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AdenosineAdenosine-5'-(N-ethylcarboxamide)Adenosine A1 Receptor AntagonistsReceptor, Adenosine A2AAdenosine A2 Receptor AntagonistsPurinergic P1 Receptor AntagonistsAdenosine A2 Receptor AgonistsReceptor, Adenosine A1Receptors, Purinergic P1Adenosine A1 Receptor AgonistsXanthinesPhenethylaminesReceptor, Adenosine A2BTheophyllinePurinergic P1 Receptor AgonistsAdenosine DeaminaseReceptor, Adenosine A3Adenosine KinaseReceptors, Adenosine A2Adenosine MonophosphateReceptors, PurinergicAdenosine A3 Receptor Antagonists2-ChloroadenosineAdenosine A3 Receptor AgonistsPhenylisopropyladenosineInosineCyclic AMP5'-NucleotidaseAdenosine TriphosphatasesTubercidinCationsAdenine NucleotidesDose-Response Relationship, DrugFlufenamic AcidCalciumRats, Sprague-DawleyNucleoside DeaminasesCoformycinIon ChannelsDipyridamoleTheobromineCyclooxygenase 2 InhibitorsVasodilator AgentsTriazinesRats, WistarKineticsPurinesCells, CulturedPentostatinAdenosine PhosphosulfatePurinergic AntagonistsEnzyme InhibitorsAdenineMembrane PotentialsPatch-Clamp TechniquesCyclooxygenase InhibitorsReceptors, Purinergic P2Guinea PigsTRPC Cation ChannelsThioinosineTriazolesPhosphodiesterase InhibitorsAnti-Inflammatory Agents, Non-SteroidalDeoxyadenosinesVasodilationAminophyllineMyocardiumTRPM Cation ChannelsSulfonamidesTime FactorsNucleoside Transport ProteinsPotassium ChannelsCoronary CirculationHypoxanthineAdenylate CyclaseNucleotidasesIsoproterenolCaffeine1-Methyl-3-isobutylxanthineHypoxanthinesCalcium ChannelsRabbitsNucleosidesColforsinDogsRadioligand AssayApyrasePropanolaminesLanthanumExtracellular SpaceCell LineAdrenergic beta-AntagonistsSignal TransductionCell MembranePyrazolesPotassium8-Bromo Cyclic Adenosine MonophosphatePurinergic P2 Receptor AntagonistsNitric OxideGlyburide
ReceptorsAntagonistCaffeineCyclicIntracellularNucleosideInhibitionExtracellularTriphosphateReceptor subtypesAgonist adenosineSpecific adenosineNECAAminophyllinePharmacologicalModulatesPotentAntagonistsInduceA2ARMetabolismAdenineAntagonismTherapeuticIncreasesBiologicalHypoxiaAcuteBindingPhysiologicalActivationMechanismResultsMaximalSevereActivityCellsSystemReleaseRate
Receptors31
  • The stimulant properties of caffeine and various analogs were correlated with the blockade of adenosine receptors. (wikipedia.org)
  • It was clear that ligands of adenosine receptors and inhibitors for phosphodiesterase were targets for drug development. (wikipedia.org)
  • In 1992, the therapeutic potential for both agonists and antagonists of the adenosine receptors was highlighted for A2 receptors, and in 2001 the therapeutic potential for adenosine antagonists was highlighted. (wikipedia.org)
  • Broad reviews from 2006 have been focusing on adenosine receptors as therapeutic targets, adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti-inflammatories and many more. (wikipedia.org)
  • report findings in adenosine deaminase-deficient mice that suggest the occurrence of anti-inflammatory actions of adenosine in the lung, mediated through A 1 adenosine receptors on macrophages. (jci.org)
  • Here we discuss the history of the study of adenosine receptor ligands for asthma and how enhanced understanding of adenosine receptor biology may aid in the rational exploitation of these receptors as therapeutic targets. (jci.org)
  • ATP, released by cells, is rapidly metabolized by extracellular nucleotidases to adenosine, a potent signaling molecule that can activate several cell surface receptors to produce myriad effects on both parenchymal and immune cells throughout the body (Figure 1 ). (jci.org)
  • Adenosine can act at 4 different 7-transmembrane, G-protein-coupled receptors present on the surfaces of both infiltrating leukocytes and resident parenchymal cells. (jci.org)
