Myocardial adenosine a2a receptors adenosine a2 receptor antagonists. Medical search. Frequent questions

Stimulation of the A1 receptor has a myocardial depressant effect by decreasing the conduction of electrical impulses and suppressing pacemaker cell function, resulting in a decrease in heart rate. (wikipedia.org)

Through this mechanism, the increased level of adenosine after sleep deprivation could affect the light sensitivity of the circadian clock. (adxs.org)

A1 receptors are also present in smooth muscle throughout the vascular system. (wikipedia.org)
Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. (wikipedia.org)

citation needed] Caffeine, as well as theophylline, has been found to antagonize both A1 and A2A receptors in the brain. (wikipedia.org)
Theophylline and caffeine are nonselective adenosine antagonists that are used to stimulate respiration in premature infants. (wikipedia.org)

However, in altered cardiac function, such as hypoperfusion caused by hypotension, heart attack or cardiac arrest caused by nonperfusing bradycardias, adenosine has a negative effect on physiological functioning by preventing necessary compensatory increases in heart rate and blood pressure that attempt to maintain cerebral perfusion. (wikipedia.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)

the mechanism of punicalagin on ventricular remodeling (VR) after acute myocardial infarction (AMI) remains unclear. (bvsalud.org)

Thus, it may prove more advantageous to use selective A1 antagonists to help reduce adenosine-induced brain injury. (wikipedia.org)

The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. (wikipedia.org)
Adenosine is found in almost all body cells. (adxs.org)

This effect on the A1 receptor also explains why there is a brief moment of cardiac standstill when adenosine is administered as a rapid IV push during cardiac resuscitation. (wikipedia.org)

The development of potent and selective agonists and antagonists of adenosine receptors (ARs) has been a target of medicinal chemistry research for several decades, and recently the US Food and Drug Administration has approved Lexiscan, an adenosine derivative substituted at the 2 position, for use as a pharmacologic stress agent in radionuclide myocardial perfusion imaging. (nih.gov)
Currently, some other adenosine A(2A) receptor (A(2A)AR) agonists and antagonists are undergoing preclinical testing and clinical trials. (nih.gov)
Highlights on the development of A(2A) adenosine receptor agonists and antagonists. (nih.gov)
1. Modulation of insulin release by adenosine A1 receptor agonists and antagonists in INS-1 cells: the possible contribution of 86Rb+ efflux and 45Ca2+ uptake. (nih.gov)
6. Adenosine A2A receptor agonists inhibit lipopolysaccharide-induced production of tumor necrosis factor-alpha by equine monocytes. (nih.gov)
14. Repeated administration of selective adenosine A1 and A2 receptor agonists in the spontaneously hypertensive rat: tolerance develops to A1-mediated hemodynamic effects. (nih.gov)
According to the invention, "adenosine-receptor-selective ligands" are substances which bind selectively to one or more subtypes of the adenosine receptors, thus either mimicking the action of adenosine (adenosine agonists) or blocking its action (adenosine antagonists). (allindianpatents.com)

However, in altered cardiac function, such as hypoperfusion caused by hypotension, heart attack or cardiac arrest caused by nonperfusing bradycardias, adenosine has a negative effect on physiological functioning by preventing necessary compensatory increases in heart rate and blood pressure that attempt to maintain cerebral perfusion. (wikipedia.org)

15. Theophylline inhibits the differentiation of human monocyte into dendritic cell potentially via adenosine receptor antagonism. (nih.gov)
The administration of the xanthines has been proposed as a non-dopaminergic strategy for neuroprotection in PD and the mechanisms of protection have been associated with antagonism of adenosine A2A receptors and Monoamine Oxidase type B (MAO-B) inhibition. (benthamscience.com)

Thus, it may prove more advantageous to use selective A1 antagonists to help reduce adenosine-induced brain injury. (wikipedia.org)
According to their receptor selectivity, adenosine-receptor-selective ligands can be divided into different categories, for example ligands which bind selectively to the Al or A2 receptors of adenosine and in the case of the latter also, for example, those which bind selectively to the A2a or the A2b receptors of adenosine. (allindianpatents.com)

The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand. (wikipedia.org)
The endogenous levels of the purine nucleoside, adenosine, increase significantly following cardiovascular events. (frontiersin.org)
Adenosine, a nucleoside consisting of adenine and D-ribose, is an endogenous factor having cell-protective activity, in particular under cell-damaging conditions with limited oxygen and substrate supply, such as, for example, in the case of ischaemia in various organs (for example heart and-brain). (allindianpatents.com)

8. Adenosine opposes thrombin-induced inhibition of intercellular calcium wave in corneal endothelial cells. (nih.gov)
19. Adenosine A1 receptor-mediated inhibition of dopamine release from rat striatal slices is modulated by D1 dopamine receptors. (nih.gov)
20. A(2b) receptor mediates adenosine inhibition of taurine efflux from pituicytes. (nih.gov)
In the case of the binding of adenosine to the A2a or A2b receptors, the intracellular cAMP is increased via activation of the membrane-bound adenylate cyclase, whereas binding of adenosine to A1 or A3 receptors results in a decrease of the intracellular cAMP concentration via inhibition of adenylate cyclase. (allindianpatents.com)

This receptor has an inhibitory function on most of the tissues in which it rests. (wikipedia.org)
9. A1 receptors mediate adenosine inhibitory effects in mouse ileum via activation of potassium channels. (nih.gov)

