A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.
A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.
A subclass of ADENOSINE RECEPTORS that are generally considered to be coupled to the GS, STIMULATORY G-PROTEIN which causes up regulation of CYCLIC AMP.
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Purine bases found in body tissues and fluids and in some plants.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)
A glycoprotein enzyme present in various organs and in many cells. The enzyme catalyzes the hydrolysis of a 5'-ribonucleotide to a ribonucleoside and orthophosphate in the presence of water. It is cation-dependent and exists in a membrane-bound and soluble form. EC 3.1.3.5.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
A group of enzymes which catalyze the hydrolysis of ATP. The hydrolysis reaction is usually coupled with another function such as transporting Ca(2+) across a membrane. These enzymes may be dependent on Ca(2+), Mg(2+), anions, H+, or DNA.
An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.
Catalyze the hydrolysis of nucleosides with the elimination of ammonia.
A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)
3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)
A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
5'-Adenylic acid, monoanhydride with sulfuric acid. The initial compound formed by the action of ATP sulfurylase on sulfate ions after sulfate uptake. Synonyms: adenosine sulfatophosphate; APS.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)
Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES.
A purine base and a fundamental unit of ADENINE NUCLEOTIDES.
Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
The rate dynamics in chemical or physical systems.
A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.
Drugs used to cause dilation of the blood vessels.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Proteins involved in the transport of NUCLEOSIDES across cellular membranes.
A purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.
A class of enzymes that catalyze the conversion of a nucleotide and water to a nucleoside and orthophosphate. EC 3.1.3.-.
Purine bases related to hypoxanthine, an intermediate product of uric acid synthesis and a breakdown product of adenine catabolism.
Purine or pyrimidine bases attached to a ribose or deoxyribose. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.
The circulation of blood through the CORONARY VESSELS of the HEART.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Nucleosides in which the purine or pyrimidine base is combined with ribose. (Dorland, 28th ed)
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
An enzyme which catalyzes the catabolism of S-ADENOSYLHOMOCYSTEINE to ADENOSINE and HOMOCYSTEINE. It may play a role in regulating the concentration of intracellular adenosylhomocysteine.
A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
The monomeric units from which DNA or RNA polymers are constructed. They consist of a purine or pyrimidine base, a pentose sugar, and a phosphate group. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).
A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Elements of limited time intervals, contributing to particular results or situations.
Treatment process involving the injection of fluid into an organ or tissue.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.
Purines with a RIBOSE attached that can be phosphorylated to PURINE NUCLEOTIDES.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A group of compounds which consist of a nucleotide molecule to which an additional nucleoside is attached through the phosphate molecule(s). The nucleotide can contain any number of phosphates.
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
A process that changes the nucleotide sequence of mRNA from that of the DNA template encoding it. Some major classes of RNA editing are as follows: 1, the conversion of cytosine to uracil in mRNA; 2, the addition of variable number of guanines at pre-determined sites; and 3, the addition and deletion of uracils, templated by guide-RNAs (RNA, GUIDE).
A subtype of equilibrative nucleoside transporter proteins that is sensitive to inhibition by 4-nitrobenzylthioinosine.
Inhibitor of phosphodiesterases.
Esters formed between the aldehydic carbon of sugars and the terminal phosphate of adenosine diphosphate.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
A purine nucleoside that has guanine linked by its N9 nitrogen to the C1 carbon of ribose. It is a component of ribonucleic acid and its nucleotides play important roles in metabolism. (From Dorland, 28th ed)
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The hollow, muscular organ that maintains the circulation of the blood.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
A subtype of equilibrative nucleoside transporter proteins that is insensitive to inhibition by 4-nitrobenzylthioinosine.
The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.
A rather large group of enzymes comprising not only those transferring phosphate but also diphosphate, nucleotidyl residues, and others. These have also been subdivided according to the acceptor group. (From Enzyme Nomenclature, 1992) EC 2.7.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
Established cell cultures that have the potential to propagate indefinitely.
Relatively complete absence of oxygen in one or more tissues.
Enzymes that catalyze the hydrolysis of CYCLIC AMP to form adenosine 5'-phosphate. The enzymes are widely distributed in animal tissue and control the level of intracellular cyclic AMP. Many specific enzymes classified under this heading demonstrate additional spcificity for 3',5'-cyclic IMP and CYCLIC GMP.
Pyrazolopyrimidine ribonucleosides isolated from Nocardia interforma. They are antineoplastic antibiotics with cytostatic properties.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
An enzyme that catalyzes the reaction between a purine nucleoside and orthophosphate to form a free purine plus ribose-5-phosphate. EC 2.4.2.1.
The veins and arteries of the HEART.
An enzyme that catalyzes the deamination of AMP to IMP. EC 3.5.4.6.
Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
Exposure of myocardial tissue to brief, repeated periods of vascular occlusion in order to render the myocardium resistant to the deleterious effects of ISCHEMIA or REPERFUSION. The period of pre-exposure and the number of times the tissue is exposed to ischemia and reperfusion vary, the average being 3 to 5 minutes.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
A pentose active in biological systems usually in its D-form.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Coronary vasodilator with some antiarrhythmic activity.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.
Analogs of those substrates or compounds which bind naturally at the active sites of proteins, enzymes, antibodies, steroids, or physiological receptors. These analogs form a stable covalent bond at the binding site, thereby acting as inhibitors of the proteins or steroids.
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is an inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal side effect is nephrotoxicity. In vivo, dideoxyadenosine is rapidly metabolized to DIDANOSINE (ddI) by enzymatic deamination; ddI is then converted to dideoxyinosine monophosphate and ultimately to dideoxyadenosine triphosphate, the putative active metabolite.
N(6)-[delta(3)-isopentenyl]adenosine. Isopentenyl derivative of adenosine which is a member of the cytokinin family of plant growth regulators.
The decrease in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.

Patterns of A2A extracellular adenosine receptor expression in different functional subsets of human peripheral T cells. Flow cytometry studies with anti-A2A receptor monoclonal antibodies. (1/693)

Signaling through A2A adenosine receptors (A2AR) regulates T lymphocyte expansion and modulates T cell receptor (TCR)-mediated effector functions in vitro. To understand the role of A2ARs in the regulation of immune response, we investigated the expression levels of this receptor in different functional lymphocyte subsets. Monoclonal anti-A2AR antibody was used to develop a flow cytometric assay to quantify the expression A2ARs on lymphocytes. We report that detectable levels of expression of A2ARs are much higher among T cells than B cells. More CD4(+) than CD8(+) T cells express A2ARs, but activation of T cells increases A2AR expression, predominantly in CD8(+) T cells. No significant differences were found in the proportion of A2AR+ cells between CD8(low) and CD8(high) T cells or between TCR/CD3(low) and TCR/CD3(high) T cells. Studies of T helper cell subsets (TH1 and TH2) reveal that lymphokine-producing cells are much more likely to express A2ARs than are cells that do not produce lymphokines. These results suggest that A2ARs are variably expressed on T cell subsets and may regulate cytokine production in activated T lymphocytes.  (+info)

Role of K+ channels in A2A adenosine receptor-mediated dilation of the pressurized renal arcuate artery. (2/693)

1. Adenosine A2A receptor-mediated renal vasodilation was investigated by measuring the lumenal diameter of pressurized renal arcuate arteries isolated from the rabbit. 2. The selective A2A receptor agonist CGS21680 dilated the arteries with an EC50 of 130 nM. The CGS21680-induced vasodilation was, on average, 34% less in endothelium-denuded arteries. 3. The maximum response and the EC50 for CGS21680-induced vasodilation in endothelium-intact arteries were not significantly affected by incubation with the K+ channel blockers apamin (100 nM), iberiotoxin (100 nM), 3,4-diaminopyridine (1 mM), glibenclamide (1 microM) or Ba2+ (10 microM). However, a cocktail mixture of these blockers did significantly inhibit the maximum response by almost 40%, and 1 mM Ba2+ alone or 1 mM Ba2+ in addition to the cocktail inhibited the maximum CGS21680-response by 58% and about 75% respectively. 4. CGS21680-induced vasodilation was strongly inhibited when the extracellular K+ level was raised to 20 mM even though the dilator response to 1 microM levcromakalim, a K(ATP) channel opener drug, was unaffected. 5. CGS21680-induced vasodilation was inhibited by 10 microM ouabain, an inhibitor of Na+/K(+)-ATPase, but ouabain had a similar inhibitory effect on vasodilation induced by 30 nM nicardipine (a dihydropyridine Ca2+ antagonist) or 1 microM levcromakalim. 6. The data suggest that K+ channel activation does play a role in A(2A) receptor-mediated renal vasodilation. The inhibitory effect of raised extracellular K+ levels on the A(2A) response may be due to K(+)-induced stimulation of Na+/K(+)-ATPase.  (+info)

Stimulation of expression for the adenosine A2A receptor gene by hypoxia in PC12 cells. A potential role in cell protection. (3/693)

The purpose of this study was to examine the regulation of adenosine A2A receptor (A2AR) gene expression during hypoxia in pheochromocytoma (PC12) cells. Northern blot analysis revealed that the A2AR mRNA level was substantially increased after a 3-h exposure to hypoxia (5% O2), which reached a peak at 12 h. Immunoblot analysis showed that the A2AR protein level was also increased during hypoxia. Inhibition of de novo protein synthesis blocked A2AR induction by hypoxia. In addition, removal of extracellular free Ca2+, chelation of intracellular free Ca2+, and pretreatment with protein kinase C inhibitors prevented A2AR induction by hypoxia. Moreover, depletion of protein kinase C activity by prolonged treatment with phorbol 12-myristate 13-acetate significantly inhibited the hypoxic induction of A2AR. A2AR antagonists led to a significant enhancement of A2AR mRNA levels during hypoxia, whereas A2AR agonists caused down-regulation of A2AR expression during hypoxia. This suggests that A2AR regulates its own expression during hypoxia by feedback mechanisms. We further found that activation of A2AR enhances cell viability during hypoxia and also inhibits vascular endothelial growth factor expression in PC12 cells. Thus, increased expression of A2AR during hypoxia might protect cells against hypoxia and may act to inhibit hypoxia-induced angiogenic activity mediated by vascular endothelial growth factor.  (+info)

Amplification of the cyclic AMP response to forskolin in pheochromocytoma PC12 cells through adenosine A(2A) purinoceptors. (4/693)

In this study, we present evidence on the ability of endogenous adenosine to modulate adenylyl cyclase activity in intact PC12 cells. The adenosine receptor antagonists PD 115199, xanthine amine congener, 8-cyclopentyl-1,3-dipropylxanthine, 8-(p-sulfophenyl)theophylline, and 3,7-dimethyl-1-propargylxanthine inhibited 10 microM forskolin-induced cyclic AMP (cAMP) accumulation, with IC(50) values of 2.76 +/- 1.16 nM, 17.4 +/- 1.08 nM, 443 +/- 1. 03 nM, 2.00 +/- 1.01 microM, and 2.25 +/- 1.05 microM, respectively. Inhibition by 2.5 nM PD 115199 was only partially reversed by increasing forskolin concentrations up to 100 microM. The addition of PD 115199 with or 60 min after forskolin caused a comparable inhibition of forskolin effect over the next hour. Both exogenous adenosine (0.1 microM) and its precursor, AMP (10 and 100 microM), significantly enhanced forskolin-induced cAMP accumulation, whereas inosine was ineffective. Forskolin activity was also potentiated by the hydrolysis-resistant adenosine receptor agonists 5'-N-ethylcarboxamido adenosine and CGS 21680 (8.9- and 12.2-fold increase, respectively). Adenosine deaminase (1 U/ml) and 8-SPT (25 microM), which nearly abolished the response to 1 microM adenosine, also reduced cAMP accumulation caused by AMP (-78 and -54%, respectively). These results demonstrate that in PC12 cells, activation of adenylyl cyclase by forskolin is highly dependent on the occupancy of A(2A) adenosine receptors and that AMP potentially contributes to the amplification of forskolin response.  (+info)