  • Notably, cellular responses to hypoxia are characterized by robust increases in extracellular adenosine production and the markedly induced adenosine receptors, which provide a novel target for preferential control of pathological angiogenesis without affecting normal vascular development. (unboundmedicine.com)
  • TY - JOUR T1 - Adenosine receptors and caffeine in retinopathy of prematurity. (unboundmedicine.com)
  • Adenosine causes nonselective activation of four different receptors, including A2A-mediated vasodilation of the coronary microcirculation and 'off target' A2B receptor-mediated mast cell degranulation and bronchial constriction. (rcpe.ac.uk)
  • Caffeine, one of the most consumed central nervous system (CNS) stimulants, is an antagonist of A 1 and A 2A adenosine receptors. (frontiersin.org)
  • By attempting to counteract the hypoxic condition, activation of adenosine A2A receptors (A2AR) occurs in a cooperative fashion with hypoxia, modulating the anti-inflammatory pathway and stimulating VEGF release [3]. (scienceopen.com)
  • HB7814(30 nM) binding to live CHO cells expressing adenosine A1 receptors. (hellobio.com)
  • cell sorting at adenosine A 1 / A 2A / A 3 receptors use solutions up to 100 nM. (hellobio.com)
  • Adenosine receptors are closely associated with dopamine receptors and form heteromer s with them. (adxs.org)
  • At the same time, adenosine modulates striatal DA release by stimulating glutamate release at adenosine receptors in the striatum , which increases dopamine levels. (adxs.org)
  • Part of this adenosine is discharged from the cell and binds to adenosine receptors of neighboring cells, which is supposed to compensate for the disturbed balance between energy consumption and energy supply. (adxs.org)
  • Cellular signalling occurs through adenosine receptors (ARs). (turkupetcentre.net)
  • All four adenosine receptor subtypes (A 1 , A 2A , A 2B , and A 3 ) are G protein-coupled receptors (GPCRs), either increasing or decreasing intracellular cAMP levels by affecting adenylate cyclase activity. (turkupetcentre.net)
  • Like other GPCRs, adenosine receptors have a single polypeptide chain, forming three extracellular and three intracellular loops. (turkupetcentre.net)
  • Adenosine receptors are also referred to as purine receptors , or P1 purinoceptors . (turkupetcentre.net)
  • Adenosine has the highest affinity to the A 1 R and A 2A R, intermediate affinity to A 3 R, and lowest affinity to A 2B R. Adenosine activates A 1 and A 2A receptors already in nanomolar concentrations. (turkupetcentre.net)
  • Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors. (dcchemicals.com)
  • Blockade of beta-receptors results in decreased production of intracellular cyclic adenosine monophosphate (cAMP) with a resultant blunting of multiple metabolic and cardiovascular effects of circulating catecholamines. (medscape.com)
  • Propranolol is a nonselective beta-blocker, demonstrating equal affinity for both beta1- and beta2-receptors. (medscape.com)
  • Pentoxifylline is also a non-selective antagonist of adenosine receptors A 1 and A 2A that are located in both the heart and brain. (epiphanyasd.com)
  • Nevertheless, the potencies of adenosine agonists in locomotor major depression were recently discovered to correlate towards the potencies from the analogs at A2 adenosine receptors rather than to potencies at A1 adenosine receptors (Durcan and Morgan, 1989a), resulting in the proposal that mainly A2 receptors get excited about these results. (thetechnoant.info)
  • Although A1-selective agonists have already been created, adenosine agonists or antagonists really selective for A2 adenosine receptors for make use of as physiological probes have already been difficult to recognize. (thetechnoant.info)
  • Lately, we reported that APEC is normally a powerful locomotor depressant in mice which the pharmacological profile of the actions suggests activation of A2 adenosine receptors (Nikodijevic 1990). (thetechnoant.info)
