Adenosine A2A receptor

5-HT1D receptor

5-HT1D receptor

Adenosine A1 receptor

Adenosine

Adenozinski A2A receptor

Molecular and epigenetic mechanisms of alcoholism

Cysteinyl leukotriene receptor 2

Prostaglandin receptor

പ്രോസ്റ്റാഗ്ലാൻഡിൻ EP3 റിസപ്റ്റർ - വിക്കിപീഡിയ

GPCR16

• This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. (wikipedia.org)
• The adenosine A1 receptor (Adora1) is a G-protein coupled receptor (GPCR) that is involved in maintaining glucose homeostasis and regulating glucagon secretion ( 11 , 12 ). (diabetesjournals.org)
• The multicomponent modular nature of G protein-coupled receptor (GPCR) systems provides cells with numerous potential combinations by which to transduce signals. (aspetjournals.org)
• A typical cell appears to express a dozen or so different GPCR genes (of which nearly a thousand exist in the human genome), several different combinations of G protein subunits and multiple isoforms of effector molecules that can be activated by each type of G protein. (aspetjournals.org)
• The current dogma is that high-affinity protein-protein interactions determine the identity of the G protein with which a particular GPCR interacts and, in turn, dictates the biochemical pathways that are activated by that receptor. (aspetjournals.org)
• Various GPCR and receptor tyrosine kinases have been localized in caveolae or caveolin-rich cellular fractions along with many of the molecules critical for transducing the signals initiated by these types of receptors: e.g. (aspetjournals.org)
• Some GPCR are enriched or excluded from caveolae whereas certain GPCR reportedly translocate out of or into caveolae upon activation by an agonist. (aspetjournals.org)
• The adenosine A 1 GPCR (A 1 AR) is a major therapeutic target for cardioprotection, but current agents acting on the receptor are clinically limited for this indication because of on-target bradycardia as a serious adverse effect. (pnas.org)
• He discovered a novel signalling mechanism for G-Protein Coupled Receptors (GPCR) in synapses in brain ( Nature ). (edu.au)
• His team is investigating the molecular mechanisms responsible for tolerance at the µ-opioid receptor, action-related learning and plasticity in the cortico-striatal network, and studying novel GPCR mechanisms to treat neural hyper-excitation in chronic pain. (edu.au)
• There is also lack of knowledge on the stoichiometry of the participating receptor protomers in GPCR heteroreceptor complexes. (springer.com)
• The GPCR complexes can also contain ion channel receptors, receptor tyrosine kinases (RTKs), sets of G protein interacting proteins and/or transmitter transporters increasing their integrative capability (Borroto-Escuela et al. (springer.com)
• DiscoverX is proud to be the only outsourced GPCR service provider that can offer complete compound characterization by providing multiple, functional readouts for the same receptor. (discoverx.com)
• Access to the same GPCR target in different technology formats enables identification of G-protein or Arrestin biased ligands. (discoverx.com)
• The PTGER4 gene is located on human chromosome 5p13.1 at position p13.1 (i.e. 5p13.1), contains 7 exons, and codes for a G protein coupled receptor (GPCR) of the rhodopsin-like receptor family, Subfamily A14 (see rhodopsin-like receptors#Subfamily A14 ). (orange.com)
• Characterizing the role of any GPCR involves the identification of both the activating ligand and the activated G protein. (biomedcentral.com)

Antagonist16

• 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)
• 1. A method of enhancing an immune response in a host, comprising administering to the host an A.sub.2a receptor antagonist in combination or alternation with a checkpoint inhibitor. (patents.com)
• Consistent with a role for CXCR7 in cell survival and adhesion, a specific, high affinity small molecule antagonist to CXCR7 impedes in vivo tumor growth in animal models, validating this new receptor as a target for development of novel cancer therapeutics. (rupress.org)
• CADO inhibition of barium currents was also sensitive to the A1 antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX). (gotomydoctor.com)
• In competition with antagonist radioligand biphasic curves were observed for agonists. (biomedsearch.com)
• a ligand of M1 and M5, a ligand of M2 and M5, and a ligand of M3 and M5), but until both a selective agonist and a selective antagonist of the M5 receptor are developed this data must be considered merely theoretical. (wikidoc.org)
• 2014). "Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)-Selective M5 -Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe" . (wikidoc.org)
• Aki Y, Tomohiro A, Nishiyama A et al (1997) Effects of KW-3902, a selective and potent adenosine A1 receptor antagonist, on renal hemodynamics and urine formation in anesthetized dogs. (springer.com)
• In order to uncover the estrogen effects on adenosine receptor expression, estrogen-positive MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor subtypes were evaluated. (readbyqxmd.com)
• Estrogen-positive MCF-7 cells were treated with various concentrations of 17β estradiol (E2) as an estrogen agonist, and ICI 182,780 as an estrogen antagonist. (readbyqxmd.com)
• Bladder smooth muscle contraction was induced using acetylcholine (ACh, 10⁻⁴ M). The materials such as, atropine (a muscarinic receptor antagonist), U73122 (a phospholipase C inhibitor), DPCPX (an adenosine A1 receptor antagonist), udenafil (a PDE5 inhibitor), prazosin (an α₁-receptor antagonist), papaverine (a smooth muscle relaxant), verapamil (a calcium channel blocker), and chelerythrine (a protein kinase C inhibitor) were pre-treated in bladder smooth muscle. (bvsalud.org)
• Riccardin C (59) was identified as a LXRa agonist and a LXRp antagonist 148 unfortunately it exhibits. (americorpshealth.biz)
• The ATP-evoked Ca 2+ transients were present under the blockade of neuronal activity, but were inhibited by Ca 2+ store depletion and antagonism of the G protein coupled purinergic P2Y 1 receptor subtype-specific antagonist MRS2179. (biomedcentral.com)
• This anti-hyperalgesic impact involves vertebral 5-HT2A receptors and GABAergic interneurons since it is normally abolished with a 5-HT2A antagonist (M100907, 150 ng/rat, intrathecally) and a GABAA antagonist, (bicuculline, 3 g/rat, intrathecally). (immune-source.com)
• The present invention relates to novel biphenyl compounds having muscarinic receptor antagonist or anticholinergic activity. (google.com)
• However, even when administered by inhalation, a significant amount of the muscarinic receptor antagonist is often absorbed into the systemic circulation resulting in systemic side effects, such as dry mouth, mydriasis and cardiovascular side effects. (google.com)