Neutrophil A2A adenosine receptor inhibits inflammation in a rat model of meningitis: synergy with the type IV phosphodiesterase inhibitor, rolipram. (5/693)

Bacterial meningitis is a disease worsened by neutrophil-induced damage in the subarachnoid space. In this study, the A2A adenosine receptors on human neutrophils were characterized, and the role of A2A receptors on the trafficking of leukocytes to the cerebrospinal fluid and on blood-brain barrier permeability (BBBP) was assessed in a rat meningitis model. Neutrophils bind the A2A selective antagonist, 125I-ZM241385 (Bmax=843 receptors/neutrophil; KD=0.125 nM). A selective A2A receptor agonist, WRC-0470 (2-cyclohexylmethylidene-hydrazinoadenosine; 0.03-1 microM), alone and synergistically with the type IV phosphodiesterase inhibitor, rolipram, increased neutrophil [cAMP]i and reduced cytokine-enhanced neutrophil adherence, superoxide release, and degranulation. These effects of WRC-0470 were reversed by ZM241385 (100 nM). In a lipopolysaccharide-induced rat meningitis model, WRC-0470 (0-0.9 microgram/kg/h), with or without rolipram (0-0.01 microgram/kg/h), inhibited pleocytosis and reduced the lipopolysaccharide-induced increase in BBBP, indicative of decreased neutrophil-induced damage.  (+info)

A role of p75 in NGF-mediated down-regulation of the A(2A) adenosine receptors in PC12 cells. (6/693)

Nerve growth factor (NGF) induces differentiation of the rat pheochromocytoma clone (PC12) by activating the high affinity receptor, p140(trkA), linked to mitogen-activated protein kinase. While the physiological role of the low affinity NGF receptor (p75) has not been clearly defined, this receptor promotes activation of nuclear factor (NF) kappaB in Schwann cells. PC12 cells express the A(2A) adenosine receptor (AR), whose expression is significantly decreased by NGF treatment. In this study, we determined whether TrkA or p75 is involved in NGF-mediated regulation of A(2A)AR expression. NGF treatment decreased A(2A)AR in a time-dependent manner, with maximal effects observed by 1 day, and continued down-regulation of the receptor for up to 3 days in the presence of NGF. The decrease in A(2A)AR was associated with a more delayed decrease in the steady-state levels of the A(2A)AR mRNA. Down-regulation of the A(2A)AR at 1 day was mimicked by activators of NFkappaB, such as H(2)O(2), and ceramide, and was attenuated by the inhibitor pyrrolidine dithiocarbamate or following transient transfection of PC12 cells with a dominant negative IkappaBalpha mutant. Moreover, NGF stimulated nuclear accumulation of p65 subunits of NFkappaB (but not p50 subunits) in PC12 cells, as determined by electrophoretic mobility shift assays and by Western blotting. In contrast, inhibition of TrkA by AG879 or of TrkA-dependent mitogen-activated protein kinase mitogen-activated protein kinase kinase with PD98059 blocked PC12 cell differentiation without affecting A(2A)AR down-regulation, suggesting dissociation between these two phenomena. Taken together, these data provide strong support for the involvement of the p75/NFkappaB pathway in NGF-mediated down-regulation of A(2A)AR in PC12 cells.  (+info)

Activation of leukotriene synthesis in human neutrophils by exogenous arachidonic acid: inhibition by adenosine A(2a) receptor agonists and crucial role of autocrine activation by leukotriene B(4). (7/693)

We report here that the apparent inability of isolated human polymorphonuclear leukocytes (PMNs) to efficiently transform arachidonic acid (AA) is the consequence of A(2a) receptor engagement by endogenous adenosine accumulating in incubation media. Indeed, when adenosine is eliminated from PMN suspensions by the addition of adenosine deaminase, or when cells are incubated with adenosine A(2a) receptor antagonists, important quantities (40-80 pmol/10(6) cells) of 5-lipoxygenase products are synthesized by PMN incubated with 1 to 5 microM exogenous AA. The selective A(2a) receptor agonist CGS21680 was a very potent inhibitor of the AA-induced leukotriene (LT) synthesis, showing an IC(50) of approximately 1 nM. The mechanism of AA-induced stimulation of LT synthesis observed in the absence of extracellular adenosine was investigated. In adenosine deaminase-treated PMN, exogenous AA induced Ca(2+) mobilization and the translocation of 5-lipoxygenase to nuclear structures. A time lag of 20 to 60 s (variable between PMN preparations) was observed consistently between the addition of AA and the elevation of intracellular Ca(2+) concentration (and LT synthesis), indicating that AA itself did not trigger the Ca(2+) mobilization in PMN. This AA-induced Ca(2+) mobilization, as well as the corresponding 5-lipoxygenase translocation and stimulation of LT synthesis, was blocked efficiently by the LT synthesis inhibitor MK0591, the LTB(4) receptor antagonists CP105696 and LY223982, and the LTA(4) hydrolase inhibitor SC57461A. These data demonstrate that AA is a highly potent and effective activator of LT synthesis and acts through a mechanism that requires an autocrine stimulatory loop by LTB(4).  (+info)

A(2A) adenosine receptor deficiency attenuates brain injury induced by transient focal ischemia in mice. (8/693)

Extracellular adenosine critically modulates ischemic brain injury, at least in part through activation of the A(1) adenosine receptor. However, the role played by the A(2A) receptor has been obscured by intrinsic limitations of A(2A) adenosinergic agents. To overcome these pharmacological limitations, we explored the consequences of deleting the A(2A) adenosine receptor on brain damage after transient focal ischemia. Cerebral morphology, as well as vascular and physiological measures (before, during, and after ischemia) did not differ between A(2A) receptor knock-out and wild-type littermates. The volume of cerebral infarction, as well as the associated neurological deficit induced by transient filament occlusion of the middle cerebral artery, were significantly attenuated in A(2A) receptor knock-out mice. This neuroprotective phenotype of A(2A) receptor-deficient mice was observed in different genetic backgrounds, confirming A(2A) receptor disruption as its cause. Together with complimentary pharmacological studies, these data suggest that A(2A) receptors play a prominent role in the development of ischemic injury within brain and demonstrate the potential for anatomical and functional neuroprotection against stroke by A(2A) receptor antagonists.  (+info)