  • The mechanism by which caffeine exerts its effects is now largely accepted to be through non-selective antagonism of adenosine A1 and A2A receptors (1), with A1 receptors being more closely related to neural activation and A2A receptor antagonism leading to vascular effects, including vasoconstriction and a reduction in cerebral blood flow (CBF) (1). (neubria.com)
Antagonist13
  • Recently, the A2A receptor antagonist 3-chlorostyrylcaffeine has been reported to be a potent inhibitor of monoamine oxidase B. An inverse relationship between non-selective adenosine receptor antagonists, the consumption of caffeine and the risk of developing Parkinson's disease has been indicated from epidemiological studies. (wikipedia.org)
  • Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. (adooq.com)
  • The clinical and initial animal evidence that implicate the therapeutic effect of caffeine (a non-selective adenosine receptor antagonist) in treatment of ROP are highlighted. (unboundmedicine.com)
  • Caffeine (CAF), a nonselective adenosine A1 and A2A receptor antagonist and commonly used psychoactive substance, may affect these disorders in a dose-dependent manner. (aaem.pl)
  • In this regard, the effects of PDRN in the experimental model of ischemic colitis are abolished using DMPX, a specific adenosine A2AR antagonist. (scienceopen.com)
  • of two different anxiogenic/panicogenic medications (FG-7142, an inverse agonist on the benzodiazepine site from the GABAA receptor, and caffeine, a non-selective competitive adenosine receptor antagonist) elevated c-Fos induction in a particular subset of orexin neurons situated in the dorsomedial/ perifornical (DMH/PeF) however, not the lateral hypothalamus. (bioinf.org)
  • Competitive fluorescent adenosine receptor antagonist (apparent K D values are 7.50, 7.37 and 7.30 for A 2A , A 3 and A 1 respectively). (hellobio.com)
  • The CellAura fluorescent adenosine antagonist [XAC] ligand was shown to antagonize the activity of the adenosine receptor agonist adenosine-5'-N-ethyluronamide (NECA), in three separate recombinant CHO cell lines expressing the human A 1 , A 2A or A 3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.The cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions. (hellobio.com)
  • Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. (dcchemicals.com)
  • PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. (dcchemicals.com)
  • Responses to the previously studied non-selective adenosine-receptor (AR) agonist adenosine, the A3-selective agonist Cl-IB-MECA and the A3-selective antagonist MRS 1191 were all enhanced to varying degrees, in time and magnitude, by corneal impalement. (edu.hk)
  • The nonselective adenosine-receptor antagonist caffeine as well as the selective A1 adenosine-receptor antagonist DPCPX however not the selective A2A adenosine-receptor antagonist SCH58261 totally avoided allopurinol-induced anti-nociception. (biopaqc.com)
  • Pre-treatment with pertussis toxin (Gi/o-protein inhibitor), DPCPX (A1 adenosine receptor antagonist) or TG2 inhibitors (Z-DON and R283) attenuated the A1 adenosine receptor-induced pharmacological pre- and post-conditioning. (ntu.ac.uk)
Caffeine4
  • Notable adenosine A2A receptor antagonists include caffeine, theophylline and istradefylline. (wikipedia.org)
  • Lastly, we discussed the translational potential as well therapeutic advantage of adenosine receptor- and caffeine-based therapy for ROR and possibly other proliferative retinopathy. (unboundmedicine.com)
  • Caffeine, a nonselective competitive PDE inhibitor, due to its structural similarity to adenosine molecule maintains the cAMP level by occupying PDE enzymes such as PDE-3A inside the oocyte and PDE-4 and PDE-5 in the cumulus cells. (sruc.ac.uk)
  • Caffeine adenosine DPCPX and SCH58261 dosages had been based on previously function (Lara (1993). (biopaqc.com)
Cyclic5
Intracellular1
Nucleoside6