GPCRs18

• 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)
• The concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). (pnas.org)
• G protein-coupled receptors (GPCRs) are the largest family of cell surface proteins and tractable drug targets ( 1 , 2 ). (pnas.org)
• GPCRs respond to various ligands extracellularly, such as amines, peptides, hydrophobic effectors, hormones, small proteins and volatiles, which allows the receptors to activate the G-proteins intracellularly. (europeanpharmaceuticalreview.com)
• Pharmacological agents that act at GPCRs can broadly be categorised into four main classes: agonists, inverse agonists, antagonists and allosteric modulators. (europeanpharmaceuticalreview.com)
• However, exploitation of the 3D structures of GPCRs is now preferable due to the elucidation of the structure of rhodopsin17, followed by those of the beta118, beta219, adrenergic, adenosine A2A20, dopamine D321, CXCR4 chemokine22, histamine H1 receptors23 and recently sphingosine 1-phosphate receptor24 and the M2 muscarinic acetylcholine receptor25. (europeanpharmaceuticalreview.com)
• Since G protein coupled receptors (GPCRs) are target of forty percent of clinically used drugs, here we discuss the newly identified cardioprotective agents that bind GPCRs of adrenalin, adenosine, melatonin, ghrelin, galanin, apelin, prokineticin and cannabidiol. (frontiersin.org)
• Adenosine is a purine nucleoside, responsible for the regulation of a wide range of physiological and pathophysiological conditions by binding with four G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B and A3 adenosine receptors (ARs). (eurekaselect.com)
• An approach to use multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors (GPCRs) was recently introduced. (biomedcentral.com)
• Involved in the activation of AKT1 upon stimulation by G-protein coupled receptors (GPCRs) ligands such as CXCL12, sphingosine 1-phosphate, and lysophosphatidic acid. (genecards.org)
• Plays a role in platelet activation signaling triggered by GPCRs, alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) and ITAM (immunoreceptor tyrosine-based activation motif)-bearing receptors such as GP6. (genecards.org)
• The cell-membrane G-protein coupled receptors (GPCRs) are one of the largest known superfamilies and are the main focus of intense pharmaceutical research due to their key role in cell physiology and disease. (biomedcentral.com)
• Cross-genome phylogenetic analyses were performed to identify eight major groups of GPCRs dividing them into 32 clusters of 371 human and 113 Drosophila proteins (excluding olfactory, taste and gustatory receptors) and reveal unexpected levels of evolutionary conservation across human and Drosophila GPCRs. (biomedcentral.com)
• Similarly, a group of Drosophila GPCRs (methuselah receptors), associated in aging, is not present in humans. (biomedcentral.com)
• Our analysis suggests ligand class association to 52 unknown Drosophila receptors and 95 unknown human GPCRs. (biomedcentral.com)
• Different GPCRs respond to a wide variety of different external stimuli (light, odorants, peptides, lipids, ions, nucleotides etc) and activate a number of different GTP binding proteins (G proteins), there by initiating a wide spectrum of intracellular responses. (biomedcentral.com)
• A majority of the identified GPCRs are with no known ligand specificity (orphan receptors), which presents a challenge for identifying their native ligands and defining their function. (biomedcentral.com)
• The physiological role of these receptors can be well understood by the identification of natural ligands, which further advance the design of pharmacologically active surrogate activators or inhibitors of the GPCRs that have defined native ligands. (biomedcentral.com)

Endogenous8

• 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)
• Since A1R agonists would be associated with severe cardiovascular effects, it was hypothesized that inhibitors of nucleoside equilibrative transporters, such as dipyridamole, by increasing the tonic A1R activation mediated by endogenous adenosine, could represent a new alternative therapeutic strategy for RLS. (frontiersin.org)
• In the presence of GTP all receptors were converted to a single low affinity state indicating functional coupling to endogenous G proteins. (biomedsearch.com)
• Binding of the endogenous ligand acetylcholine to the M 5 receptor triggers a number of cellular responses such as adenylate cyclase inhibition, phosphoinositide degradation, and potassium channel modulation. (wikidoc.org)
• Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
• The adenosine A1 receptor (A1R) is a key mediator of the neuroprotective effect by endogenous adenosine. (aspetjournals.org)
• Adenosine is an endogenous purine nucleoside that modulates a wide range of physiological functions ( 1 ). (jimmunol.org)
• 20. Henderson, G., McKnight, A.T. (1997) The orphan opioid receptor and its endogenous ligand-nociceptin/orphanin FQ. (pharmacologicalsciences.us)

Kinase16

• however, stimulation of this receptor is known to effectively decrease cyclic AMP levels and downregulate the activity of protein kinase A (PKA). (wikidoc.org)
• 1996). "Phosphorylation of human m1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 and protein kinase C. (wikidoc.org)
• These results indicate that regulatory events leading to desensitization, internalization, and recycling in a functional state of hDOR involve phosphorylation by a G protein-coupled receptor kinase, internalization via clathrin-coated vesicles, and dephosphorylation by acid phosphatases. (aspetjournals.org)
• have shown that desensitization was dependent on the activity of G protein-coupled receptor kinase (GRK) 2, a member of the GRK family. (aspetjournals.org)
• PIK3CB (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Beta) is a Protein Coding gene. (genecards.org)
• May have a role in insulin signaling as scaffolding protein in which the lipid kinase activity is not required. (genecards.org)
• 11. The method according to claim 5 wherein an adenylate kinase inhibitor, which prevents AMP from conversion into adenosine diphosphate (ADP) or adenosine triphosphate (ATP) is administered. (patentsencyclopedia.com)
• Therefore, the increased proteins concentrations result in a FLJ34064 rise in kinase activity of the CDK9/cyclin T1 complicated. (angiogenesis-blog.com)
• Palmitoylation of rPLD1 is not necessary for catalytic activity, since N-terminal truncation mutants lacking the first 168 or 319 amino acids exhibit high basal activity although they cannot be stimulated by protein kinase C (PKC). (embl-heidelberg.de)
• Activation of D 5 receptors is shown to promote expression of brain-derived neurotrophic factor and increase phosphorylation of protein kinase B in rat and mice prefrontal cortex neurons. (wikidoc.org)
• Included in these are PSD?95/Disk Huge/Zonula occludens-1 (PDZ) domains containing proteins from the membrane-associated guanylate kinase (MAGUK) family . (immune-source.com)
• ERK also plays a part in cell loss of life through the suppression of anti-apoptotic signaling molecule RAC- serine/threonine-protein kinase (34). (cancer-pictures.org)
• An orally available, small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. (blogspot.com)
• Upon oral administration, ASP3026 binds to and inhibits ALK tyrosine kinase, ALK fusion proteins and ALK point mutation variants. (blogspot.com)
• An orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (Pyk2), with potential antineoplastic activity. (blogspot.com)
• An orally available inhibitor of multiple kinases, including the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, the proto-oncogene SRC, and focal adhesion kinase (FAK), with potential antineoplastic activity. (blogspot.com)