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A concise synthesis of a series of N6-substituted adenosines with bicyclo[3.2.1]octan-6-yl and polycyclic N6-substituents has been developed. The adenosine A1 receptor (A1R) affinity and potency of these compounds was initially assessed using competitive binding assays and cyclic adenosine monophosphate (cAMP) accumulation assays in DDT1 MF-2 cells. The potency and receptor subtype selectivity of selected examples was further evaluated by measuring their effects on cAMP accumulation at all human adenosine receptor subtypes expressed in CHO cells. The results of these assays indicated that all of the synthesised N6-substituted adenosines are full agonists at A1R and activate this receptor selectively over the other adenosine receptor subtypes. The two standout compounds in terms of potency were N6-(3-thiabicyclo[3.2.1]octan-6-yl)adenosine and N6-(cubanylmethyl)adenosine with EC50 values at human A1R of 2.3 nM and 1.1 nM, respectively. The cubanylmethyl derivative in particular proved to be highly ...
TY - JOUR. T1 - The effect of development on the pattern of A1 and A2a-adenosine receptor gene and protein expression in rat peripheral arterial chemoreceptors.. AU - Gauda, Estelle B.. AU - Cooper, Reed Z.. AU - Donnelly, David F.. AU - Mason, Ariel. AU - McLemore, Gabrielle L.. PY - 2006. Y1 - 2006. UR - http://www.scopus.com/inward/record.url?scp=33745272264&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=33745272264&partnerID=8YFLogxK. M3 - Article. C2 - 16683708. VL - 580. JO - Advances in Experimental Medicine and Biology. JF - Advances in Experimental Medicine and Biology. SN - 0065-2598. ER - ...
Adenosine is an important mediator of the endogenous defense against ischemia-induced injury in the heart. Adenosine can achieve cardioprotection by mediating the effect of ischemic preconditioning and by protecting against myocyte injury when it is present during the infarct-producing ischemia. A novel adenosine A3 receptor can mediate this protective function. One approach to achieve cardioprotection is to enhance myocardial sensitivity to the endogenous adenosine by increasing the number of adenosine receptors instead of administering an adenosine receptor agonist. The objective of the present study was to investigate whether genetic manipulation of the cardiac myocyte, achieved by gene transfer and overexpression of the human A3 receptor cDNA, renders the myocytes resistant to the deleterious effect of ischemia. Prolonged hypoxia with glucose deprivation, causing myocyte injury and adenosine release, was used to simulate ischemia in cultured chick embryo ventricular myocytes. During simulated
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Adenosine mediates many physiological functions via activation of extracellular receptors. The modulation of cell growth by adenosine was found to be receptor-mediated. In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. When both A1 and A2 receptors were blocked, colony formation or growth was not inhibited at low concentrations of adenosine but was inhibited at high adenosine concentrations ...
Intra- and extracellular adenosine levels rise in response to physiological stimuli and with metabolic/energetic perturbations, inflammatory challenge and tissue injury. Extracellular adenosine engages members of the G-protein coupled adenosine receptor (AR) family to mediate generally beneficial acute and adaptive responses within all constituent cells of the heart. In this way the four AR sub-types - A1, A2A, A2B, and A 3Rs - regulate myocardial contraction, heart rate and conduction, adrenergic control, coronary vascular tone, cardiac and vascular growth, inflammatory-vascular cell interactions, and cellular stress-resistance, injury and death. The AR sub-types exert both distinct and overlapping effects, and may interact in mediating these cardiovascular responses. The roles of the ARs in beneficial modulation of cardiac and vascular function, growth and stress-resistance render them attractive therapeutic targets. However, interactions between ARs and with other receptors, and their ubiquitous
In this function, we ask if the simultaneous motion of agonist and antagonist among surface area receptors (i. in modulating G-protein activation and receptor desensitization. Quite simply, we determine the results from the simultaneous motion of agonist and antagonist among surface area receptors for G-protein activation and receptor desensitization. A Monte Carlo model construction can be used to monitor the diffusion and result of specific receptors, allowing the necessity for receptors and G-proteins or receptors and kinases to discover one another by diffusion (collision coupling) to become applied explicitly. Simulations are accustomed to scan a wide range of circumstances and to recognize regimes which may be of experimental curiosity. Strategies Estimating the function of diffusion The reactions making GPCR activation and phosphorylation are proven schematically in Fig. 1. To be able to accurately simulate these reactions, we initial determine which bimolecular reactions will tend to be ...
The report displayed here plans showcase players to make steady progress while adequately managing one of a kind difficulties in the worldwide Adenosine advertise. The examiners and analysts creating the report have thought about different elements anticipated to emphatically and contrarily sway the worldwide Adenosine advertise. The report incorporates SWOT and PESTLE investigations to give a more profound comprehension of the worldwide Adenosine advertise. The entirety of the main organizations remembered for the report are profiled dependent on net edge, piece of the overall industry, tentative arrangements, late advancements, target client socioeconomics, items and applications, and other basic variables. The report additionally offers local examination of the Adenosine advertise with high spotlight on showcase development, development rate, and development potential. Top Players Considered in Global Builders and Adenosine Market :- , Yamasa, Meihua Group, Tuoxin, Mingxin Pharmaceuticla, ...
Synonyms for adenosine 5'-diphosphate in Free Thesaurus. Antonyms for adenosine 5'-diphosphate. 1 synonym for adenosine diphosphate: ADP. What are synonyms for adenosine 5'-diphosphate?
Read A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics by with Rakuten Kobo. This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide ...
The protein encoded by this gene is an adenosine receptor that belongs to the G-protein coupled receptor 1 family. There are 3 types of adenosine receptors, each with a specific pattern of ligand binding and tissue distribution, and together they regulate…
A nucleoside that is composed of adenine and d-ribose. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
Adenosine is a ubiquitous signaling molecule whose physiological functions are mediated by its interaction with four G-protein-coupled receptor subtypes, termed A(1), A(2A), A(2B) and A(3). As a result of increased metabolic rates, this nucleoside is released from a variety of cells throughout the b …
Breakdown of excessive amounts of adenosine triphosphate (ATP), the main energy source of a cell, leads to the formation of extracellular adenosine, an important signaling molecule involved in multiple pathways that regulate neuronal and immunological function. Adenosine is either actively produced by certain cells or is released from damaged tissue, particularly when cells are starved of oxygen. Adenosine levels are tightly regulated at all points throughout its production, release, uptake and degradation, and disruptions in control that result in excessively high levels are associated with a number of human pathologies, including severe combined immunodeficiency (SCID).. The diversity in the regulation and function of adenosine (both of which differ in a tissue- and cell-specific manner) means that it has been difficult to unravel its exact role at the molecular level. In addition, data obtained in vitro, or in tissue culture, might not be relevant to whole organisms, and mammalian model ...
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5-(4-((aminocarbonyl)(hydroxy)amino)but-1-ynyl)-2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)benzamide: has antiasthma activity; structure in first source
Adora1 - Adora1 (untagged) - Mouse adenosine A1 receptor (cDNA clone MGC:90841 IMAGE:30536680), (10ug) available for purchase from OriGene - Your Gene Company.
View mouse Adora1 Chr1:134199225-134235431 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
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Mechanisms involved in increased sensitivity to adenosine A2A receptor activation and hypoxia-induced vasodilatation in porcine coronary ...
duralone ATP injection(Adenosine Tri-Phosphate) is utilized in the Krebs Cycle - which physiologically is one of the key providers of duralone ATP
Adenosine is so readily formed in the brain that for some time its quantity there was overestimated by a factor of 20 or more (Berne et al. 1974; Newman and McIlwain, 1977). Now, rapid fixation...
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4-((8-amino-3,6,10,13,16,19-hexaazabicyclo(6.6.6)icosane-1-ylamino)methyl)benzoic acid: a bifunctional chelating agent; structure in first source
Note:Only the main profile, including all conditions, is shown. Additional statistics and tissue specific profiles are available here.. ...
Note:Only the main profile, including all conditions, is shown. Additional statistics and tissue specific profiles are available here.. ...
This study demonstrates that three structurally distinct A1 receptor antagonists increase extracellular adenosine levels in two different types of cardiovascular cells, i.e., cardiac fibroblasts and vascular smooth muscle cells, and in two species, rats and humans. The extracellular adenosine responses to A1 receptor antagonists are concentration dependent, and are attenuated by pertussis toxin, a toxin that inactivates inhibitory G proteins, and by AMPCP, an inhibitor of ecto-5′-nucleotidase. This study also demonstrates that augmentation of extracellular adenosine levels attenuates the increase in extracellular adenosine induced by A1 receptor antagonists. Finally, this study shows that the effects of A1receptor antagonists on extracellular adenosine levels develop with a time lag of several hours.. Our working hypothesis is that high-affinity A1receptors detect elevated levels of adenosine in the biophase of the cell surface and engage a signal transduction process that ultimately decreases ...
Our work demonstrates that human endothelial cells of disparate origin are characterized by differential expression of adenosine receptor subtypes. HUVECs express mRNA for A2A and A2B receptors at a ratio of 10:1, and this preferential gene expression agrees well with the typical pharmacological phenotype of A2A receptor-mediated simulation of adenylate cyclase by adenosine analogs. Using complementary techniques, RT-PCR, and gene expression array, we found that A1 and A3 adenosine receptors are not expressed in HUVECs. Previous studies in HUVECs have suggested a potential role of A1 receptor in maintaining endothelial barrier function4 and of A1 and A3 receptors in modulation of tissue factors expression.6 The apparent contradiction between these results and ours can be explained by the use of nonselective concentrations of adenosine receptor ligands in previous studies.. HMEC-1 also express only A2A and A2B mRNA, but in contrast to HUVECs, they express predominantly A2B receptor mRNA, with a ...
TY - JOUR. T1 - Microwave-assisted and conventional synthesis of benzothieno [3,2-e] [1,3,4] triazolo[4,3-c]pyrimidines. T2 - A comparative study. AU - Gaonkar, Santhosh L.. AU - Ahn, Chuljin. AU - Princia, AU - Shetty, Nitinkumar S.. PY - 2014/8/20. Y1 - 2014/8/20. N2 - Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4] triazolo[4,3-c] pyrimidines (5a-c) were synthesized from the precursor 2-amino-7-oxo-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile 1 by employing the conventional method as well as the microwave irradiation technique. The precursor 2-amino-3-cyanothiophene analogue 1 was synthesized by employing the well-known Gewald reaction. In the present work it has been found that the microwave supported syntheses are more efficient than the conventional classical heating methods. The structures of all the compounds were ascertained by spectral and analytical data.. AB - Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4] triazolo[4,3-c] pyrimidines ...
The review summarizes data evaluating the role of adenosine receptor signaling in murine hematopoietic functions. The studies carried out utilized either non-selective activation of adenosine receptors induced by elevation of extracellular adenosine or by administration of synthetic adenosine analogs having various proportions of selectivity for a particular receptor. Numerous studies have described stimulatory effects of non-selective activation of adenosine receptors, manifested as enhancement of proliferation of cells at various levels of the hematopoietic hierarchy. Subsequent experimental approaches, considering the hematopoiesis-modulating action of adenosine receptor agonists with a high level of selectivity to individual adenosine receptor subtypes, have revealed differential effects of various adenosine analogs. Whereas selective activation of A(1) receptors has resulted in suppression of proliferation of hematopoietic progenitor and precursor cells, that of A(3) receptors has led to ...
