Adenosine agonist. Medical search. Frequent questions

Furthermore, PDRN treatment enhanced the concentration of cyclic adenosine-3,5'-monophosphate (cAMP) as well as phosphorylation of cAMP response element-binding protein (p-CREB). (iasp-pain.org)
Cyclic adenosine monophosphate ( cAMP , cyclic AMP , or 3',5'-cyclic adenosine monophosphate ) is a second messenger , or cellular signal occurring within cells, that is important in many biological processes. (wikipedia.org)
Earl Sutherland of Vanderbilt University won a Nobel Prize in Physiology or Medicine in 1971 "for his discoveries concerning the mechanisms of the action of hormones", especially epinephrine, via second messengers (such as cyclic adenosine monophosphate, cyclic AMP). (wikipedia.org)
The stimulation of cells with isoproterenol (7683592) in the presence of TDI failed to release cyclic-adenosine- monophosphate (cAMP). (cdc.gov)
Activator of protein kinase A (cyclic AMP agonist). (biolog.de)

Examples include the neurotransmitter adenosine, its phosphates, adenosine monophosphate (AMP), adenosine diphosphate (ADP), and adenosine triphosphate (ATP), and the pharmaceutical drug regadenoson. (wikipedia.org)
cAMP is a derivative of adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway . (wikipedia.org)
In this study, we used lipopolysaccharide (LPS) and adenosine triphosphate (ATP) to simulate an inflammatory environment as the testing model. (spandidos-publications.com)
Adenosine triphosphate (ATP), released from dying cells, has a high concentration within the cell. (spandidos-publications.com)

ATL146e (A2A selective) PD81,723 (A1 allosteric enhancer) CF102 (Adenosine A3 receptor) Adenosine receptor antagonist Adenosine reuptake inhibitor Glover, David K. (wikipedia.org)
In order to confirm the participation of the adenosine A2A receptor in the effects mediated by PDRN, 8 mg/kg 7-dimethyl-1-propargylxanthine (DMPX), adenosine A2A receptor antagonist, was treated with PDRN. (iasp-pain.org)
KW-6356 is a novel adenosine A 2A receptor (A 2A receptor) antagonist/inverse agonist, and its efficacy as monotherapy in Parkinson's disease (PD) patients has been reported. (aspetjournals.org)
In this study, we investigated the in vitro pharmacological profile of KW-6356 as an A 2A receptor antagonist/inverse agonist and the mode of antagonism and compared them with istradefylline. (aspetjournals.org)
Significance Statement KW-6356 is a potent and selective adenosine A 2A receptor antagonist/inverse agonist and exhibits insurmountable antagonism, while istradefylline, a first-generation adenosine A 2A receptor antagonist, exhibits surmountable antagonism. (aspetjournals.org)
Application of the A1 receptor antagonist 8-cyclo-pentyl-theophylline (200 nM) blocked the effects of adenosine. (nih.gov)

The adenosine signaling pathway activated by sleep deprivation has shown rapid benefits in preclinical and clinical studies. (grantome.com)
An adenosine A3 receptor agonist inhibits DSS-induced colitis in mice through modulation of the NF-κB signaling pathway. (rndsystems.com)

A fluorescent adenosine receptor ligand derived from NECA, non-selective adenosine agonist. (hellobio.com)
Hemodynamic effects of histamine release elicited by the selective adenosine A 3 receptor agonist 2-Cl-IB-MECA in conscious rats. (rndsystems.com)

Detailed three dimensional structures of GPCRs in various activation states can now help to explain the functional impact of cancer-associated GPCR mutations, and guide the rational design of signalling-selective GPCR agonists, antagonists and allosteric modulators. (nature.com)

Clinicians should avoid using the imaging agents regadenoson ( Lexiscan , Astellas Pharma US) and adenosine ( Adenoscan , Astellas Pharma US) for cardiac nuclear stress tests of patients with signs or symptoms of unstable angina or cardiovascular instability because the drugs may increase their risk for a fatal heart attack, the US Food and Drug Administration (FDA) announced today. (medscape.com)
The agency approved adenosine in 1995 and regadenoson in 2008 for radionuclide myocardial perfusion imaging in patients who cannot undergo exercise stress testing. (medscape.com)
The labels for both regadenoson and adenosine had previously warned of the risk for MI. (medscape.com)
Ensure that cardiac resuscitation equipment and trained staff are available before administering adenosine or regadenoson. (medscape.com)
Cite this: FDA Issues Warning on Regadenoson, Adenosine - Medscape - Nov 20, 2013. (medscape.com)
Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing. (chemspider.com)
The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects.Regadenoson has a 2 to 3 minute biological half-life. (chemspider.com)