Dopamine receptor9

• It is a main tenet of this essay that, in RLS, a single alteration in the adenosinergic system, downregulation of A1R, disrupts the adenosine-dopamine-glutamate balance uniquely controlled by adenosine and dopamine receptor heteromers in the striatum and also the A1R-mediated inhibitory control of glutamatergic neurotransmission in the cortex and other non-striatal brain areas, which altogether determine both PLMS and hyperarousal. (frontiersin.org)
• He contributed to the first cloning of the D2 dopamine receptor ( Nature ) and achieved the first expression of a mammalian voltage-gated potassium channel ( Science ), and first functional demonstration of its heteropolymerisation ( Neuron ). (edu.au)
• Through a reorganization of these heteroreceptor complexes upon chronic dopaminergic treatment a pathological and prolonged inhibition of D2R receptor protomer signaling can develop with motor inhibition and wearing off of the therapeutic effects of levodopa and dopamine receptor agonists. (springer.com)
• To investigate the role of A 2A adenosine receptors in adaptive responses to chronic intermittent dopamine receptor stimulation, we compared the behavioral sensitization elicited by repeated l -DOPA treatment in hemiparkinsonian wild-type (WT) and A 2A adenosine receptor knock-out (A 2A KO) mice. (jneurosci.org)
• Dopamine receptor D 5 , also known as D1BR , is a protein that in humans is encoded by the DRD5 gene . (wikidoc.org)
• D 5 receptor is a subtype of the dopamine receptor that has a 10-fold higher affinity for dopamine than the D 1 subtype. (wikidoc.org)
• D 5 receptor is expressed more widely in the CNS than its close structural homolog dopamine receptor D1 . (wikidoc.org)
• Dopamine receptor D 5 is exclusively expressed by large aspiny neurons in neostriatum of primates, which are typically cholinergic interneurons . (wikidoc.org)
• Polymorphisms in the DRD5 gene, which encodes dopamine receptor D 5 , have been suggested to play a role in the initiation of smoking. (wikidoc.org)

Effects of adenosine6

• Because of the effects of adenosine on AV node-dependent SVTs, adenosine is considered a class V antiarrhythmic agent. (wikipedia.org)
• The cardiovascular protective effects of adenosine have been described in recent years. (pnas.org)
• Effects of adenosine on tubular transport are most pronounced in the proximal tubule where the nucleoside stimulates NaCl reabsorption in the subnormal concentration range while inhibiting transport at elevated levels. (springer.com)
• Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
• Beach RE, Good DW (1992) Effects of adenosine on ion transport in rat medullary thick ascending limb. (springer.com)
• Functional effects of adenosine were investigated in proliferation-experiments with CD4 + T cells and specific inhibitors. (springer.com)

Glutamate7

• 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, drug addiction and Parkinson's disease. (wikipedia.org)
• Neurotransmission in the hippocampus is modulated variously through presynaptic metabotropic glutamate receptors (mGluRs). (jneurosci.org)
• Metabotropic glutamate receptors (mGluRs) have various modulatory functions on neuronal excitability, transmitter release, and synaptic plasticity in the CNS ( Pin and Duvoisin, 1995 ). (jneurosci.org)
• In detail, the synaptic channels are NMDA receptors, GABAA receptors, glutamate receptors of the neuromuscular junction, and presynaptic glutamate receptors of the kainate subtype as well as glycine receptors of the spinal chord. (uni-jena.de)
• There are various neurotransmitters that are involved in anxiety such as serotonin, glutamate, gamma-amino butyric acid, Cholecystokinnin, Adenosine etc. (ijpsr.com)
• Launch Chronic inflammatory discomfort and neuropathic discomfort share a number of common neuroplastic adjustments taking place in the spinal-cord, including changed ion channel appearance in dorsal main ganglion neurons, improved glutamate discharge and glutamate receptor function, aswell as glial cell activation . (immune-source.com)
• This was coupled with an increase in glutamate levels in the striatal tissues. (cancer-pictures.org)

Adenylyl9

• This is mediated via the A1 receptor, inhibiting adenylyl cyclase, reducing cAMP and so causing cell hyperpolarization by increasing K+ efflux via inward rectifier K+ channels, subsequently inhibiting Ca2+ current. (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)
• In this study all human subtypes were stably transfected into Chinese hamster ovary (CHO) cells in order to be able to study their pharmacological profile in an identical cellular background utilizing radioligand binding studies (A1, A2A, A3) or adenylyl cyclase activity assays (A2B). (biomedsearch.com)
• The relative potencies of agonists for the A2B adenosine receptor could only be tested by measurement of receptor-stimulated adenylyl cyclase activity. (biomedsearch.com)
• Although adenosine activates multiple receptor subtypes (A1, A2a, A2b, and A3 receptors), the adenylyl cyclase stimulatory A2a adenosine receptors (A2aARs) are regarded mainly as cardioprotective receptors ( 1 ). (pnas.org)
• Indirect evidence suggests that the adenylyl cyclase stimulatory A2b adenosine receptors (A2bARs) also affect vascular function ( 4 - 6 ). (pnas.org)
• a2-adrenergic receptors are associated with following except (A) Increase in phospholipase C activity (B) Increase in potassium channel conductance (C) Decrease in calcium channel conductance (D) Increase in adenylyl cyclase activity 86. (himpustak.com)
• The D 5 subtype is a G-protein coupled receptor , which promotes synthesis of cAMP by adenylyl cyclase via activation of Gα s/olf family of G proteins . (wikidoc.org)
• Both D 5 and D 1 subtypes activate adenylyl cyclase . (wikidoc.org)

Pharmacological9

• Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity. (wikipedia.org)
• The A1 subtype showed the typical pharmacological profile with 2-chloro-N6-cyclopentyladenosine (CCPA) as the agonist with the highest affinity and a marked stereoselectivity for the N6-phenylisopropyladenosine (PIA) diastereomers. (biomedsearch.com)
• Overall, the pharmacological characteristics of the human receptors are similar to other species with some species-specific characteristics. (biomedsearch.com)
• The CHO cells with stably transfected adenosine receptors provide an identical cellular background for such a pharmacological characterization. (biomedsearch.com)
• Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (eurekaselect.com)
• The renewed interest in the adenosine A 2B receptor (A2BR) subtype can be traced by studies in which the introduction of new genetic and chemical tools has widened the pharmacological and structural knowledge of this receptor as well as its potential therapeutic use in cancer and inflammation- or hypoxia-related pathologies. (physiology.org)
• Presently, most pharmacological agents for the treatment of allergic disease target receptors for inflammatory mediators. (aspetjournals.org)
• Although preliminary, these results indicate that purinergic receptors are putative pharmacological targets that should be further explored in future studies. (biomedcentral.com)
• Studies of the Pharmacological Properties of the Toxic Proteins Abrin and Ricin and on the «in vitro» Activity and their Conjugates with an Antimeloanoma Antibody 1082 Andersen Bjørg Marit (dr.med. (docplayer.net)

Purinergic receptors3

• Purinergic receptors are implicated in the pathogenesis of gastrointestinal disorders and are being explored as potential therapeutic targets. (readbyqxmd.com)
• While ATP primarily acts as a proinflammatory signal on purinergic P2 receptors, its degradation product adenosine signals through P1 purinergic receptors, mediating both anti- and proinflammatory effects depending on the receptor subtype. (physiology.org)
• Ulrich, H. Purinergic receptors in embryonic and adult neurogenesis. (eurekaselect.com)

Inhibitor4

• Here, we show that the expression of a potential glucagon inhibitor, the adenosine A1 receptor (Adora1), is gradually diminished in α-cells of NOD mice, autoantibody-positive (AA + ) and overtly type 1 diabetic (T1D) patients during the progression of disease. (diabetesjournals.org)
• CD73-derived adenosine acts as potent inhibitor of inflammation, and regulatory T cells (Treg) have been shown to express CD73 as a novel marker. (physiology.org)
• Treatment with pertussis toxin (PTX), an inhibitor of G(i)-protein, suppressed the increase in [Ca²⁺](i) evoked by S1P. (bvsalud.org)
• 12. The method according to claim 5 wherein an adenosine deaminase inhibitor which prevents the decomposition of adenosine, is administered. (patentsencyclopedia.com)

