood-brain barrier transport of synthetic adenosine A1 receptor agonists in vitro: structure transport relationships
    Marloes P Schaddelee
    Leiden Amsterdam Center for Drug Research, Division of Pharmacology, P O Box 9502, 2300 RA Leiden, The Netherlands
    Eur J Pharm Sci 20:347-56. 2003
    ..In addition, transport by the es nucleoside transporter may contribute to the transport of certain structurally distinct analogues...
  12. ncbi Activation of adenosine A1 receptor-induced neural stem cell proliferation via MEK/ERK and Akt signaling pathways
    Hideyuki Migita
    Department of Stem Cell Based Drug Discovery, Research Center Kobe, Bayer Yakuhin Ltd, Kobe, Japan
    J Neurosci Res 86:2820-8. 2008
    ..In addition, CPA-induced cell proliferation was inhibited by MEK and Akt inhibitors. These results suggest that activation of adenosine A(1) receptor-stimulated proliferation of NSCs occurs via MEK/ERK and Akt signaling pathways...
  13. pmc Ecto-5'-nucleotidase (CD73) inhibits nociception by hydrolyzing AMP to adenosine in nociceptive circuits
    Nathaniel A Sowa
    Department of Cell and Molecular Physiology, UNC Neuroscience Center and Curriculum in Neurobiology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, USA
    J Neurosci 30:2235-44. 2010
    ..Moreover, our data suggest NT5E is well localized to regulate nucleotide signaling between skin cells and sensory axons...
  14. ncbi Adenosine induces a cholinergic tracheal reflex contraction in guinea pigs in vivo via an adenosine A1 receptor-dependent mechanism
    Sandra M Reynolds
    Pharmaceutical Science Research Division, The Sackler Institute of Pulmonary Pharmacology, School of Biomedical and Health Science, King s College London, London SE1 1UL, UK
    J Appl Physiol (1985) 105:187-96. 2008
    ..In conclusion, activation of pulmonary adenosine A(1) receptors can stimulate cholinergic reflexes, and these reflexes are increased in allergic guinea pigs...
  15. pmc Role of central and peripheral adenosine receptors in the cardiovascular responses to intraperitoneal injections of adenosine A1 and A2A subtype receptor agonists
    Charles W Schindler
    Preclinical Pharmacology Section, Behavioral Neuroscience Branch, Department of Health and Human Services, National Institutes of Health National Institute on Drug Abuse, Intramural Research Program, Baltimore, MD, USA
    Br J Pharmacol 144:642-50. 2005
    1. The cardiovascular effects of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) and the adenosine A2A receptor agonist 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine (CGS 21680) were investigated in ..
  16. pmc Quantitative analysis of the formation and diffusion of A1-adenosine receptor-antagonist complexes in single living cells
    S J Briddon
    Institute of Cell Signalling, Medical School, University of Nottingham, Nottingham NG7 2UH, United Kingdom
    Proc Natl Acad Sci U S A 101:4673-8. 2004
    ..The combination of FCS with XAC-BY630 will be a powerful tool for the characterization of ligand-A1-AR interactions in single living cells in health and disease...
  17. ncbi Association analysis of adenosine A1 receptor gene (ADORA1) polymorphisms with schizophrenia in a Japanese population
    Leo Gotoh
    Department of Neuropsychiatry, Graduate School of Medical Sciences, Kyushu University, Maidashi, Higashi ku, Japan
    Psychiatr Genet 19:328-35. 2009
    The human adenosine A1 receptor gene (ADORA1) localizes to chromosome 1q32 is 76.8 kbp in length and contains six exons...
  18. ncbi Adenosine A1 receptor-dependent G-protein activity in the rat brain during prolonged wakefulness
    Lauri O Alanko
    Institute of Biomedicine, University of Helsinki, P O Box 63, FIN 00014 Helsinki, Finland
    Neuroreport 15:2133-7. 2004
    ..evidence showing that the sleep-inducing effects are mediated locally in the basal forebrain through the adenosine A1 receptor. In previous studies an increase in the mRNA expression but no apparent change in the ligand binding of ..
  19. ncbi Subcellular localization of adenosine A(1) receptors in nerve terminals and synapses of the rat hippocampus
    Nelson Rebola
    Center for Neuroscience of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
    Brain Res 987:49-58. 2003
    ....
  20. ncbi Frequency facilitation at mossy fiber-CA3 synapses of freely behaving rats is regulated by adenosine A1 receptors
    Jens Klausnitzer
    Department of Experimental Neurophysiology, Medical Faculty, Ruhr University Bochum, 44780 Bochum, Germany
    J Neurosci 28:4836-40. 2008
    ..The adenosine A1 receptor antagonists, DPCPX (8-cyclopentyl-1,3-dipropylxanthine) and phenylxanthine, markedly enhanced mossy fiber ..
  21. pmc Late preconditioning induced by NO donors, adenosine A1 receptor agonists, and delta1-opioid receptor agonists is mediated by iNOS
    Yiru Guo
    Institute of Molecular Cardiology, Univ of Louisville, Louisville, KY, USA
    Am J Physiol Heart Circ Physiol 289:H2251-7. 2005
    ..diethylenetriamine/NO (DETA/NO), nitroglycerin (NTG), and S-nitroso-N-acetyl-penicillamine (SNAP)], an adenosine A1 receptor agonist [2-chloro-N6-cyclopentyladenosine (CCPA)], and a delta1-opioid receptor agonist (TAN-670)...
  22. pmc Anti-inflammatory preconditioning by agonists of adenosine A1 receptor
    Sigal Nakav
    Department of Clinical Biochemistry, Soroka Medical University Center and Ben Gurion University of the Negev, Beer Sheva, Israel
    PLoS ONE 3:e2107. 2008
    ..We previously reported that peak A(1)R expression during leukocyte recruitment, is followed by a peak in A(2A)R during inflammation resolution...
  23. ncbi Delayed adenosine A1 receptor preconditioning in rat myocardium is MAPK dependent but iNOS independent
    Robert D Lasley
    Department of Surgery, Univ of Kentucky College of Medicine, MN276, Chandler Medical Center, 800 Rose St, Lexington, KY 40536 0298, USA
    Am J Physiol Heart Circ Physiol 289:H785-91. 2005
    b>Adenosine A1 receptor delayed preconditioning (PC) against myocardial infarction has been well described; however, there have been limited investigations of the signaling mechanisms that mediate this phenomenon...
  24. pmc Mice lacking the adenosine A1 receptor have normal spatial learning and plasticity in the CA1 region of the hippocampus, but they habituate more slowly
    Lydia Gimenez-Llort
    Medical Psychology Unit, Department of Psychiatry and Forensic Medicine, Institute of Neuroscience, Autonomous University of Barcelona, 08193 Bellaterra, Barcelona, Spain
    Synapse 57:8-16. 2005
    Using mice with a targeted disruption of the adenosine A1 receptor (A1R), we examined the role of A1Rs in hippocampal long-term potentiation (LTP), long-term depression (LTD), and memory formation...