Pulsed electromagnetic fields increased the anti-inflammatory effect of A 2 A and A 3 adenosine receptors in human T/C-28a2 chondrocytes and hFOB 1.19 osteoblasts. (rndsystems.com)

Attenuation of adverse effects of noise induced hearing loss on adult neurogenesis and memory in rats by intervention with Adenosine A2A receptor agonist. (harvard.edu)
BFx and intact rats were then given oral ALM, the benzodiazepine agonist zolpidem (ZOL) or vehicle (VEH) at lights-out. (sri.com)
BF adenosine (ADO), γ-amino-butyric acid (GABA), and glutamate levels were then determined via microdialysis from intact, freely behaving rats following oral ALM, ZOL or VEH. (sri.com)

Hypokalemia may result from either corticosteroid use or beta-agonist use. (medscape.com)

Beta-agonists, corticosteroids, and theophylline are mainstays in the treatment of status asthmaticus. (medscape.com)
theophylline decreases effects of adenosine by pharmacodynamic antagonism. (medscape.com)
Theophylline or Caffeine Adenosine receptor agonist poisoning. (standardofcare.com)

Adenosine Receptor Agonist HE-NECA Enhances Antithrombotic Activities of Cangrelor and Prasugrel in vivo by Decreasing Fibrinogen Density in Thrombus - By Polak et al. (wearecellix.com)
The animals received an A2A selective agonist, HE-NECA, and the P2Y12 inhibitor cangrelor. (wearecellix.com)
Effect of fluoxetine and adenosine receptor NECA agonist on G alpha q/11 protein of C6 glioma cells. (nel.edu)
Kovárů H, Kováru F, Lisá V. Effect of fluoxetine and adenosine receptor NECA agonist on G alpha q/11 protein of C6 glioma cells. (nel.edu)
Effect of fluoxetine or adenosine receptor NECA agonist on G-proteins of C6 glioma cells or NK immunocytes. (nel.edu)
Kovárů H, Kovaru F, Ondráčkova P, Lisá V, Fiserová A. Effect of fluoxetine or adenosine receptor NECA agonist on G-proteins of C6 glioma cells or NK immunocytes. (nel.edu)

Pharmacologically, indacaterol is a nearly full β 2 -agonist with a high intrinsic efficacy and, unlike partial agonists, it does not exhibit antagonistic behaviour in the presence of isoprenaline 6 . (ersjournals.com)

These results demonstrate that, in the magnocellular preoptic nucleus and substantia innominata region of the basal forebrain, adenosine inhibits both cholinergic neurons and a subset of noncholinergic neurons. (nih.gov)

Allosteric Modulation of Adenosine A2A Receptors as a New Therapeutic Avenue. (harvard.edu)
Probe dependence of allosteric enhancers on the binding affinity of adenosine A1 -receptor agonists at rat and human A1 -receptors measured using NanoBRET. (hellobio.com)

Enhancing endogenous adenosine A2A receptor signaling induces slow-wave sleep without affecting body temperature and cardiovascular function. (harvard.edu)

Aims: Neladenoson bialanate is a partial adenosine A1 receptor agonist with demonstrated beneficial effects on cardiac function in animal models. (unimib.it)
This technology includes A1AR-selective agonists which are full or partial agonists of the A1AR and are being considered for treatment of various conditions: seizures, stroke, diabetes, pain, cardio-protection and arrhythmias. (nih.gov)

In the basal forebrain, adenosine accumulates during wakefulness and, when locally applied, suppresses neuronal activity and promotes sleep. (nih.gov)

Database of Adenosine Receptor Agonist pharmaceutical products listed on drugs-library.com. (drugs-library.com)

This initial interaction (platelet adhesion) sets the stage for other adhesive reactions that allow the platelets to interact with other agonists in the vicinity of vessel injury, such as adenosine 5'-diphosphate (ADP), subendothelial collagen, and thrombin. (medscape.com)

Their natural ligand is adenosine, a purine metabolite in plasma, which hydrolyses adenosine monophosphate. (wearecellix.com)

Simultaneous application of an adenosine receptor agonist intensified the inhibitory effect of P2Y12 on platelet aggregation. (wearecellix.com)
Adenylate cyclase is inhibited by agonists of adenylate cyclase inhibitory G ( G i )-protein-coupled receptors. (wikipedia.org)

Extracellular Adenosine Stimulates Vacuolar ATPase-Dependent Proton Secretion in Medullary Intercalated Cells. (harvard.edu)
Adenosine A2A receptor agonist, polydeoxyribonucleotide (PDRN), suppresses the secretion of pro-inflammatory cytokines and exhibits anti-inflammatory effect. (iasp-pain.org)