Phospholipase4

• As a result, stimulation of A1 and A3 subtypes in general results in neurotransmission through the inhibition of adenylate cyclase and phospholipase C , whereas stimulation of the A2 subtypes leads to enhanced neurotransmission. (axonmedchem.com)
• Cloning and direct G-protein regulation of phospholipase D from tobacco. (embl-heidelberg.de)
• Phospholipase D (PLD) and heterotrimeric G-proteins are involved in plant signal transduction pathways at the plasma membrane. (embl-heidelberg.de)
• It is suggested that these G protein-coupled receptors redundantly activate phospholipase C in basolateral amygdala . (wikidoc.org)

Suggest that adenosine3

• Additional studies suggest that adenosine induces apoptosis of human arterial smooth muscle cells, which is mediated via the A2bAR in a cAMP-dependent pathway ( 7 ). (pnas.org)
• In vitro studies using cultured human and mouse mast cells, and studies of mice lacking A 2B receptors, suggest that adenosine receptors, specifically the G s -coupled A 2A and A 2B receptors, might provide such a target. (aspetjournals.org)
• Recent observations suggest that adenosine is involved in the antinociceptive effect of amitriptyline. (bvsalud.org)

Nucleoside3

• Adenosine is a purine nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond. (wikipedia.org)
• Because adenosine production increases in hypoxia, the issue of a role of the nucleoside in the renal injury following ischemia reperfusion has been studied extensively. (springer.com)
• the purine nucleoside adenosine is involved in many physiological and pathophysiological events ( 35 ). (physiology.org)

Membrane19

• 4 CADO inhibition was predominantly voltage-dependent and sensitive to the sulphydryl- modifying reagent N-ethylmaleimide, implicating a membrane-delimited, Gi/o-coupled signal transduction pathway in the channel regulation. (gotomydoctor.com)
• Two additional dimensions must be incorporated into our conceptual models: 1) the compartmentation of receptors and effector molecules in subcellular compartments and microdomains of the plasma membrane, and 2) the movement, or translocation, of receptors between cellular compartments (trafficking). (aspetjournals.org)
• Caveolae differ biochemically from another specialized region of the plasma membrane implicated in receptor-trafficking, clathrin-coated pits. (aspetjournals.org)
• To fulfill these tasks in a regulated manner, the parietal cell is equipped with an exclusive collection of apical and basolateral ion transporter proteins that are exposed on the membrane whenever their functions are required (see e.g., review Ref. 45 ). (physiology.org)
• Globally, a collection of neural stimuli, efferent and afferent, endocrine and paracrine agents, acting directly at apical and basolateral membrane receptors/transporters of the parietal cell or acting indirectly through the other cells of the gastric mucosa, as well as mechanical and chemical stimuli participate in acid secretion physiology (e.g., see recent reviews in Refs. (physiology.org)
• The A 3 AR selective G2.5 dendrimer was also visualized binding the membrane of cells expressing the A 3 receptor but did not bind cells that did not express the receptor. (biomedcentral.com)
• In this study, we demonstrate that A1R activation leads to a sustained localization of regulator of G protein signaling 4 (RGS4) at the plasma membrane, a process that requires neurabin (a neural tissue-specific protein). (aspetjournals.org)
• The common aim of the five projects in project area A is to elaborate and/or optimize high-end light microscopy methods designed to learn more about the function of membrane receptors. (uni-jena.de)
• Black-lipid-membrane platform with diffusion suppression for confocal single-molecule FLIM-FRET analysis of gated membrane receptors and transporters. (uni-jena.de)
• Diffusion of membrane proteins in the BLM will be suppressed by an Annexin-V network for extended observation times. (uni-jena.de)
• This project will target specifically the development for a nanoscale and label-free structure-investigation of membrane receptors, potentially even more specific membrane receptor surfaces. (uni-jena.de)
• The neuronal surface membrane contains an abundance of proteins known as ion channels that allow small charged atoms to pass through from one side of the membrane to the other. (thefreelibrary.com)
• In addition, activation of the P2X7 receptor, present on immune cells, triggers membrane permeabilization to medium-sized molecules and thereby may permit the cellular exit of ATP ( 28 ). (physiology.org)
• Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as the primary receptors for one or more of the classical, naturally occurring prostanoids viz. (wikipedia.org)
• These kinases are important in signaling pathways involving receptors on the outer membrane of eukaryotic cells and are named for their catalytic subunit. (genecards.org)
• PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. (genecards.org)
• 5 Histamine acts on G-protein coupled receptors in the brain, with H1 and H2 receptors mainly exciting the postsynaptic membrane and H3 receptors suppressing the presynaptic release of histamine and other neurotransmitters. (asahq.org)
• Within a cell, D 5 receptors are found on the membrane of soma and proximal dendrites . (wikidoc.org)
• The membrane receptor megalin modulates proliferation and survival rates in melanoma cells - could it be a novel biomarker and therapeutic target in melanoma cancer? (health-articles.net)

Inhibition8

• 5 Using Ca2+ channel subtype-selective antagonists, CADO inhibition appeared to target multiple channel subtypes, with the inhibition of o-conotoxin GVIA-sensitive calcium channels being more prominent. (gotomydoctor.com)
• 6 Our results indicate that the anti-convulsant e ects CADO in the basolateral amygdala may be mediated, in part, by the A1 receptor-dependent inhibition of voltage gated calcium channels. (gotomydoctor.com)
• For example, the A1 adenosine receptor *Author for correspondence at: Department of Medical subtype is classically associated with the inhibition of Pharmacology and Toxicology, The Texas A&M Univ. (gotomydoctor.com)
• Here, using a panel of mice lacking various combinations of adenosine receptors, and mast cells derived from these animals, we show that adenosine receptor agonists provide an effective means of inhibition of mast cell degranulation and induction of cytokine production both in vitro and in vivo. (aspetjournals.org)
• We identify A 2B as the primary receptor limiting mast cell degranulation, whereas the combined activity of A 2A and A 2B is required for the inhibition of cytokine synthesis. (aspetjournals.org)
• Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
• When the G-protein was included in the PLD assay, a strong dosage-dependent inhibition of the PLD activity was observed. (embl-heidelberg.de)
• Inhibition of liver x receptor/retinoid X receptor-mediated transcription contributes to the proatherogenic effects of arsenic in macrophages in vitro. (pharmacogenomicsguide.com)