  25. ncbi Ageing-related decline in adenosine A1 receptor binding in the rat brain: an autoradiographic study
    Peter Meerlo
    Department of Molecular Neurobiology, Graduate School of Behavioral and Cognitive Neurosciences, University of Groningen, Groningen, The Netherlands
    J Neurosci Res 78:742-8. 2004
    ..In the present study, we examined adenosine A1 receptor density in the rat brain by means of quantitative autoradiography to obtain a detailed anatomical overview ..
  26. ncbi [Relation between adenosine A1 receptor and NMDA receptor on synaptic transmission in dentate gyrus of hippocampus]
    Dan Shen Zhang
    College of Pharmacy, Hebei Medical University, Shijiazhuang 050017, China
    Yao Xue Xue Bao 39:245-9. 2004
    ..To observe the effect of adenosine A, receptor antagonist on synaptic transmission in the dentate gyrus of hippocampus and its relations with NMDA receptor...
  27. ncbi Osmotic diuretics induce adenosine A1 receptor expression and protect renal proximal tubular epithelial cells against cisplatin-mediated apoptosis
    Sandeep C Pingle
    Department of Pharmacology, Southern Illinois University School of Medicine, Springfield, Illinois 62702, USA
    J Biol Chem 279:43157-67. 2004
    ..b>Adenosine A1 receptor (A1AR) subtype present on renal proximal tubular epithelial and cortical collecting duct cells mediates ..
  28. ncbi Repeated cocaine administration changes the function and subcellular distribution of adenosine A1 receptor in the rat nucleus accumbens
    Shigenobu Toda
    Physiology and Neuroscience, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Neurochem 87:1478-84. 2003
    b>Adenosine A1 receptor (A1) protein and mRNA is increased in the nucleus accumbens following repeated cocaine treatment...
  29. ncbi Adenosine A1 receptor mapping of the human brain by PET with 8-dicyclopropylmethyl-1-11C-methyl-3-propylxanthine
    Nobuyoshi Fukumitsu
    Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Tokyo, Japan
    J Nucl Med 46:32-7. 2005
    ..In this study, we quantitatively evaluated the distribution of a major subtype A(1) adenosine receptor in the human brain by PET with a newly developed radioligand, 8-dicyclopropylmethyl-1-(11)C-methyl-3-propylxanthine ((11)C-MPDX)...
  30. ncbi Cardioprotection induced by adenosine A1 receptor agonists in a cardiac cell ischemia model involves cooperative activation of adenosine A2A and A2B receptors by endogenous adenosine
    Vijay B Urmaliya
    Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, Victoria, Australia
    J Cardiovasc Pharmacol 53:424-33. 2009
    ....
  31. ncbi Adenosine A1 receptor antagonists in clinical research and development
    Berthold Hocher
    Institute of Nutritional Science, University of Potsdam, Potsdam, Germany
    Kidney Int 78:438-45. 2010
    Selective adenosine A1 receptor antagonists targeting renal microcirculation are novel pharmacologic agents that are currently under development for the treatment of acute heart failure as well as for chronic heart failure...
  32. ncbi Induction of adenosine A1 receptor expression by pertussis toxin via an adenosine 5'-diphosphate ribosylation-independent pathway
    Sarvesh Jajoo
    Department of Pharmacology, Southern Illinois University School of Medicine, Springfield, Illinois 62794 9629, USA
    J Pharmacol Exp Ther 317:1-10. 2006
    ..We conclude that pertussis toxin promotes de novo A(1)AR synthesis by activating NF-kappaB through an ADP ribosylation-independent mechanism involving intracellular Ca(2+) release and PKC activation...
  33. pmc Recombinant ecto-5'-nucleotidase (CD73) has long lasting antinociceptive effects that are dependent on adenosine A1 receptor activation
    Nathaniel A Sowa
    Department of Cell and Molecular Physiology, UNC Neuroscience Center, University of North Carolina, CB 7545, Chapel Hill, North Carolina 27599, USA
    Mol Pain 6:20. 2010
    ..Since adenosine has antinociceptive effects in rodents and humans, we hypothesized that NT5E, an enzyme that generates adenosine, might also have antinociceptive effects in vivo...
  34. ncbi Adenosine A1 receptor knockout mice develop lethal status epilepticus after experimental traumatic brain injury
    Patrick M Kochanek
    Safar Center for Resuscitation Research, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania 15260, USA
    J Cereb Blood Flow Metab 26:565-75. 2006
    ..05) and SE was restricted to the ko mice (83% incidence). Our data suggest a critical endogenous anticonvulsant action of adenosine at A1 receptors early after experimental TBI...
  35. ncbi The effect of KW-3902, an adenosine A1 receptor antagonist, on renal function and renal plasma flow in ambulatory patients with heart failure and renal impairment
    Howard C Dittrich
    NovaCardia, Inc, San Diego, California 92130, USA
    J Card Fail 13:609-17. 2007
    ..This raises the possibility of using adenosine A1 receptor (AA1R) antagonists to selectively vasodilate the kidney in conditions, such as congestive heart failure, ..
  36. ncbi Deletion of the adenosine A1 receptor gene does not alter neuronal damage following ischaemia in vivo or in vitro
    Tomas Olsson
    Laboratory for Experimental Brain Research, Wallenberg Neuroscience Center, Lund University, BMC A13, SE 221 84, Sweden
    Eur J Neurosci 20:1197-204. 2004
    ..is considered to be neuroprotective due to its inhibitory effect on synaptic transmission mediated by the adenosine A1 receptor (A1R)...
  37. ncbi Interleukin-6-type cytokines in neuroprotection and neuromodulation: oncostatin M, but not leukemia inhibitory factor, requires neuronal adenosine A1 receptor function
    Shamsudheen Moidunny
    Department of Neuroscience, Section Medical Physiology, University Medical Center Groningen UMCG, Rijksuniversiteit Groningen RUG, Groningen, The Netherlands
    J Neurochem 114:1667-77. 2010
    ..No such effect was observed after LIF pre-treatment. Our findings thus strongly suggest that, despite known structural and functional similarities, OSM and LIF use different mechanisms to achieve neuroprotection and neuromodulation...
  38. pmc Reduced basal and lipopolysaccharide-stimulated adenosine A1 receptor expression in the brain of nuclear factor-kappaB p50-/- mice
    K A Jhaveri
    Department of Pharmacology, Southern Illinois University School of Medicine, PO Box 19629, Springfield, IL 62794 9629, USA
    Neuroscience 146:415-26. 2007
    ..Previous studies from our laboratory indicate that the expression of the adenosine A1 receptor (A1AR) is induced by oxidative stress via activation of nuclear factor (NF)-kappaB...
  39. ncbi Adenosine A1 and A2A receptors are co-expressed in pyramidal neurons and co-localized in glutamatergic nerve terminals of the rat hippocampus
    N Rebola
    Center for Neurosciences of Coimbra, Institute of Biochemistry, Faculty of Medicine, University of Coimbra, 3004 504 Coimbra, Portugal
    Neuroscience 133:79-83. 2005
    ..e. glutamatergic nerve terminals. This indicates that glutamatergic neurons in the hippocampus co-express A1 and A2A receptors and that these two receptors are co-localized in a subset of glutamatergic nerve terminals...
