Adenosine a2 receptor agonists. Medical search. Frequent questions

Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused mainly on the role of adenosine receptors in the heart, and led to several randomized controlled trials using these receptor antagonists to treat bradyasystolic arrest. (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)
Antagonists of P2 receptors counteracted the enhancing effects of ATP, suggesting that HS costimulates neutrophils by means of P2 receptor activation. (escholarship.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)
The depressive ramifications of N6-cyclopentyladenosine, a detailed analog of CHA, are reversed by extremely A1-selective antagonists such as for example CPT, indicating that A1 receptors triggered by N6-cycloalkyladenosines subserve behavioral major depression (Bruns 1988). (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)
The role of adenosine and the adenosine A1, A3, A2A and A2B receptors was studied by using adenosine deaminase and the selective antagonists DPCPX (1 μM), MRS 1191(1 μM), ZM241385 (1 μM) and MRS1754 (1 μM). (sun.ac.za)
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)
These preliminary data raise the possibility that adenosine antagonists may affect cocaine-dependent and non-dependent subjects differently. (omicsonline.org)
Medications that bind to and block dopamine receptors are called dopamine antagonists. (parkinsonsinfoclub.com)
Antagonists of the Adenosine Diphosphate (ADP) receptor, P2Y12, may inhibit platelet aggregation as a result of stimulation with arachidonic acid (AA). (org.pk)
2 Antagonists of Adenosine Diphosphate (ADP) receptor P2Y12 may block the P2Y12-dependent pathway of platelet aggregation and sufficiently inhibit platelet aggregation resulting from stimulation with arachidonic acid (AA). (org.pk)
The question is: what is the effect of different P2Y12 receptor antagonists on mean maximum aggregation ratios (MAR%) in response to AA in patients receiving conventional dosages of aspirin? (org.pk)

The encoded protein (the A2A receptor) is abundant in basal ganglia, vasculature, T lymphocytes, and platelets and it is a major target of caffeine, which is a competitive antagonist of this protein. (wikipedia.org)
The contractile response in SHR was abolished by A1 adenosine receptor antagonist N6- endonorbornan-2-yl-9-methyladenine (N-0861). (uncg.edu)
A2 adenosine receptor antagonist 3 7-dimethyl-1-proparglyxanthine (DMPX) did not a ect the contraction response of adenosine analogues. (uncg.edu)
Gamma-butyrolactone antagonism of the picrotoxin receptor: comparison of a pure antagonist and a mixed antagonist/inverse agonist. (aspetjournals.org)
However, the wake-promoting effects of modafinil, unlike those of amphetamine[Rx] , were not antagonized by the dopamine receptor antagonist haloperidol[Rx] in rats. (illnesshacker.com)
Co-administering potent P2Y12 receptor antagonist Ticagrelor with aspirin reduces the rate of death from vascular causes, myocardial infarction, or stroke as compared with Clopidogrel, while it is also associated with increased non-coronary artery bypass grafting (CABG) and non-procedure-related major bleeding after 30 days. (org.pk)
3-5 The more potent P2Y12 receptor antagonist Ticagrelor used alone may result in a consistent and full platelet inhibition, and that little further platelet inhibition is achieved by the addition of aspirin as compared with Clopidogrel. (org.pk)

Platelet-rich plasma (PRP) or isolated cells prepared from the blood of healthy, adult humans were treated with bedaquiline (0.625-10 μg/ml), followed by activation with adenosine 5'-diphosphate (ADP), thrombin or the thromboxane A2 receptor agonist (U46619). (up.ac.za)
a component of adenosine triphosphate and adenosine diphosphate. (adxs.org)
RESULTS: Fresh PLTs responded to the dual agonists arachidonic acid and adenosine diphosphate (ADP) to aggregate and produce thromboxane A2, and in both the PLT surface markers P-selectin and GPIIb-IIIa increased and GPIb decreased after stimulation. (umassmed.edu)
Via this mechanism, platelet aggregation is inhibited in response to various stimuli such as platelet activating factor (PAF), collagen and adenosine diphosphate (ADP). (guidelinecentral.com)
7 AA (2 mg/ ml) and adenosine diphosphate (ADP, 50 µmol/L) were used as agonists. (org.pk)