Dr. Jacobson and his group have identified a compound MRS5474 as a potent small- molecule A1R agonist with exceptional drug-like properties. (grantome.com)

Adenosine is an important antiinflammatory molecule in tissue inflammation, and adenosine 2A receptor (A2AR) agonists protect kidneys from IRI through their actions on leukocytes. (jci.org)
Adenosine A2A receptor agonist polydeoxyribonucleotide ameliorates short-term memory impairment by suppressing cerebral ischemia-induced inflammation via MAPK pathway. (iasp-pain.org)

Insufficient hepatic O 2 in animal and human studies has been shown to elicit a hepatorenal reflex in response to increased hepatic adenosine, resulting in the stimulation of renal as well as muscle sympathetic nerve activity and activating the renin angiotensin system. (surgicalneurologyint.com)

2-Cl-IB-MECA is a high affinity and extremely selective A 3 adenosine receptor agonist (K i = 0.33 nM). (rndsystems.com)

To characterize the mode of action of AR agonists on platelet aggregation during primary hemostasis, they used a model of in vitro thrombus formation under flow conditions. (wearecellix.com)

Kappa-opioid (KOP) receptor agonists exhibit analgesic effects without activating reward pathways. (acs.org)
Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. (rndsystems.com)

Inhibition of LPS-induced neutrophil ROS production by various adenosine receptor agonists. (avma.org)
Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. (rndsystems.com)

Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. (rndsystems.com)

Concentration of cAMP in equine neutrophils induced by 5 adenosine A 2A receptor agonists (A) and effects of ZM241385 and MRS1706 on ATL313-induced accumulation of cAMP (B). Each point represents the mean ± SEM of 3 replicates. (avma.org)
Furthermore, they also showed that increased expression of homer1a is a final common pathway mediating the antidepressant effects of different antidepressant treatments including the A1R agonist. (grantome.com)
The A1R agonist MRS5474 induced a rapid antidepressant effects in animal models of transgenic mice with intraperitoneal (IP) administration. (grantome.com)
Adenosine A1 receptors (A1R) play a key role in neuroprotection and enhanced AA1R function has shown antidepressant effects in preclinical and clinical studies. (grantome.com)
Moreover, void of "well-known" cardiovascular side effects of classical A1R agonists , TSG showcased its great potential for stroke treatment . (bvsalud.org)
A1AR agonists are also being explored for antidepressant, antianxiety, and other neuropsychiatric effects, due to their presynaptic action to decrease the release of excitatory amino acids in the brain. (nih.gov)
However, peripheral cardiovascular side effects have prevented the introduction of A1AR agonist for treating disorders of the central nervous system (CNS). (nih.gov)
Blocking the H-current with ZD7288 (20 microM) abolished adenosine effects on these neurons. (nih.gov)
green tea decreases effects of adenosine by unspecified interaction mechanism. (medscape.com)
hawthorn increases effects of adenosine by pharmacodynamic synergism. (medscape.com)
nicotine inhaled increases effects of adenosine by unknown mechanism. (medscape.com)
All doses were well tolerated with a good safety profile and were not associated with consistent or clinically relevant effects on systemic β-agonist mediated events 7 - 10 . (ersjournals.com)
studies have shown that the R- and S-enantiomers of racemic albuterol, a β 2 -adrenergic receptor agonist used in asthma treatment, have differential effects on the contractile properties of airway smooth muscle. (scirp.org)

Inhibition of erythroblast growth and fetal hemoglobin production by ribofuranose-substituted adenosine derivatives. (rndsystems.com)

The research by the team at Warwick, together with colleagues at the University of Cambridge, University of Bern, Monash University, Coventry University and industrial collaborators, is published in Nature Communications in a paper entitled "Selective activation of G?ob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression. (sciencedaily.com)

dipyridamole increases levels of adenosine by decreasing metabolism. (medscape.com)
Hepatic fructose metabolism rapidly consumes ATP resulting in increased adenosine production and hyperuricemia as well as elevated renin release and sympathetic activity. (surgicalneurologyint.com)

Professor Graham Ladds, co-principal investigator on the project, from the University of Cambridge, said: "This is an amazing story looking at agonist bias for a GPCR. (sciencedaily.com)

Receptor in Ischemic Stroke: Neuroprotection by Tetrahydroxy Stilbene Glycoside as an Agonist. (bvsalud.org)
Adenosine A1 receptor (A1R) activation could ameliorate ischemic injury , representing a very tempting target for stroke treatment . (bvsalud.org)
A1AR agonists are highly neuroprotective in ischemic and epileptic models. (nih.gov)