  40. pmc The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure
    P Kalk
    Department of Pharmacology and Toxicology, Center for Cardiovascular Research, Charite, Campus Mitte, Hessische Strasse 3 4, 10115 Berlin, Germany
    Br J Pharmacol 151:1025-32. 2007
    ..The adenosine system is involved in cardiac and renal function. Therefore, we investigated the novel selective adenosine A(1) receptor antagonist SLV320 focusing on its potential in preventing cardiomyopathy in rats with 5/6 nephrectomy...
  41. ncbi Role of adenosine receptors in regulating chemotaxis and cytokine production of plasmacytoid dendritic cells
    Max Schnurr
    Ludwig Institute Oncology Unit, Melbourne Tumour Biology Branch, Austin and Repatriation Medical Centre, Studley Rd, Heidelberg, Victoria 3084, Australia
    Blood 103:1391-7. 2004
    ....
  42. ncbi A1 adenosine receptors accumulate in neurodegenerative structures in Alzheimer disease and mediate both amyloid precursor protein processing and tau phosphorylation and translocation
    Ester Angulo
    Departament de Bioquimica i Biologia Molecular, University of Barcelona, Spain
    Brain Pathol 13:440-51. 2003
    ..b>Adenosine A1 receptor (A1R) immunoreactivity was found in degenerating neurons with neurofibrillary tangles and in dystrophic ..
  43. pmc Adenosine gates synaptic plasticity at hippocampal mossy fiber synapses
    Kimberly A Moore
    Department of Cellular and Molecular Pharmacology and Physiology, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 100:14397-402. 2003
    ....
  44. ncbi A "locked-on," constitutively active mutant of the adenosine A1 receptor
    Rianne A F de Ligt
    Division of Medicinal Chemistry, Leiden Amsterdam Center for Drug Research, Leiden University, P O Box 9502, 2300 RA Leiden, The Netherlands
    Eur J Pharmacol 510:1-8. 2005
    We studied the wild-type human adenosine A1 receptor and three mutant receptors, in which the glycine at position 14 had been changed into an alanine, a leucine, or a threonine residue...
  45. pmc Mice heterozygous for both A1 and A(2A) adenosine receptor genes show similarities to mice given long-term caffeine
    Jiang Ning Yang
    Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden
    J Appl Physiol (1985) 106:631-9. 2009
    ..Thus at least some aspects of long-term caffeine use can be mimicked by genetic manipulation of the A(1)R and A(2A)R...
  46. pmc Neuroprotective effect of paeoniflorin on cerebral ischemic rat by activating adenosine A1 receptor in a manner different from its classical agonists
    Da Zhi Liu
    Department of Pharmacology, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Pudong, Shanghai 201203, China
    Br J Pharmacol 146:604-11. 2005
    ..c.) was abolished by pretreatment of DPCPX (0.25 mg kg(-1), s.c.), a selective adenosine A1 receptor (A1R) antagonist. PF (10, 40, and 160 mg kg(-1), i.v...
  47. ncbi The antinociceptive effects of the systemic adenosine A1 receptor agonist CPA in the absence and in the presence of spinal cord sensitization
    M Mar Curros-Criado
    Departamento de Fisiologia, Facultad de Medicina, Universidad de Alcala, Madrid, Spain
    Pharmacol Biochem Behav 82:721-6. 2005
    b>Adenosine A1 receptor agonists are effective antinociceptive agents in neuropathic and inflammatory pain, though they appear to be weak analgesics in acute nociception...
  48. ncbi Adenosine A1 receptor-mediated inhibition of dopamine release from rat striatal slices is modulated by D1 dopamine receptors
    C O'Neill
    UCD School of Biomolecular and Biomedical Science, Conway Institute of Biomolecular and Biomedical Research, Belfield Dublin 4, Ireland
    Eur J Neurosci 26:3421-8. 2007
    ..While the mechanism underlying this interaction remains to be determined, it does not appear to involve an intramembrane interaction between A(1) and D(1) receptors...
  49. pmc Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity
    Gregory D Stewart
    Monash Institute of Pharmaceutical Sciences, Parkville, Victoria, Australia
    J Pharmacol Exp Ther 331:277-86. 2009
    ..Our results suggest that this yeast system is a useful tool for quantifying ligand affinity and relative efficacy, but it may lack the sensitivity required to detect functional selectivity of low-efficacy agonists...
  50. ncbi Genetic deletion of the A1 adenosine receptor limits myocardial ischemic tolerance
    Melissa E Reichelt
    Heart Foundation Research Centre, Griffith University, Southport, QLD, Australia
    Circ Res 96:363-7. 2005
    ..Data indicate the function of intrinsically activated A1ARs appears primarily to be enhancement of postischemic contractility and limitation of cell death...
  51. ncbi Differences in the expression of the adenosine A1 receptor in adipose tissue of obese black and white women
    Hisham Barakat
    Department of Medicine, Brody School of Medicine, East Carolina University, Greenville, North Carolina 27858, USA
    J Clin Endocrinol Metab 91:1882-6. 2006
    ..African-American women (AAW) lose less weight and at a slower rate than Caucasian women (CAW) under the same weight-loss regimens. A potential cause of this finding is inhibition of lipolysis...
  52. pmc Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands
    Jillian G Baker
    Institute of Cell Signalling, School of Biomedical Sciences, Medical School, University of Nottingham, Queen s Medical Centre, Nottingham, UK
    Br J Pharmacol 159:772-86. 2010
    ..This study evaluated how the physicochemical nature of the linker and the fluorophore affected the pharmacological properties of fluorescent agonists and antagonists...
  53. ncbi Nitric oxide serves as an endogenous regulator of neuronal adenosine A1 receptor expression
    Krishna A Jhaveri
    Department of Pharmacology, Southern Illinois University School of Medicine, Springfield, Illinois 62794 9629, USA
    J Neurochem 99:42-53. 2006
    ..As the expression of the adenosine A1 receptor (A1AR) is regulated by oxidative stress, we evaluated the role of NO in the regulation of A1AR expression, ..
  54. ncbi Adenosine A1 receptor activation reduces opening of mitochondrial permeability transition pores in hypoxic cardiomyocytes
    Fei Xiang
    Institute of Burn Research, State Key Laboratory of Trauma, Burn and Combined Injury, Southwest Hospital, Third Military Medical University, Chongqing, China
    Clin Exp Pharmacol Physiol 37:343-9. 2010
    ..5. These results demonstrate that CCPA reduces MPTP opening in hypoxic cardiomyocytes, possibly by activating PKC, stabilizing Deltapsi and reducing ROS production following the opening of mitoK(ATP). Consequently, fewer MPTP open...
  55. ncbi Adenosine A1 receptor binding activity of methoxy flavonoids from Orthosiphon stamineus
    Nancy Dewi Yuliana
    Division of Pharmacognosy, Section Metabolomics, Institute of Biology, Leiden University, Leiden, The Netherlands
    Planta Med 75:132-6. 2009
    ....