In this report we show that it is possible to detect the expression of a G protein-coupled receptor, the A2AR, in human lymphocytes both on the basis of a functional assay (cAMP accumulation) and by flow cytometry using an antireceptor mAb. We were able to describe for the first time the distribution of A2AR among minor T cell subpopulations through the use of a combination of anti-A2AR mAb and mAbs that recognize T cell surface markers or cytokines. The principle findings of this study are that much higher levels of A2AR expression is found in T cells than in B cells (Fig. 3) and higher levels of cytokines are detected in activated T cells that express A2AR than in activated T cells that do not express these receptors (Figs. 6 and 7).. The detection of higher levels of cytokines among A2AR+ cells is surprising because A2AR-mediated signaling antagonizes the effects of T cell activation (Koshiba et al., 1997; Huang et al., 1997). Therefore, we expected that cytokine secretion would be the lowest ...
The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. 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). 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. 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 ...
In the heart, endogenous adenosine attenuates the beta-adrenergic-elicited increase in contractile performance via activation of adenosine A1 receptors. It has been recently reported that this function of adenosine becomes more pronounced with myocardial maturation. The purpose of the present study was to determine whether mature hearts possess a greater sensitivity than immature hearts to this antiadrenergic effect of adenosine. Isolated perfused hearts or atria from immature (ca. 23 days) and mature (ca. 80 days) rats were stimulated with isoproterenol (Iso), a beta-adrenergic agonist, at 10(-8) M and concomitantly exposed to increasing concentrations of 2-chloro-N6-cyclopentyladenosine (CCPA), a highly selective and potent adenosine A1-receptor agonist, from 10(-12) to 10(-6) M. CCPA at 10(-10)-10(-6) M dose dependently reduced the Iso-elicited contractile response more in immature than in mature hearts or atria. At 10(-6) M, CCPA reduced the Iso-elicited contractile response by 103% in immature
In this study and previously (24), we have demonstrated that blockade of the A2AAR with an A2A-specific AR antagonist protected mice from EAE by hindering lymphocyte entry into the brain and spinal cord of wild-type mice. This finding was unexpected, as this function of adenosine, that is, mediating lymphocyte migration into the CNS, was previously unknown. Furthermore, the facts that adenosine suppresses the immune response and resolves inflammation (2) are at odds with the finding that blockade of the A2AAR, which mediates the preponderance of adenosines suppressive and anti-inflammatory functions (2), protects mice from EAE (24). The purpose of this study was to delineate adenosines role in the immune response from its function in mediating immune cell migration into the CNS via the A2A receptor.. We show that A2AAR−/− mice developed more severe EAE than did their wild-type counterparts. This severe disease was characterized in the CNS by increased numbers of lymphocytes and activated ...
1-1H-Indol-7-yl-3-[5-(2-{thieno[3,2-d]pyrimidin-4-ylamino}ethyl)-1,3-thiazol-2-yl]urea | C20H17N7OS2 | CID 25138117 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Synonyms for adenosine triphosphatase test in Free Thesaurus. Antonyms for adenosine triphosphatase test. 2 words related to adenosine: biochemistry, nucleoside. What are synonyms for adenosine triphosphatase test?
Two main findings arise from this study: (1) the adenosine A2A receptor antagonist SCH 58261 shows neuroprotective effects in an excitotoxic rat model of HD; and (2) the inhibition of QA-evoked increase in extracellular glutamate seems to be the main mechanism of the effects elicited by SCH 58261.. The finding that SCH 58261 significantly prevented most of the effects induced by the intrastriatal injection of an excitotoxin is in line with some findings suggesting that activation of A2A receptors could participate in the generation of excitotoxicity. Adenosine A2A receptor agonists have been reported indeed to stimulate glutamate release in the rat striatum (Popoli et al., 1995; Corsi et al., 1999). Moreover, in previous experiments, we observed that the intrastriatal injection of the adenosine A2A receptor agonist CGS 21680, together with QA, potentiated QA-induced mortality in a dose-dependent way (50, 75, and 83% of mortality after 3, 6, and 12 nmol QA plus CGS 21680, respectively; P. Popoli, ...
Cyclic AMP; 35-cyclic AMP; 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide; Acrasin; Adenosine 3,5-cyclic monophosphate; Adenosine 3,5-cyclic phosphate; Adenosine 3,5-cyclophosphate; Adenosine 3,5-monophosphate; Adenosine 3,5-cyclic monophosphorate; Adenosine 3,5-cyclic monophosphoric acid; Adenosine cyclic monophosphate; Cyclic 3,5-AMP; Cyclic 3,5-adenylate; Cyclic 3,5-adenylic acid; Cyclic adenosine 3,5-phosphate; adenosine cyclic-monophosphate; adenosine-cyclic-phosphate; adenosine-cyclic-phosphoric-acid; ...
Cyclic AMP; 35-cyclic AMP; 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide; Acrasin; Adenosine 3,5-cyclic monophosphate; Adenosine 3,5-cyclic phosphate; Adenosine 3,5-cyclophosphate; Adenosine 3,5-monophosphate; Adenosine 3,5-cyclic monophosphorate; Adenosine 3,5-cyclic monophosphoric acid; Adenosine cyclic monophosphate; Cyclic 3,5-AMP; Cyclic 3,5-adenylate; Cyclic 3,5-adenylic acid; Cyclic adenosine 3,5-phosphate; adenosine cyclic-monophosphate; adenosine-cyclic-phosphate; adenosine-cyclic-phosphoric-acid; ...
Since their discovery approximately 25 years ago, adenosine receptors have now emerged as important novel molecular targets in disease and drug discovery. These proteins play important roles in the entire spectrum of disease from inflammation to immune suppression. Because of their expression on a number of different cell types and in a number of different organ systems they play important roles in specific diseases, including asthma, rheumatoid arthritis, Parkinsons disease, multiple sclerosis, Alzheimers disease, heart disease, stroke, cancer, sepsis, and obesity. As a result of intense investigations into understanding the molecular structures and pharmacology of these proteins, new molecules have been synthesized that have high specificity for these proteins and are now entering clinical trials. These molecules will define the next new classes of drugs for a number of diseases with unmet medical needs.
This is Digital Version of (Ebook) 978-9048131433 A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics Product Will Be Delivered
The IUPHAR/BPS Guide to Pharmacology. A2B receptor - Adenosine receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
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Orthoplex Adenosine 60 Tablets contains 100mg of adenosine. Orthoplex Adenosine plays a major role in the production of cellular energy ATP
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Definition of adenosine triphosphate, with etymology, pronunciation (phonetic and audio), synonyms, antonyms, derived terms and more about the word adenosine triphosphate.
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Structure, properties, spectra, suppliers and links for: 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide.
6-Amino-1,3-dihydro-2H-purin-2-one; CAS Number: 3373-53-3; Linear Formula: C5H5N5O; find Ambeed, Inc.-AMBH46A96504 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
You are viewing an interactive 3D depiction of the molecule 5-o-(4,6-dihydroxy-2,4,6-trioxido-1,3,5,2,4,6-trioxatriphosphinan-2-yl)adenosine (C10H14N5O12P3) from the PQR.
Author: Allen Loyd V Jr, Year: 2013, Abstract: A formulation for preparing Adenosine 3-mg/mL Injection. Includes ingredients, method of preparation, discussion, and references for the compounding pharmacist.
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The A3 adenosine receptor (A3AR) has emerged as a therapeutic goal with A3AR agonists to deal with the worldwide problem of neuropathic ache; investigation into their mode of motion is important for ongoing medical growth. A3ARs on immune cells, and their activation throughout pathology, modulates cytokine launch. Thus, immune cells as a mobile substrate for. Read More ...
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What is the molecular mechanism by which lack of adenosine receptor signaling results in a pro-calcific phenotype, and are these pathways applicable to calcification seen in more common diseases ...
ウサギ・ポリクローナル抗体 ab106143 交差種: Hu 適用: WB,IHC-P,ICC/IF…Adenosine Receptor A2a抗体一覧…画像、プロトコール、文献などWeb上の情報が満載のアブカムの Antibody…
II. CÍL NÁVRHU. Cílem návrhu je umožnit novým členským státům účast v projektu Evropské hlavní město kultury před skončením platnosti stávajícího rozhodnutí v roce 2019. Návrh nemění stávající pořadí pro podávání návrhů členskými státy, ale zavádí se nový systém jmenování dvou členských států oprávněných každý rok počínaje rokem 2009 podat návrhy tak, aby v členských státech mohla být vybrána dvě hlavní města.. III. ROZBOR SPOLEČNÉHO POSTOJE. 1. Obecné poznámky. Rada v návrhu Komise neprovedla žádné změny. Komise zcela přijala 1 změnu z 5 změn navrhovaných Parlamentem (změna 1).. 2. Změny učiněné Evropským parlamentem. 2.1 Změny přijaté Radou. Rada plně potvrdila změnu navrhovanou Parlamentem a přijatou Komisí (změna 1).. 2.2 Změny nezapracované Radou. Rada stejně jako Komise usoudila, že změny 2, 3, 4 a 5 šly nad rámec návrhu, a jejich zapracování nepokládala za vhodné.. III. ZÁVĚRY. Rada se ...
Traditionally given via stopcock with immediate flush secondary to very short half life. Newer study showing that you may be able to mix with normal saline and give as single push, however further evidence is still needed[1] ...
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Genetic information processingProtein synthesistRNA and rRNA base modificationtRNA threonylcarbamoyl adenosine modification protein YeaZ (TIGR03725; HMM-score: 178.6) ...
AKI 1 is an adenosine regulating agent. It was undergoing preclinical studies in the USA with Gensia Sicor for the treatment of inflammatory disorders, however
A hub covering the latest stem cell research and news from bench science and clinical applications, and forum for research labs and societies worldwide.
... caffeine blocks adenosine receptors A1 and A2A. Adenosine is a by-product of cellular activity, and stimulation of adenosine ... Caffeine dependence forms due to caffeine antagonizing the adenosine A2A receptor, effectively blocking adenosine from the ... Continued exposure to caffeine leads the body to create more adenosine-receptors in the central nervous system, which makes it ... caffeine tolerance occurs when the body responds to an intake of caffeine through the up-regulation of adenosine-receptors. ...
"A2A adenosine receptor protects tumors from antitumor T cells." Proceedings of the National Academy of Sciences 103, no. 35 ( ... class II complexes with mixed agonist/antagonist properties provide evidence for ligand-related differences in T cell receptor- ...
... adenosine A1/A2A heteromers and dopamine D1/D2 and D1/D3 heteromers) or between entirely unrelated receptors such as CB1/A2A, ... Zezula J, Freissmuth M (March 2008). "The A2A-adenosine receptor: a GPCR with unique features?". British Journal of ... "Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain". Frontiers in Bioscience. 13 (13): 2391-9. doi: ... "Striatal adenosine A2A and cannabinoid CB1 receptors form functional heteromeric complexes that mediate the motor effects of ...
... which acts as a potent and selective agonist of the adenosine A2A receptor. It was discontinued from clinical trials following ... "Structure of an Agonist-Bound Human A2A Adenosine Receptor". Science. 332 (6027): 322-7. Bibcode:2011Sci...332..322X. doi: ... Russo, Cristina; Arcidiacono, Giuseppe; Polosa, Riccardo (2006). "Adenosine receptors: promising targets for the development of ... but its high selectivity has made it useful for detailed mapping of the internal structure of the A2A receptor. ...
... is a drug which acts as a potent and selective antagonist for the adenosine receptor A2A, with more than 50x ... Minghetti L, Greco A, Potenza RL, Pezzola A, Blum D, Bantubungi K, Popoli P (May 2007). "Effects of the adenosine A2A receptor ... Popoli P, Reggio R, Pèzzola A, Fuxe K, Ferré S (July 1998). "Adenosine A1 and A2A receptor antagonists stimulate motor activity ... November 2009). "Adenosine A2A receptor blockade prevents synaptotoxicity and memory dysfunction caused by beta-amyloid ...
Adenosine receptor Mayer CA, Haxhiu MA, Martin RJ, Wilson CG (2006). "Adenosine A2A receptors mediate GABAergic inhibition of ... CGS-21680 is a specific adenosine A2A subtype receptor agonist. It is usually presented as an organic hydrochloride salt with a ... subtype specific analogue for adenosine. This includes research in respiration where it is believed that A2A receptors are ... Xie S, Shafer G, Wilson CG, Martin HB (2006). "In vitro adenosine detection with a diamond-based sensor". Dia Rel Mater. 15 (2- ...