Exhibits high selectivity over the Na + -independent adenosine transporter. (rndsystems.com)
2-Substitution of N 6 -benzyladenosine-5'-uronamides enhances selectivity for A 3 adenosine receptors. (rndsystems.com)

The goal of this project is to develop MRS5474, a potent and orally bioavailable A1R agonist for the treatment of depression. (grantome.com)
A P₂-purinergic receptor agonist that acts as a potent insulin secretagogue. (merckmillipore.com)

Adenosine limits the therapeutic effectiveness of anti-CTLA4 mAb in a mouse melanoma model. (rndsystems.com)

The authors concluded that chronic administration of A2A agonist could be considered a potential component of dual antithrombotic therapy. (wearecellix.com)
Development of an Adenosine A1 Receptor agonist, MRS5474 for the treatment of chronic depression Project Summary Depression is a common mental disorder, which can be chronic or recurrent, markedly tarnishing a person?s ability to function in their normal life. (grantome.com)
Indacaterol is a β 2 -agonist bronchodilator in development for the treatment of asthma and chronic obstructive pulmonary disease (COPD). (ersjournals.com)

Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (harvard.edu)

In this study, we showed that mice with A2AR-deficient DCs are more susceptible to kidney IRI and are not protected from injury by A2AR agonists. (jci.org)
In addition, administration of DCs treated ex vivo with an A2AR agonist protected the kidneys of WT mice from IRI by suppressing NKT production of IFN-γ and by regulating DC costimulatory molecules that are important for NKT cell activation. (jci.org)
A 2A R agonist ATL313 (10 ng/kg/min, osmotic mini-pump, s.c.) was administered to mice 24 hours prior to kidney IRI surgery. (jci.org)
In particular, sleep deprivation upregulates adenosine A1 receptors (A1R) in mice and humans. (grantome.com)

In the first group adenosine, via activation of postsynaptic A1 receptors, reduced spontaneous firing via inhibition of the hyperpolarization-activated cation current. (nih.gov)

2′-dAdo is used in comparison studies of the functions of adenosine analogues on various biological processes. (sigmaaldrich.com)

We used whole-cell patch-clamp recordings in in vitro rat brain slices to investigate the effect of adenosine on identified cholinergic and noncholinergic neurons of the magnocellular preoptic nucleus and substantia innominata. (nih.gov)

This graph shows the total number of publications written about "Adenosine A2 Receptor Agonists" by people in Harvard Catalyst Profiles by year, and whether "Adenosine A2 Receptor Agonists" was a major or minor topic of these publication. (harvard.edu)
Below are the most recent publications written about "Adenosine A2 Receptor Agonists" by people in Profiles. (harvard.edu)

Results are reported as the percentage of radioligand binding without addition of an agonist. (avma.org)
HB7813(30 nM) binding to live CHO cells expressing adenosine A3 receptors. (hellobio.com)

A2AR agonists had no effect on DC antigen presentation or on Tregs. (jci.org)

The Global Initiative for Asthma guidelines recognise the role of long-acting β 2 -agonists (LABAs) for the optimal treatment of moderate-to-severe persistent asthma 1 . (ersjournals.com)
The availability of a once-daily β 2 -agonist could be expected to improve the treatment of asthma by providing patients with greater convenience and sustained bronchodilation. (ersjournals.com)

Inhaled β 2 -adrenoceptor agonists are the most effective bronchodilators for the management of asthma 1 . (ersjournals.com)

Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R. (rndsystems.com)

Anatomy8

Organisms9

Chemicals and Drugs111

Analytical, Diagnostic and Therapeutic Techniques and Equipment2

Phenomena and Processes13

Information Science1

Cyclic5

Triphosphate4

Receptor antagonist6

Signaling pathway2

Selective adenosine2

Antagonists1

Regadenoson7

Receptors in human1

Rats3

Beta-agonist1

Theophylline3

NECA6

Efficacy1

Inhibits1

Allosteric2

Induces1

Partial2

Basal forebrain1

Drugs1

Diphosphate1

Monophosphate1

Inhibitory2

Secretion2

Compound1

Inflammation2

Renal1

Affinity1

Primary hemostasis1

Pathways2

Neutrophil2

Suppresses1

Effects13

Derivatives1

Cardiorespiratory1

Metabolism2

GPCR1

Ischemic3

Selectivity2

Potent2

Therapeutic1

Chronic3

Activate1

Mice4

Inhibition1

Biological processes1

Vitro1

Profiles2

Binding2

Effect1

Treatment2

Asthma1

Activation1