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)

This inhibition results in an increase in local concentrations of adenosine which acts on the platelet A 2 -receptor thereby stimulating platelet adenylate cyclase and increasing platelet cyclic-3',5'-adenosine monophosphate (cAMP) levels. (guidelinecentral.com)
Although the exact mechanism by which adenosine receptor activation relaxes vascular smooth muscle is not known, there is evidence to support both inhibition of the slow inward calcium current reducing calcium uptake, and activation of adenylate cyclase through A2 receptors in smooth muscle cells. (globalrph.com)

Adenosine receptors are closely associated with dopamine receptors and form heteromer s with them. (adxs.org)
Regulation of responsiveness at D2 dopamine receptors by receptor desensitization and adenylyl cyclase sensitization. (aspetjournals.org)

BACKGROUND: Studies have been performed on human fresh, liquid-preserved, and cryopreserved platelets (PLTs) to assess PLT-adhesive surface receptors, PLT membrane procoagulant activity, PLT aggregation, and thromboxane production. (umassmed.edu)
STUDY DESIGN AND METHODS: In both human and baboon fresh and lyophilized PLTs, aggregation response and PLT production of thromboxane A2 were measured after stimulation, and PLT surface markers P-selectin, glycoprotein (GP) Ib, GPIIb-IIIa, and factor (F) V were measured before and after stimulation. (umassmed.edu)
Characterization of a thromboxane A2/prostaglandin H2 receptor in guinea pig lung membranes using a radioiodinated thromboxane mimetic. (aspetjournals.org)

The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. (wikipedia.org)

Allosteric Modulation of Adenosine A2A Receptors as a New Therapeutic Avenue. (harvard.edu)
High resolution crystal structure of Adenosine A2 receptor (AA2AR) in complex with agonist UK-432097 makes possible rational design of small molecules specifically targeting C5' substitutions of the agonist ribose ring, making possible more high affinity and subtype selective binding and potentially ligand specific modulation of adenosine receptor function. (nih.gov)
High resolution crystal structure makes possible rational design of small molecules specifically targeting C5' substitutions of the agonist ribose ring, making possible more high affinity and subtype selective binding and potentially ligand specific modulation of adenosine receptor function. (nih.gov)
2- Modulation of adenosine and/or dopamine signaling/metabolism in insulin-sensitive tissues to ameliorate glucose metabolism and tissue function in metabolic diseases. (unl.pt)
Although metabotropic glutamate receptor (mGluR) modulation has been studied extensively in neurons, it has not been investigated in astrocytes. (jneurosci.org)
Unlike the mGluR-kainate interaction, which required a pretreatment with an mGluR agonist and was insensitive to pertussis toxin (PTx), the mGluR modulation of 5HT actions was rapid and was blocked by PTx. (jneurosci.org)
These data suggest that glutamate, acting at several metabotropic receptors expressed by astrocytes, could modulate glial activity evoked by neurotransmitters and thereby influence the ongoing modulation of neurons by astrocytes. (jneurosci.org)

Hence, it would appear that A1- and A2-selective adenosine agonists possess different central depressant results, which may be potentiative. (thetechnoant.info)
The fairly high strength of NECA could possibly be because of a synergism between central A1 and A2receptor activation by this non-selective agonist. (thetechnoant.info)
This technology includes adenosine receptor binding compounds which could potentially be used for development of more selective and safe treatment of cardiovascular, psychiatric and neurodegenerative disorders. (nih.gov)
This technology presents novel rationally designed small molecule compounds capable of selective binding to adenosine receptor (subtypes A2a, A1, A2b and A3) and inducing effector-biased downstream signaling. (nih.gov)

In hypothalamic neurons, modulators such as neuropeptide Y (NPY) and adenosine depress glutamatergic transmission by either a pertussis toxin (PTx)-sensitive G-protein-coupled pathway or by inhibition of voltage-activated calcium channels (VACCs). (jneurosci.org)