10. K(ATP)-channel activation: effects on myocardial recovery from ischaemia and role in the cardioprotective response to adenosine A1-receptor stimulation. (nih.gov)
Adenosine exerts cardioprotective, neuromodulatory, and immunosuppressive effects by activating plasma membrane-bound P1 receptors that are widely expressed in the cardiovascular system. (frontiersin.org)

2. A1 and A2 adenosine receptor activation inhibits and stimulates renin secretion of rat renal cortical slices. (nih.gov)
Thus, it is known, for example, that adenosine inhibits platelet aggregation and increases the blood supply to the coronary arteries. (allindianpatents.com)

Under normoxic conditions, the concentration of free adenosine in the extracellular space is very low. (allindianpatents.com)
Spinal cord injury (SCI) is an inflammatory condition, and excessive adenosine triphosphate (ATP) is released into the extracellular space, which can be catabolized into adenosine by CD73. (biomedcentral.com)

The purine nucleoside adenosine was first identified in 1929 when Drury and Szent-Gyorgyi successfully extracted a rhythm-influencing adenylic substance from the mammalian heart and other tissues ( Drury and Szent-Gyorgyi, 1929 ). (frontiersin.org)

Also possible are adenosine receptor ligands which bind selectively to a plurality of subtypes of the adenosine receptors, for example ligands which bind selectively to the Al and the A2, but not to the A3 receptors of adenosine. (allindianpatents.com)

7. Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes. (nih.gov)
The abovementioned receptor selectivity can be determined by the effect of the substances on cell lines which, after stable transfection with the corresponding cDNA, express the receptor subtypes in question (see the publication M.E. Olah, H. Ren, J. Ostrowski, K.A. Jacobson, G.L. Stiles, "Cloning, expression, and characterization of the unique bovine Al adenosine receptor. (allindianpatents.com)

Stimulation of the A1 receptor has a myocardial depressant effect by decreasing the conduction of electrical impulses and suppressing pacemaker cell function, resulting in a decrease in heart rate. (wikipedia.org)

5. The role of intraspinal adenosine A1 receptors in sympathetic regulation. (nih.gov)

Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. (wikipedia.org)
Following Burnstock's pioneering work on the role of ATP-sensitive P2 purinoceptors, its metabolite adenosine soon became recognized as an extracellular signalling molecule through the activation of plasma membrane-bound P1 receptors family that are expressed in every organ systems in the body. (frontiersin.org)

The aim of these actions of adenosine is to increase the oxygen supply of the affected organs and/or to reduce the metabolism of these organs in order to adjust the metabolism of the organ to the blood supply of the organ under ischaemic or hypoxic conditions. (allindianpatents.com)

However, under ischaemic or hypoxic conditions, the extracellular concentration of adenosine in the affected organs is increased dramatically. (allindianpatents.com)
CD73+ hucMSC-EVs reduced concentration of ATP and promoted the level of adenosine. (biomedcentral.com)

Here, we provide a comprehensive and up-to-date critical review about the main therapeutic advantages of tuning adenosine signalling pathways in HFpEF, without discounting their side effects and how these can be seized. (frontiersin.org)
Only in 1972, Geoff Burnstock (born: May 10, 1929, died: June 2, 2020) coined the term purinergic signalling referring to the extracellular effects of adenosine 5′-triphosphate (ATP). (frontiersin.org)
Effects of CD73+ hucMSC-EVs on hydrolyzing ATP into adenosine were detected. (biomedcentral.com)

A1 receptors are also present in smooth muscle throughout the vascular system. (wikipedia.org)

The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. (wikipedia.org)

Furthermore, A2aR and A 2b R inhibitors and A2bR knockdown cells were used to investigate the activated adenosine receptor. (biomedcentral.com)

This makes adenosine a useful medication for treating and diagnosing tachyarrhythmias, or excessively fast heart rates. (wikipedia.org)

11. Adenosine receptors involved in modulation of noradrenaline release in isolated rat tail artery. (nih.gov)

The actions of these adenosine receptors are mediated intracellularly by the messenger cAMP. (allindianpatents.com)
In vitro experiments, CD73+ hucMSC-EVs increased macrophages/microglia M2:M1 polarization, activated adenosine 2b receptor (A2bR), and then promoted cAMP/PKA signaling pathway. (biomedcentral.com)

Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. (wikipedia.org)

17. Neutrophil adherence to endothelium is enhanced via adenosine A1 receptors and inhibited via adenosine A2 receptors. (nih.gov)

Anatomy8

Organisms9

Diseases1

Chemicals and Drugs147

Analytical, Diagnostic and Therapeutic Techniques and Equipment9

Psychiatry and Psychology1

Phenomena and Processes12

Depressant1

Deprivation1

Vascular2

Caffeine2

Increases2

Mechanism1

Reduce1

Found2

Effect1

Agonists7

Perfusion1

Antagonism2

Selective2

Endogenous3

Inhibition4

Inhibitory2

Cardioprotective2

Inhibits2

Extracellular space2

Nucleoside1

Ligands1

Characterization2

Stimulation1

Regulation1

Activation2

Oxygen1

Concentration2

Effects3

Present1

Body1

Cells1

Heart1

Release1

CAMP2

Blood1

Inhibited via1