  56. pmc Role of beta-arrestin1/ERK MAP kinase pathway in regulating adenosine A1 receptor desensitization and recovery
    Sarvesh Jajoo
    PO Box 19629, SIU School of Medicine, Springfield, IL 62794, USA
    Am J Physiol Cell Physiol 298:C56-65. 2010
    ..We propose that such a pathway ensures both the termination of the agonist signal and recovery by priming the cell for rapid de novo synthesis of A(1)AR once the drug is terminated...
  57. pmc Paeoniflorin attenuates neuroinflammation and dopaminergic neurodegeneration in the MPTP model of Parkinson's disease by activation of adenosine A1 receptor
    Hua Qing Liu
    Department of Pharmacology II, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi Tech Park, Pudong, Shanghai 201203, China
    Br J Pharmacol 148:314-25. 2006
    ..4. Pretreatment with 0.3 mg kg(-1) 8-cyclopentyl-1,3-dipropylxanthine, an adenosine A1 receptor (A1AR) antagonist, 15 min before each dose of PF, reversed the neuroprotective and antineuroinflammatory ..
  58. ncbi Endogenous activation of adenosine A1 receptors promotes post-ischemic electrocortical burst suppression
    A Ilie
    Center for Excellence in Neuroscience, Carol Davila University of Medicine and Pharmacy, Bucharest, Romania
    Neuroscience 159:1070-8. 2009
    ..Here we tested in vivo whether synaptic depression by adenosine A1 receptor (A1R) activation contributes to BS patterns following GCI...
  59. ncbi Oxidative stress and adenosine A1 receptor activation differentially modulate subcellular cardiomyocyte MAPKs
    Cherry Ballard-Croft
    Department of Surgery, University of Kentucky, MN265 Chandler Medical Center, 800 Rose St, Lexington, KY 40536 0298, USA
    Am J Physiol Heart Circ Physiol 294:H263-71. 2008
    ..However, the adenosine A(1) receptor-mediated MAPK activation does not involve ROS formation...
  60. ncbi Effects of targeted deletion of A1 adenosine receptors on postischemic cardiac function and expression of adenosine receptor subtypes
    R Ray Morrison
    Division of Critical Care Medicine, St Jude Children s Research Hospital, 332 N Lauderdale St, MS 734, Memphis, TN 38105, USA
    Am J Physiol Heart Circ Physiol 291:H1875-82. 2006
    ..Together, these data affirm the cardioprotective role of A(1)ARs and suggest that induced expression of other adenosine receptor subtypes may participate in the response to ischemia-reperfusion in isolated murine hearts...
  61. ncbi Up-regulation of adenosine A1 receptors in frontal cortex from Pick's disease cases
    José Luis Albasanz
    Departamento de Quimica Inorganica, Organica y Bioquimica, Facultad de Quimicas, Centro Regional de Investigaciones Biomédicas, Universidad de Castilla La Mancha, Ciudad Real, Spain
    Eur J Neurosci 26:3501-8. 2007
    ..These results show that the adenosine A(1)R-AC transduction pathway is specifically up-regulated and sensitized in frontal cortex brain in PiD...
  62. pmc Combined effects of carbonic anhydrase inhibitor and adenosine A1 receptor antagonist on hemodynamic and tubular function in the kidney
    Cynthia M Miracle
    Division of Nephrology Hypertension, University of California, Veterans Affairs San Diego Healthcare System, San Diego, CA 92161, USA
    Kidney Blood Press Res 30:388-99. 2007
    ..Adenosine A(1) receptors (A(1)R) mediate the TGF response and stimulate proximal reabsorption...
  63. ncbi Increase in adenosine A1 receptor gene expression in the liver of streptozotocin-induced diabetic rats
    I M Liu
    Department of Pharmacology, College of Medicine, National Cheng Kung University, Tainan City, Taiwan 70101, Republic of China
    Diabetes Metab Res Rev 19:209-15. 2003
    b>Adenosine A1 receptor (A1-AR) activation can lower plasma glucose in diabetic rats lacking insulin. We investigated the change in A1-AR gene expression in diabetic rats.
  64. ncbi Early renal post-ischaemic tissue damage and dysfunction with contribution of A1-adenosine receptor activation in rat
    S M S Moosavi
    Department of Physiology, The Medical School, Shiraz University Medical Sciences, Shiraz, Iran
    Nephrology (Carlton) 14:179-88. 2009
    ..This study investigated the effect of a selective A(1)-adenosine receptor (A(1)-AR) antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), on the renal dysfunction and histological damage induced by ischaemia/reperfusion at an early stage...
  65. ncbi Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes
    Luigi Aurelio
    Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia
    J Med Chem 52:4543-7. 2009
    ..More detailed concentration-response experiments were subsequently performed on two compounds (9a and 9o) utilizing both the ERK1/2 assay as well as a second assay of [(35)S]GTPgammaS binding to activated G proteins...
  66. ncbi Role of the second transmembrane domain of rat adenosine A1 receptor in ligand-receptor interaction
    Ke Qiang Xie
    Department of Pharmacology, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China
    Biochem Pharmacol 71:865-71. 2006
    ..This observation suggests that the hydrophobic region at the outer end of TM2 may mediate the recognition of the ribose group of CCPA and NECA...
  67. ncbi Increase of adenosine A1 receptor gene expression in cerebral ischemia of Wistar rats
    Dar Ming Lai
    Neurosurgical Division, Department of Surgery, National Taiwan University Hospital, Taipei 10001, Taiwan
    Neurosci Lett 387:59-61. 2005
    In an attempt to know the role of adenosine A1 receptor in cerebral ischemia, the present study employed the ligation of bilateral carotid arteries to induce ischemia in Wistar rats...
  68. ncbi Delineating the mode of action of adenosine A1 receptor allosteric modulators
    Celine Valant
    Drug Discovery Biology and Department of Pharmacology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia
    Mol Pharmacol 78:444-55. 2010
    ..These mechanisms need to be factored into allosteric ligand structure-activity studies...
  69. pmc Adenosine and ATP link PCO2 to cortical excitability via pH
    Chris G Dulla
    Neuroscience Program, Department of Neurology, University of Colorado Health Sciences Center, Denver, Colorado 80262, USA
    Neuron 48:1011-23. 2005
    ..These findings demonstrate a mechanism for the bidirectional effects of CO(2) on neuronal excitability in the forebrain...
  70. ncbi Effects of adenosine deaminase and A1 receptor deficiency in normoxic and ischaemic mouse hearts
    Laura Willems
    Heart Foundation Research Center, Griffith University, Southport, QLD 4217, Australia
    Cardiovasc Res 71:79-87. 2006
    ..Herein we assess effects of ADA (and A1AR) deficiency on AR-mediated responses and ischaemic tolerance...
  71. ncbi A novel role for protein phosphatase 2A in receptor-mediated regulation of the cardiac sarcolemmal Na+/H+ exchanger NHE1
    Andrew K Snabaitis
    Cardiovascular Division, King s College London, London SE1 7EH, UK
    J Biol Chem 281:20252-62. 2006
    ....