  • The endogenous purine nucleoside adenosine is one proinflammatory mediator that has garnered interest as a contributor to asthma pathogenesis, particularly with regard to acute exacerbations of the disease. (jci.org)
  • Adenosine is an endogenous purine nucleoside, composed of nucleobase adenine and β-D-ribose moieties. (turkupetcentre.net)
  • Adenosine is rapidly catabolized by adenosine deaminases to inosine, which can be further deribosylated by purine nucleoside phosphorylase to hypoxantine . (turkupetcentre.net)
  • Adenosine cannot freely pass across the cell and vesicular membranes, but it needs to be transported by nucleoside transporters, which are present in most cells, including erythrocytes . (turkupetcentre.net)
  • Dipyridamole elevates extracellular adenosine concentrations by inhibiting equilibrative nucleoside transporters (ENTs). (turkupetcentre.net)
  • Though causes of miscarriage remain unclear, adenosine, a proangiogenic nucleoside, may help determine pregnancy outcome. (unipr.it)
Inhibition2
  • Elevations of extracellular adenosine are present in the asthmatic lung due to both increased release of ATP from cells and inhibition of ADA by local hypoxia. (jci.org)
  • Methotrexate ( MTX ) increases adenosine release by inhibition of purine metabolism. (turkupetcentre.net)
Extracellular3
  • Extracellular adenosine is produced predominantly by the metabolism of ATP released from cells. (jci.org)
  • ADA is the primary catabolic enzyme for adenosine, and its absence in ADA-deficient mice results in marked elevations of extracellular adenosine. (jci.org)
  • Interstitial adenosine concentration is normally in the range 20-200 nM, and its extracellular half-life is short, a few seconds at most. (turkupetcentre.net)
Triphosphate2
Receptor subtypes1
  • Here, we review the experimental evidence in support of adenosine receptor-based therapeutic strategy for ROP, including the aberrant adenosine signaling in oxygen-induced retinopathy and the role of three adenosine receptor subtypes (A1R, A2AR, A2BR) in development and treatment of ROP using oxygen-induced retinopathy models. (unboundmedicine.com)
Agonist adenosine1
  • Agonists, including endogenous agonist adenosine, lead to the activation of all AR subtypes, and subsequent regulation by desensitization and trafficking ( Mundell and Kelly, 2011 ). (turkupetcentre.net)
Specific adenosine1
  • While both proinflammatory and anti-inflammatory signals can be sent depending on the specific adenosine receptor activated, adenosine produces a net proinflammatory effect in the asthmatic airway. (jci.org)
NECA2
  • Antagonizes the activity of NECA, an adenosine receptor agonist. (hellobio.com)
  • The non-selective adenosine agonist 5′-N-ethylcarboxamidoadenosine (NECA) increased NO, by activating, predominantly, A1AR and A2AAR through a molecular pathway involving hypoxia-inducible-factor-1 (HIF-1α), and increased VEGF, mainly through A2B. (unipr.it)
Aminophylline1
  • Physicians should be aware of the utility of bolus intravenous aminophylline providing targeted therapy to reverse and treat adenosine-related bronchospasm. (rcpe.ac.uk)
Pharmacological1
  • The primary aim of this study was to determine the role of TG2 in A1 adenosine receptor and β2-adrenoceptor-induced pharmacological pre- and post-conditioning in the H9c2 cells. (ntu.ac.uk)
Modulates1
Potent1
  • Several attempts have been made by using virtual screening to identify potent A2A adenosine receptor antagonists. (wikipedia.org)
Antagonists3
  • Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. (wikipedia.org)
  • As growing lines of evidence have supported a proinflammatory role for adenosine in the asthmatic lung, interest in adenosine receptor antagonists has risen. (jci.org)
  • The locomotor effects in mice of selective A1 and A2 adenosine agonists, antagonists and combinations of agonists were investigated utilizing a computerized activity monitor. (thetechnoant.info)
Induce2