... , sold under the brand name Lexiscan among others, is an A2A adenosine receptor agonist that is a coronary ... Kim DG, Bynoe MS (May 2016). "A2A adenosine receptor modulates drug efflux transporter P-glycoprotein at the blood-brain ... Cerqueira MD (July 2004). "The future of pharmacologic stress: selective A2A adenosine receptor agonists". The American Journal ... as regadenoson vasodilates via the adenosine pathway without stimulating beta adrenergic receptors.[citation needed] One side ...
... adenosine A2A receptors (A2A), DRD2-A2A heterotetramers, and enkephalin. Both types express glutamate receptors (NMDAR and ... and express the peptide enkephalin and a high density of dopamine D2 and adenosine A2A receptors (they also express adenosine ... and express the peptides dynorphin and substance P and dopamine D1 and adenosine A1 but not A2A receptors (Ferréet al., 1997; ... "Allosteric mechanisms within the adenosine A2A-dopamine D2 receptor heterotetramer". Neuropharmacology. 104: 154-60. doi: ...
Ventures have been undertaken to explore antagonists of adenosine receptors (specifically A2A) as an avenue for novel drugs for ... Jenner P (2014). "An overview of adenosine A2A receptor antagonists in Parkinson's disease". International Review of ... Several dopamine agonists that bind to dopamine receptors in the brain have similar effects to levodopa. These were initially ... and underlying brain pathology or changes in neurotransmitters or their receptors (e.g., acetylcholine, serotonin) are also ...
Adenosine modulates the preBötC output via activation of the A1 and A2A receptor subtypes. An adenosine A1 receptor agonist has ... Another synthetic drug specific to the adenosine A2A receptor subtype is CGS-21680 that has been shown to cause apneas in 14- ... Mayer CA, Haxhiu MA, Martin RJ, Wilson CG (January 2006). "Adenosine A2A receptors mediate GABAergic inhibition of respiration ... Since many of these neurons express GABA, glutamate, serotonin and adenosine receptors, chemicals custom tailored to bind at ...
July 2008). "Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: ... SCH-442,416 is a highly selective adenosine A2a subtype receptor antagonist. It is widely used in its 11C radiolabelled form to ... April 2005). "In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416". European Journal of ... El Yacoubi M, Costentin J, Vaugeois JM (December 2003). "Adenosine A2A receptors and depression". Neurology. 61 (11 Suppl 6): ...
Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). "Oligomerization of adenosine A2A and dopamine D2 receptors in living ... as it produces stimulant effects by inhibiting adenosine receptors. Adenosine receptors are thought to be a large driver of ... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors, however the implications for humans are ... Caffeine is an adenosine receptor antagonist, and only indirectly increases catecholamine transmission in the brain. Pitolisant ...
Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). "Oligomerization of adenosine A2A and dopamine D2 receptors in living ... as it produces stimulant effects by inhibiting adenosine receptors.[64] Adenosine receptors are thought to be a large driver of ... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors,[67] however the implications for humans ... as it exerts its effects by antagonizing adenosine receptors instead of acting directly on monoamines.[44] ...
Other substrates include the adenosine A2A receptor and the Ro52 (TRIM21) protein. USP4 is a nucleocytoplasmic shuttling ...
"The adenosine A2A receptor interacts with the actin-binding protein alpha-actinin". The Journal of Biological Chemistry. 278 ( ...
... is a high affinity antagonist ligand selective for the adenosine A2A receptor. In animal models, ZM-241,385 has been ... a high affinity antagonist radioligand selective for the A2a adenosine receptor". Molecular Pharmacology. 48 (6): 970-4. PMC ... "Neuroprotection by caffeine and adenosine A2A receptor blockade of beta-amyloid neurotoxicity". British Journal of Pharmacology ... Gołembiowska K, Dziubina A (September 2004). "Striatal adenosine A(2A) receptor blockade increases extracellular dopamine ...
"Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation". Nature. 474 (7352): 521-525. doi: ... 2010 and since then his group has used structural biology to discover how the beta1-adrenoceptor and the adenosine A2A receptor ... Tate is known for his contributions to the understanding of G protein-coupled receptors. Tate was awarded the degree of BSC ( ... Recent work has focused on understanding how G proteins coupled to G protein-coupled receptors, which has been facilitated by ...
Giving an adenosine A2A receptor antagonist on top of existing treatment for Parkinson's disease. In pharmacology, the term is ... Zhu, C; Wang, G; Li, J; Chen, L; Wang, C; Wang, Y; Lin, P; Ran, H (November 2014). "Adenosine A2A receptor antagonist ...
Subsequently, cAMP signaling is triggered in T cell that express the adenosine A2A receptor. Adenosine receptor are also ... In addition, the tumor cells may also express adenosine A1 and A3 receptors associated with Gαi proteins, promoting both the ... which limits the inflammatory immune response by negative feedback in neutrophil which express the adenosine receptor. Some ... Free adenosine generated by NT5E inhibits cellular immune responses and thereby promotes immune escape of tumor cells. Due to ...
... this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A-D2 receptor heterotetramer has ... this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor) and the A2A-D2 receptor heterotetramer ( ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ... Adenosine A2A receptor (A2AR)-dopamine D2 receptor (D2R) heteromers are key modulators of striatal neuronal function. It has ...
... with the human adenosine A2A receptor". J. Recept. Signal Transduct. Res. 26 (4): 241-58. doi:10.1080/10799890600710592. PMID ... It also mediated D1 receptor signalling in the striatum and is hence involved in motor control. Second messenger system G ... protein-coupled receptor Heterotrimeric G protein Adenylyl cyclase Protein kinase A Olfactory receptors GRCh38: Ensembl release ... a member of the Gs alpha subunit family that is a key component of G protein-coupled receptor-regulated adenylyl cyclase signal ...
... present and future of A2A adenosine receptor antagonists in the therapy of Parkinson's disease". Pharmacology & Therapeutics. ... In animal models it was shown that the intake of Adenosine receptor antagonists together with Levodopa can amplify its ... Dopamine agonists in the brain have a similar effect to levodopa since they bind to dopaminergic postsynaptic receptors. ...
"Prevention of dyskinesia by an NMDA receptor antagonist in MPTP monkeys: effect on adenosine A2A receptors". Synapse (New York ... Barton ME, White HS (March 2004). "The effect of CGX-1007 and CI-1041, novel NMDA receptor antagonists, on kindling acquisition ... Kovács G, Kocsis P, Tarnawa I, Horváth C, Szombathelyi Z, Farkas S (January 2004). "NR2B containing NMDA receptor dependent ... "Implication of NMDA receptors in the antidyskinetic activity of cabergoline, CI-1041, and Ro 61-8048 in MPTP monkeys with ...
... the subset of these neurons that expresses both D2-type dopamine receptors and adenosine A2A receptors), located within the ... Here, we show that chemogenetic or optogenetic activation of excitatory adenosine A2A receptor-expressing indirect pathway ... "Striatal adenosine A2A receptor neurons control active-period sleep via parvalbumin neurons in external globus pallidus". eLife ... The nucleus accumbens comprises a contingent of neurons specifically expressing the post-synaptic A2A-receptor (A2AR) subtype ...
Adams CL, Cowen MS, Short JL, Lawrence AJ (March 2008). "Combined antagonism of glutamate mGlu5 and adenosine A2A receptors ... Lea, P. M.; Faden, A. I. (2006). "Metabotropic Glutamate Receptor Subtype 5 Antagonists MPEP and MTEP". CNS Drug Reviews. 12 (2 ... Li, X.; Need, A. B.; Baez, M.; Witkin, J. M. (2006). "Metabotropic Glutamate 5 Receptor Antagonism is Associated with ... Rasmussen K, Martin H, Berger JE, Seager MA (February 2005). "The mGlu5 receptor antagonists MPEP and MTEP attenuate behavioral ...
Adenosine binds with much lower affinity to A2A and A2B receptors causing dilation of efferent arterioles. The binding of ... "In part because of the striking effect of deletion of A1 adenosine receptors (A1AR), adenosine generated from released ATP has ... "Afferent arteriolar vasodilator effect of adenosine predominantly involves adenosine A2B receptor activation". American Journal ... Adenosine constricts the afferent arteriole by binding with high affinity to the A1 receptors a Gi/Go. ...
Here, we show that chemogenetic or optogenetic activation of excitatory adenosine A2A receptor-expressing indirect pathway ... "Striatal adenosine A2A receptor neurons control active-period sleep via parvalbumin neurons in external globus pallidus". eLife ... the medium spiny neurons of the D2-type which co-express adenosine A2A receptors), and a GABAergic nucleus in the lateral ...
... and the affinity of these receptors for adenosine. Micromolar concentrations of adenosine activate A2A and A2B receptors. This ... whereas the activation of the adenosine A2A receptor inhibits osteoclast function. The other three adenosine receptors are ... The P2RX7 receptor is overexpressed in most malignant tumors. The expression of the adenosine A2A receptor on endothelial cells ... Formation of foam cells is inhibited by adenosine A2A receptors. Abnormal levels of ATP and adenosine are present in the ...
July 2003). "Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic ... is a drug which acts as a potent and selective antagonist for the adenosine receptors, with some selectivity for the A1 ... relation to adenosine antagonism". Psychopharmacology. 95 (1): 19-24. doi:10.1007/bf00212759. PMID 3133696. Karcz-Kubicha M, ... receptor subtype, as well as a non-selective phosphodiesterase inhibitor. It has stimulant effects in animals with slightly ...
... a high affinity antagonist radioligand selective for the A2a adenosine receptor". Molecular Pharmacology. 48 (6): 970-4. PMID ... Neuroprotection by caffeine and adenosine A2A receptor blockade of beta-amyloid neurotoxicity". British Journal of Pharmacology ... Gołembiowska K, Dziubina A (2004). „Striatal adenosine A(2A) receptor blockade increases extracellular dopamine release ... ZM-241,385 je antagonist visokog afiniteta koji je selektivan za adenosinski A2A receptor.[3] ...
transmembrane signaling receptor activity. • Wnt-activated receptor activity. • G-protein coupled receptor activity. ... "Frizzled Receptors: FZD5". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ... cell surface receptor signaling pathway. • vasculature development. • regulation of autophagy of mitochondrion. • branching ...
taste receptor activity. • fatty acid binding. • lipid binding. • G-protein coupled receptor activity. ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ... G-protein coupled receptor 120 is a protein that in humans is encoded by the GPR120 gene.[5][6] ... "Entrez Gene: GPR120 G protein-coupled receptor 120".. *^ Oh DY, Talukdar S, Bae EJ, Imamura T, Morinaga H, Fan W, Li P, Lu WJ, ...
G-protein coupled receptor signaling pathway. • signal transduction. • G-protein coupled purinergic nucleotide receptor ... G-protein coupled purinergic nucleotide receptor activity. • G-protein coupled receptor activity. • signal transducer activity ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ... Probable G-protein coupled receptor 34 is a protein that in humans is encoded by the GPR34 gene.[5][6][7] ...
A2A adenosine receptor[edit]. Main article: Adenosine A2A receptor. As with the A1, the A2A receptors are believed to play a ... A1 adenosine receptor[edit]. Main article: Adenosine A1 receptor. The adenosine A1 receptor has been found to be ubiquitous ... "Entrez Gene: ADORA2A adenosine A2A receptor".. *^ a b Jacobson KA, Gao ZG (2006). "Adenosine receptors as therapeutic targets" ... The adenosine receptors (or P1 receptors[1]) are a class of purinergic G protein-coupled receptors with adenosine as the ...
Receptorji P1 imajo podtipe A1, A2a, A2b in A3 (A je ostalo od stare nomenklature, kot adenozinski receptor) in vsi so ... Gajewski E, Steckler D, Goldberg R (1986). "Thermodynamics of the hydrolysis of adenosine 5'-triphosphate to adenosine 5'- ... 1995). "Adenosine 5'-(gamma-thiotriphosphate): an ATP analog that should be used with caution in muscle contraction studies". ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14) ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom.[1] ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ...
腺苷酸(英语:Adenosine receptor) (A1, A2A, A2B, A3) · P2Y(英语:P2Y receptor) (1(英语:P2RY1), 2(英语:P2RY2), 4(英语:P2RY4), 5(英语:LPAR6), 6(英语: ... 乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺(英语:Dopamine receptor) (D1, D2, D3, D4, D5) · 组织胺(英语:Histamine receptor) (H1, H2, H3, H4) · 褪黑素( ... α1(英语:Alpha-1 adrenergic receptor) (A, B, D) · α2(英语:Alpha-2 adrenergic receptor) (A, B, C) · β1 · β2 · β3 ... 英语:Melatonin receptor) (1A, 1B, 1C) · 痕量胺相关受体 (1(英语:TAAR1), 2(英语:TAAR2), 3(英语:TAAR3), 5
"Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ... Prostaglandin E2 receptor 4 (EP4). അവലംബം[തിരുത്തുക]. *↑ 1.0 1.1 1.2 GRCh38: Ensembl release 89: ENSG00000050628 - Ensembl, May ... "EP3-2 receptor mRNA expression is reduced and EP3-6 receptor mRNA expression is increased in gravid human myometrium". Journal ...
... (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.[5] ... "Galanin Receptors: GAL1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it. *v ... galanin receptor activity. • protein binding. Cellular component. • integral component of membrane. • membrane. • plasma ...
... which focuses on blocking the adenosine A2A receptor, in a deal worth up to $510 million.[51] In the same month the company's ... "Eolas and AstraZeneca Agree to Develop Orexin-1 Receptor Antagonist for Multiple Indications". GEN.. ... CD19 directed chimeric antigen receptor T-cell candidates.[47] In late June the company announced it has entered into a ... month the company announced it would partner with Orca Pharmaceuticals to develop retinoic acid-related orphan nuclear receptor ...
2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system.". J. Comp ... "The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia.". J. Biol. ... "Adenosine Receptors: A2B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... 2001). "Adenosine A2B receptors behave as an alternative anchoring protein for cell surface adenosine deaminase in lymphocytes ...
Taste receptor 2 member 38 is a protein that in humans is encoded by the TAS2R38 gene. TAS2R38 is a bitter taste receptor; ... G-protein coupled receptor activity. • signal transducer activity. • bitter taste receptor activity. ... TAS2R38, PTC, T2R38, T2R61, taste 2 receptor member 38, THIOT. External IDs. OMIM: 607751 MGI: 2681306 HomoloGene: 47976 ... Fischer A, Gilad Y, Man O, Pääbo S (2005). "Evolution of bitter taste receptors in humans and apes". Mol. Biol. Evol. 22 (3): ...
leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... "Leukotriene Receptors: CysLT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Cysteinyl leukotriene receptor 2, also termed CYSLTR2, is a receptor for cysteinyl leukotrienes (LT) (see leukotrienes# ... G-protein coupled peptide receptor activity. • signal transducer activity. • G-protein coupled receptor activity. • ...
The bombesin receptors are a group of G-protein coupled receptors which bind bombesin.. Three bombesin receptors are currently ... BB1, previously known as Neuromedin B receptor NMBR. BB2, previously known as Gastrin-releasing peptide receptor GRPR. BB3, ... previously known as Bombesin-like receptor 3 BRS3. External links[edit]. *. "Bombesin Receptors". IUPHAR Database of Receptors ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ...
adenylate cyclase-activating G-protein coupled receptor signaling pathway. • G-protein coupled receptor signaling pathway. • ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ... G-protein coupled receptor activity. Cellular component. • plasma membrane. • membrane. • integral component of membrane. • ... Probable G-protein coupled receptor 26 is a protein that in humans is encoded by the GPR26 gene.[5] ...
mineralocorticoid receptor activity. • steroid binding. • G-protein coupled receptor activity. • steroid hormone receptor ... Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... G protein-coupled estrogen receptor 1 (GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans ... "Estrogen (G protein coupled) Receptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and ...
"Tachykinin Receptors: NK3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... tachykinin receptor activity. • G-protein coupled receptor activity. • signal transducer activity. • protein binding. ... "Entrez Gene: TACR3 tachykinin receptor 3".. *^ Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from ... tachykinin receptor signaling pathway. • positive regulation of flagellated sperm motility. • G-protein coupled receptor ...
There is no 5-HT1C receptor, as it was reclassified as the 5-HT2C receptor.[2] For more information, please see the respective ... The 5-HT1 receptors are a subfamily of the 5-HT serotonin receptors that bind to the endogenous neurotransmitter serotonin ( ... 5-HT7 receptor. References[edit]. *^ Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey ... "HTR2C 5-hydroxytryptamine receptor 2C [ Homo sapiens (human) ]". NCBI. 19 Mar 2017. Retrieved 26 Mar 2017.. ...
Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as ... All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ... There are 9 established prostanoid receptors. The following table gives these receptors: a) full name; b) shortened names; c) ... "Prostanoid receptors - G protein-coupled receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.. ...
Rats rely heavily on olfactory sensory input from olfactory receptors for behavioral attitudes.[28] Studies show that bilateral ... The olfactory tubercle has been shown to be concerned primarily with the reception of sensory impulses from olfactory receptors ... receptor D3 is abundant in this two areas [6]). In addition, the OT contains tightly packed cell clusters known as the islands ... makes it likely to be involved in several psychiatric disorders in which olfaction and dopamine receptors are affected. Many ...
"Structure of an agonist-bound human A2A adenosine receptor". Science. 332 (6027): 322-7. doi:10.1126/science.1202793. PMC ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... is a receptor that can bind with stimulative signal molecules, while inhibitory hormone receptor (Ri) is a receptor that can ... Wikimedia Commons has media related to G protein-coupled receptors.. *G-protein-coupled+receptors at the US National Library of ...
... an adenosine A2A receptor antagonist which is in Phase I clinical trials for non-small cell lung cancer, from Palobiofarma.[65] ...
The dopamine receptor D4 is a G protein-coupled receptor encoded by the DRD4 gene on chromosome 11 at 11p15.5.[5] ... dopamine neurotransmitter receptor activity. • G-protein coupled receptor activity. • protein binding. • dopamine binding. • ... "Dopamine Receptors: D4". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. ... dopamine receptor signaling pathway. • G-protein coupled receptor signaling pathway. • adenylate cyclase-inhibiting dopamine ...
G-protein coupled receptor activity. • signal transducer activity. • taste receptor activity. • bitter taste receptor activity ... This gene product belongs to the family of candidate taste receptors that are members of the G-protein-coupled receptor ... Taste receptor. References[edit]. *^ a b c ENSG00000261984, ENSG00000276541 GRCh38: Ensembl release 89: ENSG00000212127, ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ...
... increasing the intracellular concentration of the second messenger cyclic adenosine monophosphate (cAMP).[6] ... μ-opioid receptors. ↑μ-opioid receptors. ↑κ-opioid receptors. ↑μ-opioid receptors. ↑μ-opioid receptors. No change. No change. [ ... The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 receptors are ... Dopamine receptor D1 and Dopamine receptor D5 are Gs coupled receptors that stimulate adenylyl cyclase to produce cAMP, ...
"Frizzled Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.. ... Frizzled is a family of G protein-coupled receptor proteins[2] that serves as receptors in the Wnt signaling pathway and other ... Malbon CC (2004). "Frizzleds: new members of the superfamily of G-protein-coupled receptors". Front. Biosci. 9: 1048-58. doi: ... Vantictumab is a monoclonal antibody against five frizzled receptors that is under development for the treatment of cancer. ...
... with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid ... prostaglandin D receptor activity. • G-protein coupled receptor activity. • prostaglandin J receptor activity. • prostaglandin ... "Prostanoid Receptors: DP2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... G-protein coupled receptor signaling pathway. • adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway. • G- ...
As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all ... The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This ... "Entrez Gene: ADORA2A adenosine A2A receptor". Ohta A, Sitkovsky M (2001). "Role of G-protein-coupled adenosine receptors in ...
Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine ... adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti- ... A2A receptors are G-protein coupled receptor (GPCR) that increases cyclic adenosine monophosphate (cAMP). These receptors are ... It is believed it acts as an adenosine A2A receptor neutral antagonist or as an inverse agonist. Caffeines A2A receptor ...
A2A adenosine receptor protects tumors from antitumor T cells. Akio Ohta, Elieser Gorelik, Simon J. Prasad, Franca Ronchese, ... A2A adenosine receptor protects tumors from antitumor T cells. Akio Ohta, Elieser Gorelik, Simon J. Prasad, Franca Ronchese, ... A2A adenosine receptor protects tumors from antitumor T cells. Akio Ohta, Elieser Gorelik, Simon J. Prasad, Franca Ronchese, ... The A2A adenosine receptor (A2AR) has been shown to be a critical and nonredundant negative regulator of immune cells in ...
Structure-based discovery of A2A adenosine receptor ligands.. Carlsson J1, Yoo L, Gao ZG, Irwin JJ, Shoichet BK, Jacobson KA. ... adenosine receptor, based on complementarity to its recently determined structure. The A(2A) adenosine receptor signals in the ... Structures of Known Agonists (1−3) and Antagonists (4−6) of the A2A Adenosine Receptor ... Receptor, Adenosine A2A/drug effects*. *Receptor, Adenosine A2A/metabolism. *Receptors, G-Protein-Coupled ...
Rabbit polyclonal Adenosine Receptor A2a antibody. Validated in WB, IHC, ICC and tested in Mouse, Human. Cited in 21 ... Anti-Adenosine Receptor A2a antibody. See all Adenosine Receptor A2a primary antibodies. ... All lanes : Anti-Adenosine Receptor A2a antibody (ab3461) at 1/500 dilution. Lane 1 : Human placenta cell lysate. Lane 2 : ... Anti-Adenosine Receptor A2a antibody [EPR23731-50] (ab260032) *Research with confidence - consistent and reproducible results ...
Cloning and expression of the A2a adenosine receptor from guinea pig brain.. Meng F1, Xie GX, Chalmers D, Morgan C, Watson SJ ... demonstrate typical characteristics of the A2 type adenosine receptor. The messenger RNA (mRNA) of this A2 receptor is found in ... A full-length complementary DNA (cDNA) clone encoding the guinea pig brain A2 adenosine receptor has been isolated by ... The pharmacological profile and anatomical distribution of this receptor indicate that it is of the A2a subtype. This work ...
J:243585 Riff R, et al., Systemic inflammatory response syndrome-related lymphopenia is associated with adenosine A1 receptor ...
References for Abcams Recombinant Human Adenosine Receptor A2a protein (ab126024). Please let us know if you have used this ...
... mediated formation of adenosine is critical for the striatal adenosine A2A receptor functions. J Neurosci 33:11390-11399. https ... Quarta D, Ferré S, Solinas M et al (2004) Opposite modulatory roles for adenosine A1 and A2A receptors on glutamate and ... Phillis JW (1995) The effects of selective A1 and A2a adenosine receptor antagonists on cerebral ischemic injury in the gerbil ... DallIgna OP, Porciúncula LO, Souza DO et al (2003) Neuroprotection by caffeine and adenosine A2A receptor blockade of beta- ...
The investigators hypothesize, that adenosine can activate BAT, and that adenosine A2A receptor density changes when BAT is ... A2A receptor density in BAT [ Time Frame: Effect within 3 hours ]. Density of A2A receptors in BAT measured with [11C]-TMSX PET ... Adenosine and A2A Receptors in Human Brown Adipose Tissue (AdenoBAT). The safety and scientific validity of this study is the ... Another PET radiotracer [11C]TMSX is used to quantify adenosine A2A receptor density of BAT, WAT and muscle in room temperature ...
1996) Opposing actions of adenosine A2a receptor and dopamine D2 receptor activation on GABA release in the basal ganglia: ... Breeding of A2A adenosine receptor knock-out mice. The A2A adenosine receptor knock-out (A2A KO) mouse line was generated in a ... 1995) Adenosine A2A receptor stimulation enhances striatal extracellular glutamate levels in rats. Eur J Pharmacol 287:215-217. ... 1997) Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2a receptor. Nature 388:674-678. ...
Adenosine A2A receptor (A2AR) is one of the G protein-coupled receptors. The protein uses adenosine as the preferred endogenous ... Arousal effect of caffeine depends on adenosine A2A receptors in the shell of the nucleus accumbens. J Neurosci. 2011 Jul 6;31( ... Agonist-bound adenosine A(2A) receptor structures reveal common features of GPCR activation. Nature. 2011 May 18. PMID:21593763 ... For details see G protein-coupled receptor. A2AR is blocked by producing the arousal effect.[2] For details see Caffeine. ...
However, the roles of astrocytic Gs-coupled receptors in cognitive function are not known. We found that humans with ... Astrocytes express a variety of G protein-coupled receptors and might influence cognitive functions, such as learning and ... Astrocytic adenosine receptor A2A and Gs-coupled signaling regulate memory Nat Neurosci. 2015 Mar;18(3):423-34. doi: 10.1038/nn ... had increased levels of the Gs-coupled adenosine receptor A2A in astrocytes. Conditional genetic removal of these receptors ...
