• Notable adenosine A2A receptor antagonists include caffeine, theophylline and istradefylline. (wikipedia.org)
  • the A2 receptor antagonists 8-(p-sulfophenyl)theophylline, 3,7-dimethyl-1-(2-propynyl)xanthine, 1,3,7-trimethyl-8-(3-chlorostyryl)xanthine, and 3-propylxanthine, but not A1 and A3 receptor antagonists, decreased the suppressive effect of HS, indicating that HS suppresses neutrophils via A2 receptor activation. (escholarship.org)
  • 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)
  • Due to indirect modulation of dopamine transmission, adenosine receptor antagonists may be useful in either treating cocaine use or improving disrupted cognitive-behavioral functions associated with chronic cocaine use. (omicsonline.org)
  • To compare and contrast the stimulant effects of adenosine antagonism to direct dopamine stimulation, we administered 150 mg and 300 mg caffeine, 20 mg amphetamine, and placebo to cocaine-dependent vs. healthy control subjects, matched on moderate caffeine use. (omicsonline.org)
  • Medications that bind to and block dopamine receptors are called dopamine antagonists. (parkinsonsinfoclub.com)
  • The presence of heterodimeric complexes has progressed in suggesting new ways to regulate neuronal activity by targeting the A2A receptor. (wikipedia.org)
  • Adenosine deaminase treatment abolished the suppressive effect of HS, indicating that HS inhibits neutrophils through adenosine generation. (escholarship.org)
  • A2A receptor antagonists may prevent hepatic cirrhosis, and pentoxifylline may inhibit phosphodiesterase and provide renal protection. (wikipedia.org)
  • The A2A receptor antagonists may be used for treatment of attention deficit hyperactivity disorder (ADHD), because of the receptors ability to regulate neurotransmission in the basal ganglia and cortex, particularly dopaminergic and glutamatergic signaling. (wikipedia.org)
  • The adenosine system is closely linked to the dopaminergic system. (adxs.org)
  • Recently, selective A2A receptor antagonists are used in treatment of diseases such as Parkinson's disease, ischemia, and multiple sclerosis. (wikipedia.org)
  • Recent evidence has shown that in cases of generalized ischemia after hemorrhagic shock, the effectiveness of melatonin in improving liver function depends on the melatonin receptor (40). (ectrx.org)
  • The process of ischemia and reperfusion is known to cause inducible nitric oxide synthase induction and activation, and there is evidence that interleukin (IL)-1β (46), IL-1 receptor (47), and IL-1 receptor along with nuclear factor-kappa beta (48) may have an important role in that induction. (ectrx.org)
  • We have previously shown that hypertonic stress (HS) can suppress chemoattractant-induced neutrophil responses via cyclic adenosine monophosphate and enhance these responses through p38 mitogen-activated protein kinase (MAPK) activation. (escholarship.org)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • Here, we report that HS dose-dependently releases adenosine 5'-triphosphate (ATP) from neutrophils and that extracellular ATP is rapidly converted to adenosine or activates p38 MAPK and enhances N-formyl-methionyl-lencyl-phenylalanine-induced superoxide formation. (escholarship.org)
  • The blockade of A2A receptors has potentially shown to be protective in several tumor models, through pharmacological inhibition or genetic deletion. (wikipedia.org)
  • Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. (guidetopharmacology.org)
  • Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. (guidetopharmacology.org)
  • 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)
  • In recent studies, the consumption of caffeine-containing beverages and a certain non-xanthine A2A receptor antagonist appear to possibly have some protective effects from Alzheimer's disease. (wikipedia.org)
  • The stimulant properties of caffeine and various analogs were correlated with the blockade of adenosine receptors. (wikipedia.org)
  • Most of the therapeutic applications are connected to agonists, but the main focus with antagonists are diseases connected to motor skills, learning and memory, for example Parkinson's and Alzheimer's. (wikipedia.org)
  • Trial results indicated that the viability of A2A receptor antagonists have potential advantages over the current standard treatments for Parkinson's disease. (wikipedia.org)
  • Similar to other G protein-coupled receptors, A2A receptors form both homo- and heterodimers. (wikipedia.org)
  • The protein expression of nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing 3 (NLRP3), apoptosis speck-like protein (ASC), caspase-1, gasdermin D (GSDMD), and GSDMD-N, the mRNA expression of NLRP3, caspase-1, GSDMD, interleukin-1ß (IL-1ß) and IL-18 were evaluated. (bvsalud.org)
  • Through this mechanism, the increased level of adenosine after sleep deprivation could affect the light sensitivity of the circadian clock. (adxs.org)
  • His seminal contributions, documented in more than 490 publications and 27 book chapters, encompass key developments such as mechanism-based PK-PD models, which incorporate biologically realistic considerations such as understanding of target site distribution and receptor theory. (eacpt.org)
  • Selective A2A receptor antagonists have shown to be beneficial for enhancing the therapeutic effects of L-DOPA and reducing dyskinesia from long-term L-DOPA treatment. (wikipedia.org)
  • Furthermore, a series of important implications on inflammation and the immune system that are induced by the activity of cannabinoid receptors stimulated by the delta-9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD) have been noticed. (encyclopedia.pub)
  • Antagonists of P2 receptors counteracted the enhancing effects of ATP, suggesting that HS costimulates neutrophils by means of P2 receptor activation. (escholarship.org)
  • These preliminary data raise the possibility that adenosine antagonists may affect cocaine-dependent and non-dependent subjects differently. (omicsonline.org)
  • Adenosine is found in almost all body cells. (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)
  • Adenosine A2A receptor locations in the body could help us to understand the possible therapeutic applications in the future. (wikipedia.org)
  • We conclude that hypertonic stress regulates neutrophil function via a single molecule (ATP) and its metabolite (adenosine), using positive- and negative-feedback mechanisms through the activation of P2 and A2 receptors, respectively. (escholarship.org)
  • Various neuropeptides play important roles in the regulation of feeding behavior, including relaxin-3 (RLN3), which stimulates food intake in rats through the activation of the relaxin-family peptide-3 receptor (RXFP3). (jneurosci.org)
  • Among other things, adenosine is used for autoregulation in the event of an imminent lack of energy in the cell (e.g. when the cell's performance is overloaded or when there is a lack of oxygen): If the ATP content in a cell drops, more adenosine is produced as a hydrolysis product. (adxs.org)