Adenosine deaminase treatment abolished the suppressive effect of HS, indicating that HS inhibits neutrophils through adenosine generation. (escholarship.org)
Once inside the cell, adenosine is rapidly phosphorylated by adenosine kinase to adenosine monophosphate, or deaminated by adenosine deaminase to inosine. (globalrph.com)

CD39 limits P2X7 receptor inflammatory signaling and attenuates sepsis-induced liver injury. (harvard.edu)

This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices, as well as an extracellular N-terminus and an intracellular C-terminus. (wikipedia.org)
The activity of the encoded protein, a G protein-coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase, which induce synthesis of intracellular cAMP. (wikipedia.org)
The A2A receptor binds with the Gs protein at the intracellular site of the receptor. (wikipedia.org)
Abundant extracellular adenosine can then bind to the A2A receptor resulting in a Gs-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e. (wikipedia.org)
The intracellular uptake of adenosine is mediated by a specific transmembrane nucleoside transport system. (globalrph.com)
These intracellular metabolites of adenosine are not vasoactive. (globalrph.com)

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)

The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). (wikipedia.org)
Thrombin cleaves its G-protein-linked seven-transmembrane domain receptor, thereby releasing a 41-aa peptide and generating a new amino terminus that acts as a tethered ligand for the receptor. (umassmed.edu)

Extracellular Adenosine Stimulates Vacuolar ATPase-Dependent Proton Secretion in Medullary Intercalated Cells. (harvard.edu)
Extracellular adenosine gathers in response to cellular stress and breakdown through interactions with hypoxia induced HIF-1α. (wikipedia.org)
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)
Extracellular stimuli that activate cell surface receptors modulate glucocorticoid actions via as yet unclear mechanisms. (rupress.org)

Enhancing endogenous adenosine A2A receptor signaling induces slow-wave sleep without affecting body temperature and cardiovascular function. (harvard.edu)
Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
Release of endogenous catecholamines and activation of the beta-adrenergic receptors (b-AR) have also been shown to be involved in ischaemic preconditioning. (sun.ac.za)

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)

A1 receptors can also inhibit calcium mineral fluxes (Cerbai 1988) and induce potassium fluxes (Belardinelli and Isenberg, 1983). (thetechnoant.info)
MCs express receptors for both estrogen and progesterone that induce degranulation upon binding. (frontiersin.org)

The gene encodes a protein which is one of several receptor subtypes for adenosine. (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)

Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (harvard.edu)
Peptides corresponding to the new amino terminal end of the proteolyzed seven-transmembrane domain thrombin receptor [TR42-55, SFLLRNPNDKYEPF, also known as TRAP (thrombin receptor-activating peptide)], previously have been demonstrated to activate the receptor. (umassmed.edu)
MCs can secrete nociceptor sensitizing and activating agents, such as serotonin, prostaglandins, histamine, and proteolytic enzymes that can also activate the pain-mediating transient receptor potential vanilloid channels. (frontiersin.org)
The molecular underpinnings common to and connecting these disorders are not known, but may include shared genetic risk factors ( 1 , 8 ), regulation of brain cations ( 9 , 10 ), or common receptor signaling events that activate pain ( 11 ), inflammation ( 12 ), or oxidative ( 13 ) pathways. (frontiersin.org)

The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, and Parkinson's disease. (wikipedia.org)
Suprachiasmatic nucleus (SCN) and cortical astrocytes showed striking differences in sensitivity to glutamate and to mGluR agonists, even after several weeks in culture. (jneurosci.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)

Here, we report that the guanine nucleotide-binding protein (G protein)-coupled receptor-activated WD-repeat Gβ interacts with the glucocorticoid receptor (GR), comigrates with it into the nucleus and suppresses GR-induced transactivation of the glucocorticoid-responsive genes. (rupress.org)

however, modafinil is inactive in other in vitro assay systems known to be responsive to á-adrenergic agonists, such as the rat vas deferens preparation. (illnesshacker.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)
1 Isolated aortic rings (endothelium-intact and -denuded) from spontaneously hypertensive (SHR) and Wistar-Kyoto (WKY) rats were used in this study to examine the vasoactive e ects of various adenosine analogues. (uncg.edu)
8 These data suggest that the contractile response to adenosine analogues in SHR aorta is probably mediated by free radicals which are generated through the increased cyclo-oxygenase ctivity occurring in the vascular endothelium of SHR but not the WKY rats. (uncg.edu)
Nevertheless, in similar research in rats, the 100- to 300-collapse greater strength of R-PIA in accordance with S-PIA is definitely more consonant using the participation of A1 receptors (Goldberg 1985). (thetechnoant.info)