Purinergic P2 receptors trigger adenosine release leading to adenosine A2A receptor activation and facilitation of long-term ... Purinergic P2 receptors trigger adenosine release leading to adenosine A2A receptor activation and facilitation of long-term ... or adenosine A2a receptor agonist-induced sleep [8].. *However, the rats perfused with 50 microM CGS21680, an adenosine A2A ... Effects of an adenosine A2A receptor blockade in the nucleus accumbens on locomotion, feeding, and prepulse inhibition in rats. ...
Adenosine A2A receptor and dopamine D3 receptor interactions: evidence of functional A2A/D3 heteromeric complexes. Torvinen, M ... and mice treated with adenosine A2A receptor antagonist [11].. *RESULTS: Adenosine A2A receptor occupancy promoted collagen ... a selective adenosine A2A receptor agonist, affected nucleoside release [22].. *The selective adenosine A2A receptor antagonist ... Adenosine A2A receptor and dopamine D3 receptor interactions: evidence of functional A2A/D3 heteromeric complexes [21]. ...
11C]-labeled form of ten A2a adenosine receptor specific 8-styryl-7-methyl-xanthine derivatives ([11C]-caffeines) were ... 11C]-labeled form of ten A2a adenosine receptor specific 8-styryl-7-methyl-xanthine derivatives ([11C]-caffeines) were ... These labeled ligands may facilitate the positron emission tomographic (PET) investigation of adenosine A2a receptors. ... 11C]-labeling of some caffeine derivatives for mapping adenosine A2a receptors by PET technique. ...
This process involves the activation of A2A adenosine receptors (A2AAR) in human umbilical vein endothelial cells (HUVECs). ... adenosine transport inhibitor) and/or adenosine receptors agonist/antagonists. We also determined hCAT-1 protein and mRNA ... Insulin and NBTI increased the extracellular adenosine concentration, the maximal velocity for L-arginine transport without ... Adenosine causes vasodilation of human placenta vasculature by increasing the transport of arginine via cationic amino acid ...
Of the four known adenosine receptors (A1, A2A, A2B, and A3), A1 receptor (A1R) and A2A receptor (A2AR) are primarily ... Adenosine A2A-dopamine D2 receptor-receptor heteromerization: qualitative and quantitative assessment by fluorescence and ... we demonstrate that heteromerization of adenosine A1 receptors (A1Rs) and A2A receptors (A2ARs) allows adenosine to exert a ... Rosin DL, Hettinger BD, Lee A, Linden J (2003) Anatomy of adenosine A2A receptors in brain: morphological substrates for ...
Adenosine A2A Receptor Activation Prevents Wear Particle-Induced Osteolysis Message Subject. (Your Name) has forwarded a page ... Adenosine A2A Receptor Activation Prevents Wear Particle-Induced Osteolysis. By Aránzazu Mediero, Sally R. Frenkel, Tuere ... Adenosine A2A Receptor Activation Prevents Wear Particle-Induced Osteolysis. By Aránzazu Mediero, Sally R. Frenkel, Tuere ... An adenosine A2A receptor agonist prevents osteolysis caused by polymeric wear particles in mouse calvaria. ...
Compare Adenosine A2a Receptor ELISA Kits and find the right product on antibodies-online.com. ... Order Adenosine A2a Receptor ELISA Kits for many Reactivities. Dog, Human, Mouse and more. ... adenosine A2a receptor , adenosine receptor A2a , adenosine receptor A2a.1 , A2a adenosine receptor , adenosine receptor A2a- ... Browse our Adenosine A2a Receptor (ADORA2A) ELISA Kits. Full name:. Adenosine A2a Receptor ELISA Kits (ADORA2A). On www. ...
Adenosine A2A Receptor Agonist Polydeoxyribonucleotide Alleviates Interstitial Cystitis-Induced Voiding Dysfunction by ... On the other hand, co-treatment of adenosine A2A receptor antagonist DMPX with adenosine A2A receptor agonist PDRN did not ... 17 There are four subtypes of adenosine receptors such as A1, A2A, A2B, and A3. Among them, the adenosine A2A receptor is ... Targeting G protein-coupled A2a adenosine receptors to engineer inflammation in vivo. Int J Biochem Cell Biol. 2003;35(4):410- ...
In particular, inhibition of adenosine A2A receptors (A2AR) in animal models for hepatic and skin fibrosis resulted in a ... These data suggest that adenosine the A2AR plays a crucial role in the formation of myocardial fibrosis in a variety of cardiac ... In addition, pharmacologic adenosine A2AR inhibition using the antagonist ZM241385 demonstrated a partial rescue of myocardial ... Further, adenosine A2AR KO mice undergoing transverse aortic constriction demonstrated significantly less fibrosis formation ...
Adenosine is released from metabolically active cells by facilitated diffusion, and is generated extracellularly by degradation ... Adenosine mediates its effects through four receptor subtypes: the A1, A2a, A2b and A3 receptors. The A2a receptor (A2aR) is ... Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2a receptor Nature. 1997 Aug 14;388(6643): ... Here we investigate the role of the A2a receptor by disrupting the gene in mice. We found that A2aR-knockout (A2aR-/-) mice ...
April 10 FirstCall/...Lexiscan is the first A2A adenosine receptor agonist shown to be safe...,CV,Therapeutics,and,Astellas, ... First A2A Adenosine Receptor Agonist Approved for Use as Pharmacolo... Stress Agent in Myocardial Perfusion Imaging- ...PALO ... The A2A adenosine receptor is the adenosine receptor subtype responsible for coronary vasodilation. ... Lexiscan is an A2A adenosine receptor agonist approved for use as a pharmacologic stress agent in radionuclide MPI studies in ...
... including the A2A adenosine receptor. Instead, as in β1AR and β2AR, the D/ERY motif in the A2A adenosine receptor participates ... also has high affinity for the A2A adenosine receptor (57). In a recent study on new antagonists for the A2A adenosine receptor ... The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist ... A) A surface rendering of the binding pocket for ZM241385 in the A2A adenosine receptor. Helical positions for A2A adenosine ( ...
Adenosine A2A receptors intrinsically regulate CD8+ T cells in the tumor microenvironment. Caglar Cekic and Joel Linden ... Adenosine A2A receptor (A2AR) blockade enhances innate and adaptive immune responses. However, mouse genetic studies have shown ... Adenosine A2A receptors intrinsically regulate CD8+ T cells in the tumor microenvironment ... Adenosine A2A receptors intrinsically regulate CD8+ T cells in the tumor microenvironment ...
Role of A2a extracellular adenosine receptor-mediated signaling in adenosine-mediated inhibition of T-cell activation and ... Gene dose effect reveals no Gs-coupled A2A adenosine receptor reserve in murine T-lymphocytes: studies of cells from A2A- ... Memory of extracellular adenosine A2A purinergic receptor-mediated signaling in murine T cells. J. Biol. Chem. 272:25881. ... Activation of A2A adenosine receptors inhibits expression of α4/β1 integrin (very late antigen-4) on stimulated human ...
Adenosine receptor A2a. A. 329. Homo sapiens. Mutation(s): 8 Gene Names: ADORA2A, ADORA2. ... Thermostabilised Adenosine A2A receptor in complex with 6-(2,6-Dimethylpyridin-4-yl)-5-phenyl-1,2,4-triazin-3-amine. *DOI: ... Discovery of 1,2,4-Triazine Derivatives as Adenosine A(2A) Antagonists using Structure Based Drug Design. Congreve, M., Andrews ... receptor. The X-ray crystal structures of compounds 4e and 4g bound to the GPCR illustrate that the molecules bind deeply ...
Evaluation of [123I]MNI-420 and SPECT as a Marker of the Adenosine A2a Receptor in PD, HD and Healthy Subjects. (MNI-420). The ... Evaluation of [123I]MNI-420 and SPECT as a Marker of the Adenosine A2a Receptor in Subjects With Parkinson Disease, Huntington ... and similarly aged healthy subjects as a potential imaging biomarker of adenosine receptor type A2a (A2aR) in brain ... Adenosine. Analgesics. Sensory System Agents. Peripheral Nervous System Agents. Physiological Effects of Drugs. Anti-Arrhythmia ...
The adenosine metabolite inosine is a functional agonist of the adenosine A2A receptor with a unique signaling bias. Cell. ... Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature. 474:521-525. doi:10.1038/ ... Differential requirement for A2a and A3 adenosine receptors for the protective effect of inosine in vivo. Blood. 102:4472-4478. ... Adenosine A2A receptor activation inhibits T helper 1 and T helper 2 cell development and effector function. FASEB J. 22:3491- ...
  • The A2A adenosine receptor (A2AR) has been shown to be a critical and nonredundant negative regulator of immune cells in protecting normal tissues from inflammatory damage. (pnas.org)
  • We propose to target the hypoxia→adenosine→A2AR pathway as a cancer immunotherapy strategy to prevent the inhibition of antitumor T cells in the tumor microenvironment. (pnas.org)
  • Thus, although using the hypoxia→adenosine→A2AR pathway inhibitors may improve antitumor immunity, the recruitment of this pathway by selective drugs is expected to attenuate the autoimmune tissue damage. (pnas.org)
  • We hypothesized that cancerous tissues are protected from antitumor T cells because of immunosuppressive signaling via T cell A2A adenosine receptor (A2AR) ( 15 - 17 ) activated by extracellular adenosine produced from hypoxic tumor ( Fig. 1 a ). (pnas.org)
  • Indeed, hypoxic cancerous tissues may be protected by the same hypoxia→adenosine→A2AR pathway that was recently shown to be critical and nonredundant in preventing excessive damage of normal tissues by overactive immune cells in vivo ( 18 ). (pnas.org)
  • a ) It is assumed that adenosine and A2AR, which inhibit overactive immune cells to protect normal tissues ( 18 ), may protect malignant tissues from antitumor T cells. (pnas.org)
  • Recently it was found that adenosine activates murine and human brown adipocytes, and recruits beiging of white fat via adenosine A2A receptors (A2AR). (clinicaltrials.gov)
  • Adenosine A2A receptor (A2AR) is one of the G protein-coupled receptors. (proteopedia.org)
  • In particular, inhibition of adenosine A2A receptors (A2AR) in animal models for hepatic and skin fibrosis resulted in a reduction of fibrosis formation. (bl.uk)
  • The specific hypothesis of this investigation was that myocardial stress results in increased interstitial levels of adenosine, which activate cardiac fibroblasts via adenosine A2AR. (bl.uk)
  • Accordingly, the specific objective of this investigation was to delineate the role of adenosine A2AR signalling in the development of myocardial fibrosis. (bl.uk)
  • Further, adenosine A2AR KO mice undergoing transverse aortic constriction demonstrated significantly less fibrosis formation compared to constricted WT mice. (bl.uk)
  • In addition, pharmacologic adenosine A2AR inhibition using the antagonist ZM241385 demonstrated a partial rescue of myocardial fibrosis in both TAC and E99K animals. (bl.uk)
  • These data suggest that adenosine the A2AR plays a crucial role in the formation of myocardial fibrosis in a variety of cardiac pathologies and that this pathway is susceptible to pharmacologic modulation. (bl.uk)
  • The A2a receptor (A2aR) is abundant in basal ganglia, vasculature and platelets, and stimulates adenylyl cyclase. (nih.gov)
  • Adenosine A2A receptor (A2AR) blockade enhances innate and adaptive immune responses. (aacrjournals.org)
  • The adenosine A2A receptor (A2AR) appears to be a potential target for the improvement of behavioral, inflammatory, immune, and neurological disorders. (sigmaaldrich.com)
  • In the present study, using wild type and adenosine A 2A receptor (A2AR) null mice, we investigated whether A2ARs, known to mediate anti-inflammatory signals in macrophages, participate in the apoptotic cell-mediated immunosuppression. (pubmedcentralcanada.ca)
  • Adenosine A2a receptor (A2aR or ADORA2A) stably expressed in HEK-293 cells. (nordicbiosite.com)
  • A2aR is a member of the seven transmembrane G protein-coupled receptor (GPCR) family. (nordicbiosite.com)
  • The level of cAMP correlates with the respective adenosine (agonist) level, and the cell line can be used to measure the EC50 and IC50 values of A2aR agonists or antagonists in a quantitative manner. (nordicbiosite.com)
  • Binding of extracellular adenosine ligand or its stable analog NECA (5'-(N-Ethylcarboxamido) adenosine) to the A2aR expressed on the surface of this cell line induces cAMP expression. (nordicbiosite.com)
  • A highly potent, selective, non-xanthine adenosine A2A receptor antagonist (K i = 800 pM for human adenosine A2AR stably expressed in HEK-293 cells). (merckmillipore.com)
  • In one type of interaction, A2AR and D2R are forming heteromers and, by means of an allosteric interaction, A2AR counteracts D2R-mediated inhibitory modulation of the effects of NMDA receptor stimulation in the striatopallidal neuron. (ub.edu)
  • Adenosine is recognised to mediate anti-inflammatory effects via the adenosine A2a receptor (A2aR), as shown in experimental models of arthritis. (biomedcentral.com)
  • Among the four G-protein-coupled receptors activated by adenosine, adenosine receptor 2a (A2aR) is responsible for most of the known immunoregulatory effects of adenosine in the immune system, preventing overly exuberant immune responses that can lead to collateral tissue damage [ 4 ]. (biomedcentral.com)
  • This blocks tumor-released adenosine from interacting with A2AR and prevents the adenosine/A2AR-mediated inhibition of T-lymphocytes. (wikimd.org)
  • A2AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of T-cells and, upon activation by adenosine, inhibits T-cell proliferation and activation. (wikimd.org)