  72. ncbi Presynaptic control of striatal glutamatergic neurotransmission by adenosine A1-A2A receptor heteromers
    Francisco Ciruela
    Department of Biochemistry and Molecular Biology, University of Barcelona, 08028 Barcelona, Spain
    J Neurosci 26:2080-7. 2006
    ....
  73. ncbi A comparison of the antagonist affinities for the Gi- and Gs-coupled states of the human adenosine A1-receptor
    Jillian G Baker
    Institute of Cell Signaling, Queen s Medical Centre, Nottingham NG7 2UH, UK
    J Pharmacol Exp Ther 320:218-28. 2007
    ..This was true even when the receptor was shown, in the same assay, to exist in two different conformational states coupled to two different G proteins...
  74. ncbi Subcellular distributions of adenosine A1 and A2A receptors in the rat dorsomedial nucleus of the solitary tract at the level of the area postrema
    Virginia M Pickel
    Department of Neurology and Neuroscience, Cornell University Medical College, New York 10021, USA
    Synapse 60:496-509. 2006
    ....
  75. ncbi Morphine can enhance the antiallodynic effect of intrathecal R-PIA in rats with nerve ligation injury
    Jai Hyun Hwang
    Department of Anesthesia and Pain Medicine, University of Ulsan, College of Medicine, Asan Medical Center, 388 1 Pungnap dong, Songpa Gu, Seoul 138 736, Korea
    Anesth Analg 100:461-8. 2005
    ..In this study, we examined the effect of intrathecal morphine on the antiallodynic state induced by the adenosine A1 receptor agonist, N(6)-(2-phenylisopropyl)-adenosine R-(-)isomer (R-PIA), in a rat model of nerve ligation injury...
  76. ncbi Increased nociceptive response in mice lacking the adenosine A1 receptor
    Wei ping Wu
    Department of Neurotec, Division of Clinical Neurophysiology, Karolinska Institutet, Karolinska University Hospital Huddinge, S 141 86 Stockholm, Sweden
    Pain 113:395-404. 2005
    The role of the adenosine A1 receptor in nociception was assessed using mice lacking the A1 receptor (A1R-/-) and in rats...
  77. ncbi Isoflurane tolerance against focal cerebral ischemia is attenuated by adenosine A1 receptor antagonists
    Yanhong Liu
    Department of Anesthesiology, Xijing Hospital, Fourth Military University, Xi an, Shaanxi, China
    Can J Anaesth 53:194-201. 2006
    To investigate the role of the adenosine A1 receptor in the rapid tolerance to cerebral ischemia induced by isoflurane preconditioning.
  78. ncbi RNA interference targeting of A1 receptor-overexpressing breast carcinoma cells leads to diminished rates of cell proliferation and induction of apoptosis
    Asra Mirza
    Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    Cancer Biol Ther 4:1355-60. 2005
    ..Together these findings suggest that the A1 adenosine receptor may contribute to tumor cell growth and survival in breast tumor cells...
  79. ncbi 2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers
    George Nikolakopoulos
    Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia
    Bioorg Med Chem 14:2358-65. 2006
    ..The structure-activity relationships of these classes of compound are described. A number of compounds, notably 7b, are more potent and efficacious than PD81,723 (1)...
  80. ncbi Direct excitation of inhibitory interneurons by extracellular ATP mediated by P2Y1 receptors in the hippocampal slice
    Masahito Kawamura
    Laboratory of Neurophysiology, Department of Neuroscience, Jikei University School of Medicine, Minato ku, Tokyo 105 8461, Japan
    J Neurosci 24:10835-45. 2004
    ....
  81. ncbi Influence of the adenosine A1 receptor on blood pressure regulation and renin release
    Russell D Brown
    Dept of Medical Cell Biology, Division of Integrative Physiology, Uppsala Univ, S 751 23 Uppsala, Sweden
    Am J Physiol Regul Integr Comp Physiol 290:R1324-9. 2006
    ..Our results confirm that adenosine, acting through the adenosine A1 receptor, plays an important role in regulating blood pressure, renin release, and sodium excretion.
  82. ncbi Chronic caffeine or theophylline intake during pregnancy inhibits A1 receptor function in the rat brain
    D Leon
    Area de Bioquímica, Facultad de Quimicas, Centro Regional de Investigaciones Biomédicas, Universidad de Castilla La Mancha, Avenida Camilo Jose Cela 10, 13071 Ciudad Real, Spain
    Neuroscience 131:481-9. 2005
    ....
  83. ncbi Combination of adenosine A1 and A2A receptor blocking agents induces caffeine-like locomotor stimulation in mice
    Alexander Kuzmin
    Department of Neuroscience, Karolinska Institutet, Sweden
    Eur Neuropsychopharmacol 16:129-36. 2006
    ..It is hypothesised that the stimulatory effect of low doses of caffeine in C57BL/6J mice is due to concomitant blockade of both A(1) and A(2A) adenosine receptors...
  84. pmc Recombinant mouse PAP has pH-dependent ectonucleotidase activity and acts through A(1)-adenosine receptors to mediate antinociception
    Nathaniel A Sowa
    Department of Cell and Molecular Physiology, UNC Neuroscience Center, University of North Carolina, Chapel Hill, North Carolina, USA
    PLoS ONE 4:e4248. 2009
    ..Lastly, our studies demonstrate that recombinant PAP protein can be used to treat chronic pain in animal models...
  85. ncbi New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells
    Richard J Middleton
    School of Pharmacy, Centre for Biomolecular Sciences, and School of Chemistry, University of Nottingham, University Park, Nottingham, United Kingdom
    J Med Chem 50:782-93. 2007
    ....
  86. ncbi The antinociceptive effect of 2-chloro-2'-C-methyl-N6-cyclopentyladenosine (2'-Me-CCPA), a highly selective adenosine A1 receptor agonist, in the rat
    S Maione
    Department of Experimental Medicine, Second University of Naples, Naples, Italy
    Pain 131:281-92. 2007
    ..5 nmol/rat). This study confirms the role of adenosine A(1) receptors in modulating pain and suggests a critical involvement of these receptors within PAG-RVM descending pathway for the processing of pain...
  87. pmc Adenosine modulates transmission at the hippocampal mossy fibre synapse via direct inhibition of presynaptic calcium channels
    A Gundlfinger
    Neurowissenschaftliches Forschungszentrum der Charité, Universitatsmedizin Berlin, Germany
    J Physiol 582:263-77. 2007
    ..Specifically, we found that adenosine modulates both P/Q- and N-type presynaptic voltage-dependent Ca2+ channels and thereby controls transmitter release at the mossy fibre synapse...
  88. ncbi Sex differences in mouse heart rate and body temperature and in their regulation by adenosine A1 receptors
    J N Yang
    Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden
    Acta Physiol (Oxf) 190:63-75. 2007
    ..To examine cardiac function, body temperature and locomotor behaviour in the awake adenosine A(1) receptor knock out mouse of both sexes...