Recent advances in our understanding of the role of histamine and its four receptors suggest new approaches which target the histamine receptors alone or as combination therapies to more efficiently combat pruritus and inflammation in atopic dermatitis. (springeropen.com)
With this review, we provide an overview on histamine and the expression of its four receptors on skin resident and nonresident cells. (springeropen.com)

In summary, the cleaved peptide of the seven-transmembrane domain TR (TR1-41) is a strong platelet agonist. (umassmed.edu)

A crystal structure of the A2A receptor bound with the agonist NECA and a G protein-mimic has been published in 2016 (PDB code: 5g53). (wikipedia.org)

Activator of protein kinase A (cyclic AMP agonist). (biolog.de)

Adenosine is thought to exert its pharmacological effects through activation of purine receptors (cell-surface A1 and A2 adenosine receptors). (globalrph.com)

In contrast, adenosine suppresses superoxide formation. (escholarship.org)

In addition, A2A receptor can suppress immune cells, thereby protecting tissue from inflammation. (wikipedia.org)

Adenosine is a potent vasodilator in most vascular beds, except in renal afferent arterioles and hepatic veins where it produces vasoconstriction. (globalrph.com)

Adenosine may also lessen vascular tone by modulating sympathetic neurotransmission. (globalrph.com)

3 A non-speciÂ®c adenosine receptor agonist 2-chloroadenosine (CAD) resulted in biphasic response with a small contraction at lower concentrations (1079 Â±1078 M) followed by a signiÂ®cant relaxation at higher concentration in endothelium-intact SHR tissues suggesting presence of both A1 and A2 adenosine receptors in SHR aorta. (uncg.edu)

Normally, the transient nicotinic impact was absent since just muscarinic receptors had been activated. (californiaehealth.org)

Receptor-mediated tobacco toxicity: alterations of the NF-kappaB expression and activity downstream of alpha7 nicotinic receptor in oral keratinocytes. (famri.org)

The protective effects of this phenomenon have been demonstrated to be mediated by release of autocoids such as adenosine, opioids and bradykinin. (sun.ac.za)
Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors. (illnesshacker.com)

Though adenosine has been extensively studied as a primary chemical scaffold for adenosine receptor agonists, very little structure activity data exist for C5' substitution. (nih.gov)

the respective roles of the A1-, A2-, A3-adenosine receptors as well as the involvement of the PI3-K/PKB/Akt and ERKp44/p42 signal transduction pathways, in the cardioprotective phenomemon of -adrenergic preconditioning and (iv) the contribution of the mitochondrial KATP channels (mKATP), reactive oxygen species and NO to the mechanism of -AR-induced cardioprotection. (sun.ac.za)

Anatomy13

Organisms10

Diseases1

Chemicals and Drugs201

Analytical, Diagnostic and Therapeutic Techniques and Equipment9

Psychiatry and Psychology2

Phenomena and Processes18

Disciplines and Occupations1

Health Care1

Antagonists13

Antagonist7

Diphosphate5

Activation of A2 adenosine1

Adenylate cyclase2

Dopamine receptors2

Thromboxane3

Role of adenosine1

Modulation7

Selective4

Inhibition1

Deaminase2

P2X71

Intracellular6

Antagonism1

Ligand2

Extracellular4

Endogenous3

Binds1

Induce2

Subtypes1

Striatum1

Activate4

Glutamate2

Monophosphate1

Protein-coupled receptor1

Vitro1

Rats4

Histamine2

Seven transmembrane1

NECA1

Cyclic1

Pharmacological1

Suppresses1

Inflammation1

Potent1

Vascular1

Tissues1

Transient1

Expression1

Effects2

Extensively1

Roles1