Neurons6

• We have utilized whole-cell voltage-clamp electrophysiology to examine the modulatory e ects of CADO and other adenosine receptor agonists on voltage-gated calcium channels in dissociated basolateral amygdala neurons. (gotomydoctor.com)
• 1987). Unlike A1 receptors, A2 adenosine receptors appear to couple to cholera toxin- Neurons were prepared from coronal brain slices of juvenile sensitive G proteins and can stimulate cyclic AMP male rats (*P17 ± P28) as previously described (McCool & accumulation. (gotomydoctor.com)
• His later research uncovered the mechanisms of plasticity of G-protein receptor coupling in neurons that are transforming thinking regarding opioid tolerance and ion channel plasticity in chronic pain states. (edu.au)
• The major adenosine receptor complexes in the striato-pallidal GABA neurons can be the A2AR-D2R and A2AR-D2R-mGluR5 receptor complexes, in which A2AR protomers and mGluR5 protomers can allosterically interact to inhibit D2R protomer signaling. (springer.com)
• 7 Both in vivo and in vitro studies have shown that the sedative action of some general anesthetics (pentobarbital and propofol) is mediated by γ-aminobutyric acid receptor type A on TMN histaminergic neurons. (asahq.org)
• In keeping with this hypothesis, we previously showed that disrupting the connections between vertebral 5-HT2A receptors and linked PDZ protein by an interfering peptide in a position to transduce into vertebral neurons after intrathecal shot, inhibited thermal and mechanised hyperalgesia and improved fluoxetine-induced analgesia . (immune-source.com)

Role of adenosine receptors2

• 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)
• Interestingly, evidence is growing for a certain role of adenosine receptors in the field of oncology . (axonmedchem.com)

Cellular5

• He leads a research team that studies cellular and molecular mechanisms in opioid receptor signaling in pain pathways, the biological basis of adaptations that produce chronic pain and drug dependence, and is Chief Investigator on a NHMRC Program grant involving preclinical development of novel pain therapeutics. (edu.au)
• Regulates the strength of adhesion of ITGA2B/ ITGB3 activated receptors necessary for the cellular transmission of contractile forces. (genecards.org)
• The evidences indicate a dual function of these receptors, depending on the microorganism and the cellular model involved. (biomedcentral.com)
• Members of this calcium-dependent phospholipid-binding protein family play a role in the regulation of cellular growth and in signal transduction pathways. (cancerindex.org)
• it is one of four identified EP receptors, the others being EP 1 , EP 2 , and EP 3 , all of which bind with and mediate cellular responses to PGE 2 and also, but generally with lesser affinity and responsiveness, certain other prostanoids (see Prostaglandin receptors ). (orange.com)

Superfamily2

• Adenosine A1 receptor (ADORA1, also known as A1AR) is one of four subtypes of adenosine receptors that belong to a superfamily of protein G-coupled receptors. (ptglab.com)
• ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. (blogspot.com)

Antagonists and allosteric modulators3

• This review provides an overview of the medicinal chemistry and therapeutic potential of various agonists/partial agonists, antagonists and allosteric modulators of A1 AR, with a particular emphasis on their current status and future perspectives in clinical settings. (eurekaselect.com)
• A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 AR, structure- activity relationships of A1 AR. (eurekaselect.com)
• A1 adenosine receptor agonists, antagonists, and allosteric modulators. (eurekaselect.com)

Potent6

• N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. (wikipedia.org)
• For A2A adenosine receptors CGS 21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadeno sine) and N-ethylcarboxamidoadenosine (NECA) were found to be the most potent agonists followed by R- and S-PIA with minor stereoselectivity. (biomedsearch.com)
• NECA was the most potent agonist with an EC50-value of 2.3 microM whereas all other compounds tested were active at concentrations in the high micromolar range. (biomedsearch.com)
• The N6-benzyl substituted derivatives of adenosine-5'-N-methyluronamide (MECA) turned out to be the most potent agonists. (biomedsearch.com)
• Allosteric enhancer of A1 AR is found to be potent for the treatment of neuropathic pain, culminating the side effects related to off-target tissue activation of A1 AR. (eurekaselect.com)
• Because adenosine has such potent effects on inflammation, modulators of adenosine signaling are being evaluated as potential therapeutic options for diseases that have an inflammatory component ( 8 ). (jimmunol.org)

Subunit7

• N-Methyl-D-aspartic acid (NMDA) receptors with neurotoxic activity were assessed for subunit NMDA receptor subtype 2B. (bvsalud.org)
• CysLTR2, similar to CysLTR1, is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq alpha subunit and/or Ga subunit of its coupled G protein, depending or the cell type. (wikipedia.org)
• The encoded protein is the catalytic subunit for PI3Kbeta (PI3KB). (genecards.org)
• When bound to PGE 2 or other of its agonists, it mobilizes G proteins containing the Gs alpha subunit (i.e. (orange.com)
• The alpha-subunit of a G-protein from tobacco was isolated in a similar way. (embl-heidelberg.de)
• These results provide a first indication for a direct regulation of PLDalpha by a heterotrimeric G-protein alpha-subunit in plants. (embl-heidelberg.de)
• It was previously reported that Stargazin (STG) enhances the surface expression of AMPA receptors, controls receptor gating and slows channel desensitization as an auxiliary subunit of the receptors. (readbyqxmd.com)

Allosteric modulators1

• Ampakines are a class of AMPA receptor positive allosteric modulators that modify rates of transmitter binding, channel activity and desensitization parameters. (readbyqxmd.com)

Heterotrimeric G protei2

• 1997), the long-term decrease in receptors belong to the heptahelical family of receptors seizure threshold brought about by repeated electrical and are coupled to heterotrimeric G proteins. (gotomydoctor.com)
• [email protected] inhibitory' Gi/o heterotrimeric G proteins. (gotomydoctor.com)

Adrenergic7

• Dobutamine differs from dopamine in that (A) It does not activate peripheral dopaminergic receptors (B) It does not activate adrenergic ß receptors (C) It causes pronounced tachycardia (D) It has good blood-brain barrier penetrability 89. (himpustak.com)
• Continuous exposure of ctecholaminesensitive cells and tissues to adrenergic agonists causes a progressive diminition in their capacity to respond, this phenomenon is called as (A) Refractoriness (B) Desensitization (C) Tachyphylaxis (D) All of the above 91. (himpustak.com)
• Low doses of α-adrenergic agonists constrict veins and may often shift blood from the Vu to the Vs, subsequently increasing the venous return and cardiac output, whereas higher drug doses constrict arteries and usually decrease cardiac output. (springer.com)
• It has been shown that M 1 -Muscarinic receptors cooperate with D 5 receptors and beta-2 adrenergic receptors to consolidate cued fear memory. (wikidoc.org)
• It performs its action by being released into the synaptic cleft, where it acts on adrenergic receptors, followed by the signal termination, either by degradation of norepinephrine or by uptake by surrounding cells. (worldlibrary.net)
• Beta1-adrenergic receptor polymorphisms, QTc interval and occurrence of symptoms in type 1 of long QT syndrome. (pharmacogenomicsguide.com)
• Polymorphisms of the beta-1 and beta-2 adrenergic receptors in Polish patients with idiopathic dilated cardiomyopathy. (pharmacogenomicsguide.com)