  89. ncbi Elevated expression of adenosine A1 receptor in bronchial biopsy specimens from asthmatic subjects
    R A Brown
    Sackler Institute of Pulmonary Pharmacology, Division of Pharmaceutical Sciences, London, SE1 1UL, UK
    Eur Respir J 31:311-9. 2008
    ..In conclusion, the sensitivity of asthmatics to inhaled adenosine coupled with increased adenosine A(1) receptor expression implies that these receptors play a role in the pathophysiology of this disease...
  90. ncbi Adenosine A1 but not A2a receptor agonist reduces hyperalgesia caused by a surgical incision in rats: a pertussis toxin-sensitive G protein-dependent process
    Peter K Zahn
    Department for Anaesthesiology and Operative Intensive Care, University of Muenster, Muenster, Germany
    Anesthesiology 107:797-806. 2007
    ..In the current study, the authors investigated the role of spinal adenosine A1Rs and A2aRs for the maintenance of mechanical hyperalgesia in an animal model for postoperative pain...
  91. pmc Hypoxia induces cardiac malformations via A1 adenosine receptor activation in chicken embryos
    Satish K Ghatpande
    Section of Developmental Endocrinology and Biology, Yale Child Health Research Center, Department of Pediatrics, Yale University School of Medicine, New Haven, Connecticut 06520, USA
    Birth Defects Res A Clin Mol Teratol 82:121-30. 2008
    ..Potential mediators of hypoxic effects include adenosine, which increases dramatically during hypoxic conditions and activates A(1) adenosine receptors (A(1)ARs)...
  92. ncbi Adenosine A1 receptor antagonists and the kidney
    Paul S Modlinger
    Division of Nephrology, The Cardiovascular Kidney Institute, Georgetown University, Washington, Distritic of Columbia, USA
    Curr Opin Nephrol Hypertens 12:497-502. 2003
    ..In addition, A(1)-receptors may have a role for the prevention or treatment of ischemic injury to the kidney by maintaining afferent arteriole vasodilatation and preserving the glomerular filtration rate...
  93. ncbi Hypotensive effects of intravenously administered uridine and cytidine in conscious rats: involvement of adenosine receptors
    M Sertac Yilmaz
    Uludag University Faculty of Medicine, Department of Pharmacology and Clinical Pharmacology, 16059, Gorukle, Bursa, Turkey
    Eur J Pharmacol 584:125-36. 2008
    ..The data also implicates that the mainly adenosine A(1) receptor activation is involved in the uridine-induced cardiovascular effects, while both adenosine A(1) and A(2A) receptor activations mediate the cytidine's effects...
  94. pmc A1 adenosine receptors mediate hypoxia-induced ventriculomegaly
    Christopher P Turner
    Department of Pediatrics, Yale University School of Medicine, New Haven, CT 06520, USA
    Proc Natl Acad Sci U S A 100:11718-22. 2003
    ..Thus, adenosine acting on A1ARs appears to mediate hypoxia-induced brain injury ventriculomegaly during early postnatal development...
  95. ncbi Caffeine reduces hypnotic effects of alcohol through adenosine A2A receptor blockade
    M El Yacoubi
    UMR 6036 CNRS, IFRMP 23, UFR de Médecine and Pharmacie, 22 Boulevard Gambetta, 76183 Rouen Cedex, France
    Neuropharmacology 45:977-85. 2003
    ..Thus, A(2A) receptor antagonists may be useful therapeutic agents for alleviating ethylic coma...
  96. ncbi Moderate cerebral venous congestion induces rapid cerebral protection via adenosine A1 receptor activation
    Keiichi Akaiwa
    Department of Surgery, Kurume University School of Medicine, Kurume, Japan
    Brain Res 1122:47-55. 2006
    ..The DPCPX group received the adenosine A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) prior to mild VC...
  97. ncbi p38 mitogen-activated protein kinase contributes to adenosine A1 receptor-mediated synaptic depression in area CA1 of the rat hippocampus
    Tyson B Brust
    Brain Research Centre, Department of Psychiatry, University of British Columbia, Vancouver, British Columbia, Canada V6T 2B5
    J Neurosci 26:12427-38. 2006
    ..Here, we demonstrate a novel mechanism in which adenosine A1 receptor stimulation leads to p38 mitogen-activated protein kinase (MAPK) activation and contributes to the ..
  98. ncbi The adenosine A1 receptor contributes to the stimulatory, but not the inhibitory effect of caffeine on locomotion: a study in mice lacking adenosine A1 and/or A2A receptors
    Linda Halldner
    Department of Physiology and Pharmacology, Section of Molecular Pharmacology, Karolinska Institutet, Nanna Svartz vag 2, S 171 77 Stockholm, Sweden
    Neuropharmacology 46:1008-17. 2004
    ..Furthermore, these results suggest that the inhibitory effect of high doses of caffeine is due neither to blockade of the A1R, nor of the A2AR, and an effect independent of these adenosine receptors is likely...
  99. ncbi Modulation of A1 adenosine receptor signaling by peroxynitrite
    Janette Giuntini
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Pisa, Italy
    Biochem Pharmacol 67:375-83. 2004
    ..This treatment influenced [35S]GTPgammaS binding affinity for A(1)AR activated G(i) proteins in cortical membranes. These findings suggest that ONOO(-) modulates A(1)AR signaling pathways by affecting receptor G(i) protein coupling...
  100. ncbi Protective effects of caffeine on chronic hypoxia-induced perinatal white matter injury
    Stephen A Back
    Department of Pediatrics, Oregon Health and Science University, Portland, OR, USA
    Ann Neurol 60:696-705. 2006
    ....
  101. pmc Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine
    Jiang Ning Yang
    Karolinska Institutet, Nanna Svartz vag 2, Stockholm S 171 77 Sweden
    Am J Physiol Heart Circ Physiol 296:H1141-9. 2009
    ..The A(2A)R plays an important role in the modulation of O(2)C and LA by acute and chronic caffeine administration. There is also evidence for effects of higher doses of caffeine being independent of both A(1)R and A(2A)R...

Research Grants62

  1. Astrocytic Ca2+ Signaling in the Ischemic Penumbra
    Maiken Nedergaard; Fiscal Year: 2011
    ..Preliminary observations show that the adenosine A1 receptor antagonist, DPCPX, triggered a robust increase in synaptic activity in the penumbra without a concomitant ..
  2. Purinergic Regulation of Bone Metabolism
    Bruce Neil Cronstein; Fiscal Year: 2013
    ..Moreover, adenosine A1 receptor knockout mice have increased bone formation in vivo and adenosine receptor blockade blocks bone loss in ..
  3. Somatic cell gene transfer/neurological &clinical applications
    En Ju Lin; Fiscal Year: 2013
    ..We propose to use this system to regulate expression of the adenosine A1 receptor in a spontaneous seizure model, an approach which directly complements our adenosine kinase knockout ..
  4. The Role of Adenosine in Ketogenic Diet Therapy
    Susan A Masino; Fiscal Year: 2013
    ..The central hypothesis is that ketogenic diets increase adenosine A1 receptor activation, and that this increased inhibitory influence of adenosine is critical for the anticonvulsant ..