  • Background Adenosine is frequently used during coronary angiography to induce hyperaemia and allow operators to perform quantitative measurements of lesion severity. (rcpe.ac.uk)
  • adenosine and adenosine agonists attenuate inflammation , and induce vasodilation and angiogenesis in the cardiovascular system . (turkupetcentre.net)
A2AR2
  • 1], the authors documented a PDRN ability in increasing VEGF expression, reducing the histological damage, downregulating anti-inflammatory responses, and modulating apoptosis through the interaction with adenosine A2AR. (scienceopen.com)
  • Furthermore, considering the involvement of VEGF in the activation of adenosine A2AR, we believe it could be advantageous to demonstrate the effect of PDRN on neoangiogenesis and microvessel density, which may result in an augmented oxygen supply and a subsequent balance of the apoptotic mechanism [3]. (scienceopen.com)
Metabolism1
Adenine1
Antagonism1
  • Evidence for efficacy of adenosine receptor antagonism may date back to the Victorian era, when physicians noted the beneficial effects of strong black coffee in patients with bronchial asthma. (jci.org)
Therapeutic1
  • Adenosine A2A receptor locations in the body could help us to understand the possible therapeutic applications in the future. (wikipedia.org)
Increases1
Biological1
  • Adenosine is a ubiquitous biological mediator with the capacity to produce both pro- and anti-inflammatory effects in tissues. (jci.org)
Hypoxia2
  • A1 adenosine receptor agonist), formoterol (β2-adrenoceptor agonist) or isoprenaline (non-selective β-adrenoceptor agonist) were added before hypoxia/reoxygenation (pre-conditioning) or at the start of reoxygenation following hypoxia (post-conditioning). (ntu.ac.uk)
  • These results have shown that A1 adenosine receptor and β2-adrenoceptor-induced protection against simulated hypoxia/reoxygenation occurs in a TG2 and Gi/o-protein dependent manner in H9c2 cardiomyoblasts. (ntu.ac.uk)
Acute1
  • We defined acute severe bronchospasm as acute dyspnoea and wheeze temporally related (within 5 min) to systemic adenosine administration with features of respiratory distress. (rcpe.ac.uk)
Binding1
  • Adenosine binding to both pre- and postsynaptic A 1 Rs has an inhibitory effect in the brain. (turkupetcentre.net)
Physiological1
  • Adenosine is certainly a modulator of several physiological features. (thetechnoant.info)
Activation1
  • Proinflammatory and bronchoconstrictive actions of adenosine in the asthmatic lung are well recognized, with the latter being mediated, in part, through A 1 receptor activation on airway smooth muscle. (jci.org)
Mechanism2
  • Through this mechanism, the increased level of adenosine after sleep deprivation could affect the light sensitivity of the circadian clock. (adxs.org)
  • Although adenosine receptor (AR) expression has been characterized in euploid pregnancies, no information is available for aneuploidies, which, as prone to spontaneous abortion (SA), are a potential model for shedding light on the mechanism regulating this event. (unipr.it)
Results1
  • Hence, it would appear that A1- and A2-selective adenosine agonists possess different central depressant results, which may be potentiative. (thetechnoant.info)
Maximal1
  • 1 For practical purposes, maximal hyperaemia is typically induced using systemic administration of adenosine (rather than exercise). (rcpe.ac.uk)
Severe1
  • The true incidence of severe bronchospasm relating to adenosine administration is not known. (rcpe.ac.uk)
Activity1
  • We have previously reported that transglutaminase 2 (TG2) activity is modulated by the A1 adenosine receptor and β2-adrenoceptor in H9c2 cardiomyoblasts. (ntu.ac.uk)
Cells2
  • Adenosine is found in almost all body cells. (adxs.org)
  • Adenosine deaminase isoform 1 (ADA1) is found in most cells, including blood cells. (turkupetcentre.net)
System1
Release1
Rate1
  • Our local protocol administers adenosine at a rate of 0.84 mg/kg/min through a large peripheral vein. (rcpe.ac.uk)