Opioid receptor3

• 2004). "Candidate genes for anorexia nervosa in the 1p33-36 linkage region: serotonin 1D and delta opioid receptor loci exhibit significant association to anorexia nervosa. (wikipedia.org)
• Currently, Professor Christie continues to study opioid receptor regulation in pain and analgesia, in particular the processes driving the development of opioid tolerance. (edu.au)
• Internalization, recycling, and resensitization of the human δ-opioid receptor (hDOR) were studied in the neuroblastoma cell line SK-N-BE, endogenously expressing this receptor. (aspetjournals.org)

ADORA2A1

• Adenozinski A 2A receptor ( ADORA2A ) je adenozinski receptor . (wikipedia.org)

Chemokine4

• It is generally believed that SDF-1 mediates these many disparate processes via a single cell surface receptor known as chemokine receptor 4 (CXCR4). (rupress.org)
• SDF-1 has been thought to mediate all of these functions exclusively via a single cell surface receptor known as chemokine receptor 4 (CXCR4) ( 6 ). (rupress.org)
• It is now classified as a chemokine receptor able to bind the chemokines CXCL12 /SDF-1 and CXCL11 . (wikidoc.org)
• We also observe that members of human chemokine receptors, involved in immune response, and most of nucleotide-lipid receptors (except opsins) do not have counterparts in Drosophila . (biomedcentral.com)

Phosphorylation2

• CDK9 regulates the androgen receptor through S81 phosphorylation which is an essential part of regulating not merely its transcriptional activity, also for prostate cancers cell development . (angiogenesis-blog.com)
• EP 4 also interacts with Prostaglandin E receptor 4-associated protein (EPRAP) to inhibit phosphorylation of the proteasome protein, p105 , thereby suppressing a cells ability to activate nuclear factor kappa B , a transcription factor that controls genes coding for cytokines and other elements that regulate inflammation, cell growth, and cell survival (see NF-κB#Structure ). (orange.com)

Modulation2

• Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses. (patents.com)
• The differential expression of these various proteins allows modulation of signals at many levels, resulting in messages that are customized for a specific cell type. (aspetjournals.org)

Activation26

• 1997). This anticonvulsant activity of CADO highly integrative role in the sense/memory-response is dose-dependent and blocked by ca eine, suggesting that pathway and is believed to occupy a pivotal position in activation of adenosine heptahelical receptors in the the regulation of fear and anxiety. (gotomydoctor.com)
• In fact, adenosine receptor activation can subtypes of P1 receptors can be distinguished from one even prevent the acquisition of amygdala kindling (Abdul- another by receptor pharmacology or by examination of the signal transduction pathways to which the individual receptors couple. (gotomydoctor.com)
• For instance, adenosine inhibits the proliferation of murine VSMC via activation of the A2bAR ( 4 ). (pnas.org)
• Adenosine receptors also play a major role in several inflammation-associated processes by inhibiting immune activation and preventing excessive tissue damage. (pnas.org)
• However, treatment with full A1 AR agonists has been associated with numerous challenges like cardiovascular side effects, off-target activation as well as desensitization of A1 AR leading to tachyphylaxis. (eurekaselect.com)
• In addition, both acid production and radioligand binding of adenosine analogs to isolated cell membranes were potently blocked by selective A2BR antagonists, whereas ligands for A 1 , A 2A , and A 3 adenosine receptors failed to abolish activation. (physiology.org)
• The primary stimulatory processes are considered to be of histaminergic nature via G s -coupled H 2 receptor activation and of cholinergic nature via activation of G q -coupled muscarinic receptors or receptors for gastrin ( 69 ), but other actors are also on the stage. (physiology.org)
• In contrast to nitric oxide and similar to angiotensin II, sympathoadrenergic stimulation by phenylephrine or by baroreflex activation only slightly enhanced MR [ A2 ]. (uni-freiburg.de)
• 1994). "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. (wikidoc.org)
• This rapid breakdown results in the activation of a multiplicity of receptor subtypes, which can mediate physiological processes such as proliferation, differentiation, migration, and cell death . (thefreelibrary.com)
• Adenosine-dependent regulation of renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors (A 1 AR, A 2A AR, A 2B AR, A 3 AR). (springer.com)
• Moreover, adenosine protects against renal ischemic reperfusion injury by the anti-inflammatory effect of enhancing the activity of regulatory T cell and by attenuating the inflammatory injury produced by neutrophils via A 2 AR activation. (springer.com)
• Al-Mashhadi RH, Skott O, Vanhoutte PM et al (2009) Activation of A(2) adenosine receptors dilates cortical efferent arterioles in mouse. (springer.com)
• Awad AS, Huang L, Ye H et al (2006) Adenosine A2A receptor activation attenuates inflammation and injury in diabetic nephropathy. (springer.com)
• Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
• A2B adenosine receptor (A2B AR) activation induces Gs-dependent cyclic AMP accumulation. (readbyqxmd.com)
• However, genetic deletion of CD73 in mice is associated with a proinflammatory phenotype and CD73-derived adenosine appears to be quantitatively sufficient to inhibit platelet activation, and leukocyte adhesion to the vascular endothelium in vivo ( 15 ) by acting through the A2aR ( 47 ). (physiology.org)
• Aside from its action on the endothelium, A2aR agonists inhibit T-cell activation through increasing cAMP levels, which acts immunosuppressive ( 39 ). (physiology.org)
• In addition, A 2B receptor knockout mice showed increased splenic apoptosis and phosphatase and tensin homolog activation and decreased Akt activation. (jimmunol.org)
• These results indicate that A 2B receptor activation may offer a new therapeutic approach for the management of sepsis. (jimmunol.org)
• CDK9 proteins amounts were found to improve during differentiation and activation of B lymphocytes: In storage and in turned on individual B cells the appearance of CDK9 is normally increased compared to na?ve and quiescent cells, respectively . (angiogenesis-blog.com)
• EP 4 is classified as a relaxant type of prostaglandin receptor based on its ability, upon activation, to relax the contraction of certain smooth muscle preparations and smooth muscle-containing tissues that have been pre-contracted by stimulation. (orange.com)
• EP 4 activation of G proteins also activate PI3K/AKT/mTOR , ERK , and p38 MARK pathways. (orange.com)
• 8,9 The γ-aminobutyric acid-mediated anesthetic agents that act on γ-aminobutyric acid receptor type A may decrease TMN neuronal firing and histamine release, thus reducing histamine's excitation of the cortical activation circuitry. (asahq.org)
• Second, we investigated the histamine receptor subtype responsible for electroencephalographic activation. (asahq.org)
• These characteristics implied that intercellular Ca 2+ signalling originated from the release of Ca 2+ from internal stores, triggered by the activation of P2Y 1 receptors. (biomedcentral.com)

Tyrosine kinases1

• May also act downstream receptor tyrosine kinases. (genecards.org)

RESPONSES3

• A.sub.2a receptor antagonists in particular are provided to enhance immune responses by reducing T-cell mediated tolerance to antigenic stimuli and agonists are provided to enhance effectiveness of immunosuppressive agents. (patents.com)
• The small Secretin-receptor family is structurally and functionally diverse and includes receptors for polypeptide hormones, and for Drosophila proteins that regulate stress responses and longevity 7 . (europeanpharmaceuticalreview.com)
• Furthermore, they raise the possibility that the maladaptive dyskinetic responses to chronic l -DOPA treatment in Parkinson's disease may be attenuated by A 2A receptor inactivation. (jneurosci.org)