  5. Adenosine, Hypocretin and Sleep Disorder Comorbidities Associated with Epilepsy
    Kristina A Simeone; Fiscal Year: 2013
    ..that in LH of epileptic mice (1) there is a pathology that is associated reduced adenosine levels;(2) adenosine A1 receptor-mediated inhibition of hypocretin neurons is diminished; (3) hypocretin protein is elevated and activity ..
  6. Analgesic actions of adenosine A1 receptor along axonal tracts in chronic pain
    Takahiro Takano; Fiscal Year: 2013
    ..Moreover, local administration of an adenosine A1 receptor agonist in the Zusanli acupoint in mice mimicked the analgesic actions of acupuncture...
  7. SYNAPTIC BASIS OF SLEEP CYCLE CONTROL
    Robert W McCarley; Fiscal Year: 2013
    ..We predict an increase in adenosine A1 receptor binding (number of active receptors) with 24h SD...
  8. Cellular Mechanisms Mediating the Somnogenic Effects of Ethanol
    Mahesh M Thakkar; Fiscal Year: 2010
    ..Increased adenosine, acting via adenosine A1 receptor, will inhibit the wake-promoting cholinergic neurons of the basal forebrain as evidenced by a reduction in ..
  9. ALLOSTERIC ENHANCEMENT OF ADENOSINE RECEPTORS
    Joel M Linden; Fiscal Year: 2009
    ..evaluate enhancer function in intact cells and to evaluate selected compounds for activity in modulating adenosine A1 receptor function in brain slices and stimulation of angiogenesis...
  10. Control of Synaptic Glutamate Release
    Steven J Mennerick; Fiscal Year: 2013
    ..we hypothesize that presynaptic silencing of glutamate synapses is triggered non-autonomously by prolonged adenosine A1 receptor activation...
  11. BASAL FOREBRAIN HYPOCRETIN REGULATION OF WAKING
    Priyattam J Shiromani; Fiscal Year: 2010
    ..Aim 2 will test the hypothesis that in the absence of the BF cholinergic neurons adenosine or the adenosine A1 receptor agonist CHA will not induce sleep...
  12. RESVERATROL AS A PHARMACOLOGICAL PRECONDITIONING AGENT
    Debasis Bagchi; Fiscal Year: 2004
    ..by addressing three Specific Aims: i) whether resveratrol mediated cardioprotection is achieved through adenosine A1 receptor activation; ii) whether resveratrol function through translocation and activation of protein kinase C (PKC)..
  13. Protection with Adenosine A1 Receptor Overexpression
    DAVID VAN WYLEN; Fiscal Year: 2002
    ..has recently been harnessed through a transgenic mouse model of cardiac specific overexpression of the adenosine A1 receptor that demonstrates remarkable protection against ischernia-reperfusion injury...
  14. REGULATION OF PERIPHERAL INFLAMMATION BY THE CNS
    Gary Firestein; Fiscal Year: 2002
    ..Neutrophil infiltration into dermal inflammatory sites was significantly reduced by adenosine A1 receptor agonists injected through intrathecal catheters...
  15. Neurochemical Regulation of Circadian Timing
    Michael Rea; Fiscal Year: 2005
    ..cholinergic area during sustained wakefulness, where it has been shown to promote sleep through an adenosine A1 receptor-dependent mechanism...
  16. ANTISENSE OLIGONUCLEOTIDE FOR ASTHMA
    Jonathan Nyce; Fiscal Year: 1999
    ..The investigators have developed a respirable antisense oligonucleotide, EPI 2010, which targets the adenosine A1 receptor. They have shown that it has anti-bronchoconstrictor and anti-inflammatory actions and can restore normal ..
  17. ADENOSINE A1 AND A2 RECEPTORS IN THE MYOCARDIUM
    James Dobson; Fiscal Year: 2004
    ..Additionally, the findings should significantly contribute to our basic knowledge of the molecular mechanisms of G protein coupled receptor cross-regulation in the heart. ..
  18. Myocardial Adenosine Receptors
    James G Dobson; Fiscal Year: 2010
    ..We and others have reported that adenosine A1 receptor (A1R), adenosine A2A receptor (A2AR) and ?1 adrenergic receptor (?1 R) stimulation results in a number of ..
  19. ELECTROPHYSIOLOGY & PHARMACOLOGY OF SLEEP-WAKEFULNESS
    Mahesh Thakkar; Fiscal Year: 2004
    ..Preliminary data suggest a strong suppressive effect of microdialysis-applied 8-OH-DPAT on state-related discharge activity of the dorsal raphe nucleus, and we will also investigate the effects of 5HT1A antagonists. ..
  20. ADENOSINE AND TRAUMATIC BRAIN INJURY
    Patrick Kochanek; Fiscal Year: 2007
    ..These studies explore the most promising adenosine-based therapy for TBI-A2a receptor antagonists. Our bench to bedside track record ensures translation to the clinic. [unreadable] [unreadable]..
  21. Drug-Induced Motor Recovery After Spinal Cord Injury
    Kwaku Nantwi; Fiscal Year: 2005
    ..abstract_text> ..
  22. Ischemia-Reperfusion in A2A and A2B Knockout Hearts
    R Morrison; Fiscal Year: 2007
    ....
  23. The modulation of adenosine by temperature, oxygen and glucose
    SUSAN MASINO; Fiscal Year: 2008
    ..The specific inhibitory influence of the adenosine A1 receptor subtype reduces activity and helps neurons survive a short-term compromised energy supply, such as during ..
  24. Measuring Striatal Neurotransmission in Behaving Rats after Experimental TBI
    Amy Wagner; Fiscal Year: 2008
    ..The overarching goal is to gain insight into potential mechanisms of action and efficacy of these interventions on cognition and recovery for the clinical population with TBI. [unreadable] [unreadable] [unreadable]..
  25. Screening Putative Therapeutic Agents for Fetal Ethanol-Induced Learning Deficits
    DANIEL SAVAGE; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  26. Adenosinergic Mechanisms of Intrauterine Growth Retardation
    Scott A Rivkees; Fiscal Year: 2010
    ..The goals of this proposal are to identify the mechanisms by which adenosine acts to protect the embryo in utero and how altered embryonic adenosine action leads to long-term adverse effects in adulthood. ..
  27. Role of adenosine A3 receptor in suppressing prostate cancer
    Vickram Ramkumar; Fiscal Year: 2008
    ..Therefore, these goals will form the specific aims of the current grant proposal. We believe that this study could uncover a novel method of treating prostate cancer metastasis. [unreadable] [unreadable] [unreadable]..
  28. Effect of Drugs on Myocardial Hypoxia
    Garrett Gross; Fiscal Year: 2009
    ..Information gained from these studies will hopefully lead to new therapies to treat patients with ischemic heart disease. ..
  29. Renin activation in early diabetes
    Janos Peti Peterdi; Fiscal Year: 2009
    ..These studies should yield clinically important information that can be used to develop new drugs and therapeutic approaches for the better treatment of diabetic complications in the kidney as well as high blood pressure. ..
  30. Biochemical Modulation of Nociceptive Circuits
    MARK JOHN ZYLKA; Fiscal Year: 2010
    ..Finally, we will test the hypothesis that this phosphatase modulates neuropathic pain behaviors in wild-type and phosphatase knockout mice. ..
  31. Translational Foundation of Adenosine Antagonist Use for Dyskinesias
    Michael A Schwarzschild; Fiscal Year: 2010
    ....
  32. Anti-Adenosine Therapy of Neonatal Brain Injury
    Scott Rivkees; Fiscal Year: 2007
    ..It is anticipated that these studies will lead to novel and practical strategies for directly preventing brain injury. [unreadable] [unreadable]..
  33. Renin regulation by nitric oxide
    WILLIAM BEIERWALTES; Fiscal Year: 2007
    ..These studies should reveal the dual pathways by which NO can either inhibit or stimulate renin secretion. ..
  34. Dopamine D2 and Adenosine A2A roles:Tremulous Movements
    John Salamone; Fiscal Year: 2007
    ..abstract_text> ..
  35. A-1 Adenosine Receptor Action in Developing Heart
    Scott Rivkees; Fiscal Year: 2005
    ..We anticipate that these studies will identify Rho and ROCK as critical signaling molecules in heart development and reveal that cardiac GTPase activity transduces the effects of adenosine. ..
  36. MECHANISMS OF INJURY POTENTIATION BY GROWTH FACTORS
    DOUGLAS LOBNER; Fiscal Year: 2004
    ..It is believed that these studies will aid in determining under what conditions growth factor induced potentiation of cell death may be of concern regarding their therapeutic use, and how those concerns may be addressed. ..
  37. MOLECULAR REGULATORY MECHANISMS OF BRAIN OPIOID SYSTEMS
    STEVEN CHILDERS; Fiscal Year: 2002
    ..Finally, mechanisms of chronic opioid action on receptor-G-protein interactions will be examined in both brain sections and in mu receptor-transfected NG108-15 cells. ..
  38. NO AND OXIDATIVE STRESS IN HUMAN MYOCARDIAL FAILURE
    Michael Givertz; Fiscal Year: 2003
    ..abstract_text> ..
  39. TNF-ALPHA REGULATION OF AT1 RECEPTOR & POST-MI FIBROSIS
    Barry Greenberg; Fiscal Year: 2003
    ..This information will provide important insights into the pathogenesis of post-MI fibrosis. ..
  40. Translating A2A Receptor Biology into Novel PD Therapy
    Michael Schwarzschild; Fiscal Year: 2002
    ..Thus, this timely conference stands to serve as a catalyst for developing A2A antagonists as a novel multi-faceted treatment strategy for Parkinson's disease. ..
  41. A1-ADENOSINE RECEPTOR ACTION IN HIPPOCAMPUS
    Scott Rivkees; Fiscal Year: 2003
    ..We anticipate these studies will lead to new insights into the mechanisms of A1AR action. We also anticipate that these studies will identify A1ARs as an important regulator of axon growth. ..
  42. Ca permeable non-NMDAr: New spinal sensitization pathway
    Linda Sorkin; Fiscal Year: 2005
    ..We propose to investigate the effects of Ca-permeable non-NMDAr activation on ERK and CREB phosphorylation (using Western blots and immunohistochemistry), expression of c-fos and development of hyperalgesia. ..
  43. Novel Neuroprotection by Caffeine in Parkinson's Disease
    Michael Schwarzschild; Fiscal Year: 2005
    ....
  44. Protein Biomarkers of Drinking During Pregnancy
    DANIEL SAVAGE; Fiscal Year: 2006
    ..abstract_text> ..
  45. DEVELOPING CIRCADIAN RHYTHMICITY
    Scott Rivkees; Fiscal Year: 2002
    ..These studies may also lead to the development of new care practices in Neonatal Intensive Care Units and extend the field of developmental chronobiology to the bedside. ..
  46. BEHAVIORAL EFFECTS OF NIGRAL D1 ANTAGONISM
    John Salamone; Fiscal Year: 2001
    ....
  47. Neural Analysis of Maternal Aggression
    STEPHEN GAMMIE; Fiscal Year: 2006
    ..Basic research into sex differences in aggression, then, is important to understanding the biological underpinnings of sex and gender differences in social behavior, health, and disease. ..
  48. CB1 Receptor Action on the Developing Hippocampus
    Scott Rivkees; Fiscal Year: 2005
    ..We anticipate that these studies will result in new insights into the potential effects of cannabinoid action on the developing brain. ..
  49. A2A Adenosine Receptors in Psychostimulant Sensitization
    Michael Schwarzschild; Fiscal Year: 2005
    ..clarify the role of A2A receptors in psychostimulant-induced addictive behaviors, and thus may encourage the development of novel, specific strategies for treating psychostimulant abuse and related addiction disorders ..
  50. MECHANISMS OF ARND RELATED SYNAPTIC PLASTICITY DEFICITS
    DANIEL SAVAGE; Fiscal Year: 2002
    ..Further, these results could provide insights into whether agents that affect mGluR function could be used to treat synaptic plasticity deficits and, ultimately, learning deficits in prenatal ethanol-exposed offspring. ..
  51. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2003
    ..Taken together, the results of these experiments will help to identify the pharmacological characteristics and brain circuits that underlie the motor effects of clozapine. ..
  52. Gender Differences in Dopamine Function after TBI
    Amy Wagner; Fiscal Year: 2003
    ....
  53. Targeting Adenosine A2A Receptors in Parkinson's Disease
    Michael Schwarzschild; Fiscal Year: 2006
    ..Thus this timely conference is designed to catalyze the development of A2A antagonists as a novel multi-faceted treatment strategy for Parkinson's disease and related CMS disorders. [unreadable] [unreadable] [unreadable]..
  54. Vaccine therapy of congenital adrenal Hyperplasia
    Scott Rivkees; Fiscal Year: 2003
    ..We also anticipate being able to extend this novel approach to the treatment of other receptor-mediated endocrine disorders, such as hyperthyroidism. ..
  55. ADENOSINE AND MODULATION OF SYNAPTIC TRANSMISSION
    SUSAN MASINO; Fiscal Year: 2004
    ..plays an important role in regulating the basic excitability of neurons by performing experiments in adenosine A1 receptor-knockout mice...
  56. Growth factor effects on dental pulp cells
    DOUGLAS LOBNER; Fiscal Year: 2008
    ..As a method of maintaining the viability of these cells we are proposing studying the effects of naturally occurring substances called growth factors on dental pulp cells. [unreadable] [unreadable] [unreadable]..
  57. Cytokine and MAP Kinase Involvement in Neuropathic Pain
    Linda Sorkin; Fiscal Year: 2008
    ..This approach has the potential for avoiding some of the problems that occur with complete inhibition of p38 function. ..
  58. Adenosine Agonists: Potential Antiglaucoma Agents
    Craig E Crosson; Fiscal Year: 2010
    ..abstract_text> ..