Inhibits1

• In summary, CD73-derived adenosine tonically inhibits active NF-κB in CD4 + T-cells, thereby modulating the release of a broad spectrum of proinflammatory cytokines and chemokines. (physiology.org)

Prostanoid receptors5

• All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor family except for the Prostaglandin DP2 receptor which is more closely related in amino acid sequence and functionality to chemotactic factor receptors such as the receptors for C5a and leukotriene B4 . (wikipedia.org)
• Prostanoid receptors bind and respond principally to metabolites of the straight chain polyunsaturated fatty acid (PUFA), arachidonic acid . (wikipedia.org)
• Typically, prostanoid receptors show somewhat less affinity and responsiveness to the 1 and 3 series prostanoids. (wikipedia.org)
• There are 9 established prostanoid receptors. (wikipedia.org)
• In many respects, EP 4 actions resemble those of another type of another relaxant prostanoid receptor, EP 2 but differs from the contractile prostanoid receptors, EP 1 and EP 3 receptors which mobilize G proteins containing the Gα q - Gβγ complex . (orange.com)

19942

• Baranowski RL, Westenfelder C (1994) Estimation of renal interstitial adenosine and purine metabolites by microdialysis. (springer.com)
• 16. Mills, A., Duggan, M.J. (1994) Orphan seven transmembrane domain receptors: Reversing pharmacology. (pharmacologicalsciences.us)

Activate1

• They differ from other 7-TM proteins in their ability to activate guanine-nucleotide binding proteins or β-arrestin and so initiate a signalling cascade. (europeanpharmaceuticalreview.com)

Regulation7

• Adenosine also plays a role in regulation of blood flow to various organs through vasodilation. (wikipedia.org)
• 1991). However, direct regulation studies outlined below, infusion of the non-selective of postsynaptic processes by amygdala adenosine receptors adenosine receptor agonist 2-chloroadenosine (CADO) has not been examined. (gotomydoctor.com)
• This agonist-triggered internalization was reversible for a treatment not exceeding 1 h and became irreversible for prolonged treatment (4 h), leading probably to the degradation and/or down-regulation of the receptor. (aspetjournals.org)
• and 2) the reduction of the receptor number at the cell surface, either by sequestration (internalization), which involves the receptor endocytosis, or by down-regulation which includes the receptor sequestration and degradation. (aspetjournals.org)
• Thus, A1R and RGS4 each likely interact with one neurabin molecule in a neurabin homo-oligomer to form a ternary complex, representing a novel mode of regulation of G protein-coupled receptor signaling by scaffolding proteins. (aspetjournals.org)
• Regulation of the LDL receptor in parenchymal and non-parenchymal cell 1087 Olsvik Ørjan (dr.philos. (docplayer.net)
• D 5 receptors are expressed in kidneys and are involved in regulation of sodium excretion. (wikidoc.org)

Molecule1

• The G-protein coupled neurotensin receptor type 1 (NTSR-1) is expressed in bacteria, purified and labeled with two fluorophores for single-molecule Förster resonance energy transfer (smFRET). (uni-jena.de)

Stimulation2

• Besides, 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. (axonmedchem.com)
• Downregulation of P2X7 and upregulation of CD73 in Treg after antigenic stimulation may be an important mechanism to maintain the ability of Treg to generate immunosuppressive adenosine. (physiology.org)

Inhibitory2

• anxiety have implicated the basolateral complex (BLA), as Previous work has demonstrated that adenosine receptors being centrally important in both the acquisition and may act presynaptically in the amygdala to inhibit both expression of fear/apprehension-related behaviours (re- excitatory and inhibitory transmission (Heinbockel & viewed in Davis, 1992). (gotomydoctor.com)
• Different control proteins did not exhibit this inhibitory effect. (embl-heidelberg.de)

Triphosphate1

• Derivatives of adenosine are widely found in nature and play an important role in biochemical processes, such as energy transfer-as adenosine triphosphate (ATP) and adenosine diphosphate (ADP)-as well as in signal transduction as cyclic adenosine monophosphate (cAMP). (wikipedia.org)

Physiological3

• In particular, A1 AR is ubiquitously present, mediating a variety of physiological processes throughout the body, thus represents a promising drug target for the management of various pathological conditions. (eurekaselect.com)
• Adenosine-a physiological or pathophysiological agent? (eurekaselect.com)
• Such analyses will prove valuable for identifying the natural ligands of Drosophila and human orphan receptors that can lead to a better understanding of physiological and pathological roles of these receptors. (biomedcentral.com)

Inflammatory8

• In addition, A2A receptor can negatively regulate overreactive immune cells, thereby protecting tissues from collateral inflammatory damage. (wikipedia.org)
• In this study, we studied the role of A 2B adenosine receptors in regulating the mortality and inflammatory response of mice following polymicrobial sepsis. (jimmunol.org)
• Although there are four adenosine receptor (AR) subtypes, the A2AAR is both highly expressed on lymphocytes and known as a prime mediator of adenosine's anti-inflammatory effects. (jimmunol.org)
• 13. The method according to claim 9, wherein the disease or disorder is tissue trauma, a reperfusion injury resulting from myocardial infarction or stroke, cancer or cancer metastasis or an inflammatory disease and the administering of the recombinant protein CD73 or cytokine or another factor or a combination thereof is started immediately the patient is brought to care. (patentsencyclopedia.com)
• We Bexarotene also discovered a decreased appearance of 5-HT2A receptors in the dorsal spinal-cord of inflamed pets which could not really end up being rescued by TAT-2ASCV shot, while the quantity of PSD-95 had not been suffering from inflammatory discomfort. (immune-source.com)
• This research reveals a job of the connections between 5-HT2A receptors and PDZ protein in the pathophysiological pathways of inflammatory discomfort and opens brand-new perspectives in its control because of substances disrupting 5-HT2A receptor/PDZ proteins connections. (immune-source.com)
• We hypothesized that having less efficiency of SSRIs in inflammatory persistent pain circumstances might reveal alteration of 5-HT2A receptor-operated signalling. (immune-source.com)
• The A3 adenosine receptor (A3AR) is the only adenosine subtype overexpressed in inflammatory and cancer cells. (bvsalud.org)

Effect of adenosine2

• Little, however, is known about the effect of adenosine on myeloid cells. (springer.com)
• Considering that tumor associated macrophages (TAM) and myeloid-derived suppressor cells (MDSC) constitute up to 20 % of OvCA tissue, we investigated the effect of adenosine on myeloid cells and explored a possible contribution of myeloid cells to adenosine generation in vitro and ex vivo. (springer.com)

Selective agonists3

• 2 CADO, adenosine, and the A1 subtype-selective agonists N6-(L-2-Phenylisopropyl)adenosine (R- PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA) reversibly modulated whole cell Ba2+ currents in a concentration-dependent fashion. (gotomydoctor.com)
• No highly selective agonists or antagonists for the M 5 receptor have been discovered as of 2018, but several non-selective muscarinic agonists and antagonists have significant affinity for M 5 . (wikidoc.org)
• The apparent liabilities of LXRa p dual agonists coupled with data garnered from LXR KO studies have led to a strong emphasis on the identification of LXR subtype selective agonists suitable for pharmacologic evaluation. (americorpshealth.biz)

Neuronal3

• eN is transiently associated with synapses during synaptogenesis, however in adult brain it is more glial than neuronal enzyme. (eurekaselect.com)
• Ulrich, H. New insights into purinergic receptor signaling in neuronal differentiation, neuroprotection, and brain disorders. (eurekaselect.com)
• It really CD109 is well known that BDNF includes a neuroprotective impact by avoiding the neuronal loss of life induced by metabolic and oxidative tension and excitotoxicity, and modulating calcium mineral reactions to AMPA and NMDA receptors, which might be 1197160-78-3 from the MAPK signaling pathway. (cancer-pictures.org)

Seven transmembrane1

• Several allosteric ligands to these receptors have been identified and these appear to bind within the seven transmembrane region. (europeanpharmaceuticalreview.com)

Affinity3

• The notion of xanthine-insensitivity of the A3 receptor should be dropped at least for the human receptor as xanthines with submicromolar affinity were found. (biomedsearch.com)
• Attachment of neutral amide-linked chains or thiourea-containing chains preserved the moderate affinity and efficacy at the A 1 AR subtype, but there was no selectivity for the A 3 AR. (biomedcentral.com)
• In the present paper, a PLD cDNA clone was isolated from tobacco, expressed as a GST fusion in bacteria, and the recombinant protein was purified by glutathione affinity. (embl-heidelberg.de)

Assays1

• Generation of biologically active adenosine by TAM-like macrophages was measured in luciferase-based reporter assays. (springer.com)

Orphan4

• This protein was earlier thought to be a receptor for vasoactive intestinal peptide (VIP) and was considered to be an orphan receptor. (wikidoc.org)
• They have an extended cleavable N-terminal domain thought to be involved in cell-cell contact 5 and almost all are still orphan receptors. (europeanpharmaceuticalreview.com)
• 4. Joost , P. , Methner, A. ( 2002 ) Phylogenetic analysis of 277 human G - protein -coupled receptors as a tool for the prediction of orphan receptor ligands. (pharmacologicalsciences.us)
• Phylogenetic clustering methods were used to elucidate the chemical nature of receptor ligands, which led to the identification of natural ligands for many orphan receptors. (biomedcentral.com)

Expression16

• The A 3 AR is upregulated in peripheral blood mononuclear cells of patients with rheumatoid arthritis as well as in several breast, colon and pancreatic carcinoma tissues [ 7 ], but more studies are needed to learn about the expression of this protein in normal patients. (biomedcentral.com)
• Yet targeting this receptor for neuroprotection is challenging due to its broad expression throughout the body. (aspetjournals.org)
• Effects of electroacupuncture on the expression of adenosine receptors in the heart tissue of myocardial ischemia rats]. (readbyqxmd.com)
• To explore the impact of electroacupuncture (EA) on the protein expression of adenosine receptors in the heart of the rats with myocardial ischemia (MI). (readbyqxmd.com)
• Estrogen stimulates adenosine receptor expression subtypes in human breast cancer MCF-7 cell line. (readbyqxmd.com)
• Scope includes mutations and abnormal protein expression. (cancerindex.org)
• Ovarian cancer (OvCA) tissues show abundant expression of the ectonucleotidases CD39 and CD73 which generate immunomodulatory adenosine, thereby inhibiting cytotoxic lymphocytes. (springer.com)
• Expression of ectonucleotidases also translated into increased levels of biologically active adenosine. (springer.com)
• This invention concerns a method of inducing an elevated level of adenosine in an individual by administering to the individual an effective amount of either i) recombinant protein CD73 or ii) a cytokine or another factor being capable of inducing endothelial CD73 expression, or a combination thereof. (patentsencyclopedia.com)
• 2. The method according to claim 1 wherein the elevated level of adenosine is achieved by up-regulating endothelial CD73 expression in the individual by administering to the individual an effective amount of a cytokine. (patentsencyclopedia.com)
• 5. A method for prevention or treatment of a disease or disorder requiring or benefiting from the elevation of the adenosine level in an individual, by administering to said individual an effective amount of amount of either i) recombinant protein CD73 or ii) a cytokine or another factor being capable of inducing endothelial CD73 expression, or a combination thereof. (patentsencyclopedia.com)
• 497) Bile acid receptor agonist GW4064 regulates PPARγ coactivator-1α expression through estrogen receptor-related receptor α. (blogspot.com)
• D 5 receptors are thought to positively regulate expression of renalase . (wikidoc.org)
• The protein expression degrees of p-ERK1/2, p-MEK1/2, TrKB and BDNF in the striatal cells had been significantly improved in the diabetic rats weighed against those in the standard rats. (cancer-pictures.org)
• [email protected]#To explore the action mechanism of acupoint selection along meridians to improve adenosine receptor in myocardial ischemia (MI) rats by comparing the effects of acupoint selection along meridians, acupoint selection at other meridians and non-acupoint on expression of adenosine receptor. (bvsalud.org)
• After treatment, the TTC staining was used to detect myocardial infarction, the Tunel method was used to detect cardiomyocyte apoptosis, and the immunohistochemistry was used to detect the expression of adenosine receptors A1, A2a and A2b. (bvsalud.org)

Myocardial6

• Adenosine is used as an adjunct to thallous (thallium) chloride TI 201 or Tc99m myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
• As with the A1, the A2A receptors are believed to play a role in regulating myocardial oxygen consumption and coronary blood flow. (wikipedia.org)
• The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
• More specifically, A1 and A2A receptors play a role in regulating myocardial oxygen consumption and coronary blood flow . (axonmedchem.com)
• Recently, clinical evidence was found for the A3 receptor to be involved in rheumatoid arthritis , among other myocardial functions. (axonmedchem.com)
• Preconditioning of cardiomyocytes with either A 1 or A 3 AR agonists protects against myocardial ischemia. (biomedcentral.com)

Signals1

• Adenosine signals through G-protein-coupled receptors and can regulate the host's response to sepsis. (jimmunol.org)

Monophosphate1

• 10. The method according to claim 5 wherein an effective amount of adenosine monophosphate is administered to the individual. (patentsencyclopedia.com)

Muscarinic receptors1

• Muscarinic receptors mediate many of the effects of acetylcholine in the central and peripheral nervous system. (wikidoc.org)

CD732

• Adenosine can be formed from AMP either intracellularly by cytosolic 5′-nucleotidase usually involving tissue hypoxia or extracellularly by ecto-5′-nucleotidase (CD73). (physiology.org)
• 14. The method according to claim 9, wherein the disease or disorder is a reperfusion injury resulting from organ transplantations or an other surgical operation and the administering of the recombinant protein CD73 or cytokine or another factor or a combination thereof is started before the surgical operation. (patentsencyclopedia.com)