  • VT and BPND were also obtained after preblocking with unlabeled preladenant (1 mg/kg), A2AR-selective KW-6002 (0.5-1 mg/kg), and nonselective adenosine receptor antagonist caffeine (2.5-10 mg/kg). (vumc.nl)
  • Using a yeast two-hybrid screen, we identified α-actinin, a major F-actin-cross-linking protein, as a binding partner for the C-terminal domain of the adenosine A2A receptor (A2AR). (cardiff.ac.uk)
  • A2AR activation by agonist induced the internalization of the receptor by a process that involved rapid β-arrestin translocation from the cytoplasm to the cell surface. (cardiff.ac.uk)
  • A2AΔCTR, a mutant version of A2AR that lacks the C-terminal domain and does not interact with α-actinin, was not able to internalize when activated by agonist. (cardiff.ac.uk)
  • The non-selective adenosine receptor agonist (adenosine-5′N-ethylcarboxamide, NECA) and the A2AR agonist (CGS21680) stimulated cell proliferation by up to 20-40% which was attenuated by A2B (PSB603 and MRS1754) and A2A (SCH442416) receptor selective antagonists but not by the A1 receptor antagonist (PSB36). (cf.ac.uk)
  • The adenosine A2A receptor (A2AR) is a particularly interesting example, as it has an exceptionally long intracellular carboxyl terminus, which is predicted to be mainly disordered. (jpt.com)
  • This study is aimed to explore the effects of Adenosine A2a receptors (A2aR) on hypoxia-induced pulmonary hypertension (HPH) via mitochondrial ATP-sensitive potassium channels (MitoKATP) in vivo and in vitro. (archivesofmedicalscience.com)
  • The use of antagonists, including caffeine, or targeting the A2 receptors by siRNA pretreatment of T cells improved the inhibition of tumor growth, destruction of metastases, and prevention of neovascularization by antitumor T cells. (pnas.org)
  • The A(2A) adenosine receptor signals in the periphery and the CNS, with agonists explored as anti-inflammatory drugs and antagonists explored for neurodegenerative diseases. (nih.gov)
  • 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)
  • However the development of more highly selective A2A ligands has led towards other applications, with the most significant focus of research currently being the potential therapeutic role for A2A antagonists in the treatment of Parkinson's disease. (wikipedia.org)
  • Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. (wikipedia.org)
  • Notable adenosine A2A receptor antagonists include caffeine, theophylline and istradefylline. (wikipedia.org)
  • Recently, selective A2A receptor antagonists are used in treatment of diseases such as Parkinson's disease, ischemia, and multiple sclerosis. (wikipedia.org)
  • Selective A2A receptor antagonists are believed to be neuroprotectors for their ability to reduce neuroinflammation. (wikipedia.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)
  • Trial results indicated that the viability of A2A receptor antagonists have potential advantages over the current standard treatments for Parkinson's disease. (wikipedia.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)
  • 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)
  • In 1992, the therapeutic potential for both agonists and antagonists of the adenosine receptors was highlighted for A2 receptors, and in 2001 the therapeutic potential for adenosine antagonists was highlighted. (wikipedia.org)
  • Broad reviews from 2006 have been focusing on adenosine receptors as therapeutic targets, adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti-inflammatories and many more. (wikipedia.org)
  • Several attempts have been made by using virtual screening to identify potent A2A adenosine receptor antagonists. (wikipedia.org)
  • Potent, ligand efficient, selective, and orally efficacious 1,2,4-triazine derivatives have been identified using structure based drug design approaches as antagonists of the adenosine A(2A) receptor. (rcsb.org)
  • The absence of the A2A receptor on blood-brain barrier cells is similar to the effect of pharmacologically blocking the receptor with antagonists [drugs], which also protected mice from MS-like disease," Bynoe said. (scitechdaily.com)
  • Conclusion: Finally, the proposed methodology is successfully applied to the generation of ensemble models for the ligand-based virtual screening of dual target A2A adenosine receptor antagonists and MAO-B inhibitors as potential Parkinson's disease therapeutics. (chemaxon.com)
  • Microglial cells or rats were treated with or without lipopolysaccharide (LPS) in the presence or absence of adenosine, adenosine receptor agonists/antagonists, or CBD. (arvojournals.org)
  • Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists. (semanticscholar.org)
  • Modulation of paracetamol antinociception by caffeine and by selective adenosine A2 receptor antagonists in mice. (semanticscholar.org)
  • After 24 h of incubation, hearts were isolated and randomly assigned to a group with or without adenosine receptor (Ador) antagonists (SCH 58261 and MRS 1706) administered before reperfusion. (uni-regensburg.de)
  • Adenosine A2A receptor antagonists have been shown to decrease the motor symptoms associated with PD, and are also potentially neuroprotective. (nwu.ac.za)
  • These results prompted this pilot study, which aimed to investigate the potential of the structurally related 3,4-dihydropyrimidin-2(1H)-ones (dihydropyrimidones) and 2-amino-1,4-dihydropyrimidines as adenosine A1 and A2A antagonists. (nwu.ac.za)
  • In this pilot study, a series of 3,4-dihydropyrimidones and 2-amino-1,4-dihydropyrimidines were synthesised and evaluated as adenosine A1 and A2A antagonists. (nwu.ac.za)
  • Since several adenosine A2A antagonists also exhibit MAO inhibitory activity, the MAO-inhibitory activity of selected derivatives was also assessed. (nwu.ac.za)
  • Thus, A(2A) receptor antagonists may be useful therapeutic agents for alleviating ethylic coma. (archives-ouvertes.fr)
  • Results of experiments performed with selective adenosine receptor antagonists indicated that functional effects of ATL313 were via stimulation of A 2A receptors. (elsevier.com)
  • The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. (wikipedia.org)
  • On www.antibodies-online.com are 24 Adenosine A2a Receptor (ADORA2A) ELISA Kits from 10 different suppliers available. (antibodies-online.com)
  • These data demonstrate a role of adenosine A2A receptors for sleep in humans, and suggest that a common variation in ADORA2A contributes to subjective and objective responses to caffeine on sleep. (uzh.ch)
  • ADORA2A: one of several receptor subtypes for adenosine. (mybiosource.com)
  • A read-through transcript composed of the upstream SPECC1L (sperm antigen with calponin homology and coiled-coil domains 1-like) and ADORA2A (adenosine A2a receptor) gene sequence has been identified, but it is thought to be non-coding. (sinobiological.com)
  • The ELISA Genie Dog Adenosine receptor A2a (ADORA2A) ELISA Kit can assay for Dog Adenosine receptor A2a in the following samples: serum, blood, plasma, cell culture supernatant and other related supernatants and tissues. (elisagenie.com)
  • How do our Dog Adenosine receptor A2a (ADORA2A) ELISA Kits work? (elisagenie.com)
  • The ELISA Genie Dog Adenosine receptor A2a (ADORA2A) ELISA Kits are designed for the quantitative measurement of analytes in a wide variety of samples. (elisagenie.com)
  • The amount of bound Dog Adenosine receptor A2a is proportional to the signal generated by the reaction meaning the Dog Adenosine receptor A2a (ADORA2A) ELISA Kit assay gives you a quantitative measurement of the analyte in your samples. (elisagenie.com)
  • Human ADORA2A / Adenosine Receptor A2a protein ELISA Kit - InformationThe ELISA Genie ADORA2A / Adenosine Receptor A2a protein ELISA Kit can assay for ADORA2A / Adenosine Receptor A2a protein in the. (elisagenie.com)
  • Mouse ADORA2A / Adenosine Receptor A2a protein ELISA Kit - InformationThe ELISA Genie Mouse ADORA2A / Adenosine Receptor A2a protein ELISA Kit can assay for Mouse ADORA2A / Adenosine Receptor A2a. (elisagenie.com)
  • Intra-assay Precision (Precision within an assay): 3 samples with low, middle and high level Adenosine A2a Receptor (ADORA2a) were tested 20 times on one plate, respectively. (biomatik.com)
  • Inter-assay Precision (Precision between assays): 3 samples with low, middle and high level Adenosine A2a Receptor (ADORA2a) were tested on 3 different plates, 8 replicates in each plate. (biomatik.com)
  • This assay has high sensitivity and excellent specificity for detection of Adenosine A2a Receptor (ADORA2a). (biomatik.com)
  • The microtiter plate provided in this kit has been pre-coated with an antibody specific to Adenosine A2a Receptor (ADORA2a). (biomatik.com)
  • Standards or samples are then added to the appropriate microtiter plate wells with a biotin-conjugated antibody specific to Adenosine A2a Receptor (ADORA2a). (biomatik.com)
  • After TMB substrate solution is added, only those wells that contain Adenosine A2a Receptor (ADORA2a), biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. (biomatik.com)
  • The concentration of Adenosine A2a Receptor (ADORA2a) in the samples is then determined by comparing the O.D. of the samples to the standard curve. (biomatik.com)
  • Description: A competitive ELISA for quantitative measurement of Human Adenosine receptor A2a(ADORA2A) in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. (ecopiabio.com)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Adenosine A2a Receptor (ADORA2a) in Tissue homogenates and other biological fluids. (ecopiabio.com)
  • The gene encodes a protein which is one of several receptor subtypes for adenosine. (wikipedia.org)
  • Adenosine mediates its effects through four receptor subtypes: the A1, A2a, A2b and A3 receptors. (nih.gov)
  • Extracellular adenosine plays an important role in physiology and initiates most of its effects through the activation of four guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) subtypes, A 1 , A 2A , A 2B , and A 3 ( 1 , 2 ). (sciencemag.org)
  • These receptor subtypes are primarily coupled to the cyclic adenosine monophosphate (cAMP) second-messenger system, and each has its own unique pharmacological profile. (sciencemag.org)
  • At least three of the four adenosine receptor subtypes (A 1 , A 2A , and A 2B ) are blocked by naturally occurring methylxanthines, such as caffeine, with modest affinity. (sciencemag.org)
  • Development of more selective compounds for adenosine receptor subtypes could provide a class of therapeutics for treating numerous human maladies, such as pain ( 5 ), Parkinson's disease ( 7 , 13 ), Huntington's disease ( 14 ), asthma ( 15 ), seizures ( 16 ), and many other neurological disorders ( 14 , 17 ). (sciencemag.org)
  • Extracellular adenosine initiates transmembrane signaling through four subtypes of G protein-coupled adenosine receptors (AR), A 1 , A 2A , A 2B , and A 3 ( 8 ). (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)
  • Cells that express one or more of the four G protein-coupled adenosine receptors (AR) subtypes (A1, A2A, A2B, and/or A3) have the capacity to respond to extracellular adenosine. (jimmunol.org)
  • Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A 2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A 1 , A 2B , and A 3 . (ahajournals.org)
  • Four subtypes of adenosine receptors (ARs) have been identified among vertebrates so far ( A1 , A2A , A2B and A3 ). (axonmedchem.com)
  • Among adenosine receptor subtypes, the A2A receptor is one of the few GPCRs whose crystal structure is available. (fieldofscience.com)
  • The adenosine receptor (AR) subtypes expressed in rat retinal microglial cells were assessed by quantitative real-time RT-PCR. (arvojournals.org)
  • This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily, which is subdivided into classes and subtypes. (sinobiological.com)
  • The affinities (Ki-values between 0.6 mM and 38 mM) of a series of 1,4-dihydropyridine derivatives were previously illustrated for the adenosine A1, A2A and A3 receptor subtypes by Van Rhee and co-workers (1996). (nwu.ac.za)
  • Objective - To evaluate anti-inflammatory effects of several novel adenosine receptor agonists and to determine their specificity for various adenosine receptor subtypes on neutrophils, cells heterologously expressing equine adenosine receptors, or equine brain membranes. (elsevier.com)
  • Procedures - Radioligand binding experiments were performed to compare binding affinities of adenosine receptor agonists to equine adenosine A 1 , A 2A , and A 3 receptor subtypes. (elsevier.com)
  • Effects of these agonists on endotoxin-induced production of reactive oxygen species (ROS) by equine neutrophils and roles of specific adenosine receptor subtypes and cAMP production in mediating these effects were determined. (elsevier.com)
  • The main biochemical characteristic of the A 1 R-A 2A R heteromer is the ability of A 2A R activation to reduce the affinity of the A 1 R for agonists, providing a switch mechanism by which low and high concentrations of adenosine inhibit and stimulate, respectively, glutamatergic neurotransmission. (jneurosci.org)
  • Adenosine receptor agonists, including Lexiscan, induce arterial vasodilation and hypotension. (bio-medicine.org)
  • Recently, a new class of A 2A Ado receptor agonists was synthesized. (ahajournals.org)
  • Conclusions - ATL-193 and ATL-146e are highly potent and selective Ado A 2A receptor agonists with excellent potential for use as vasodilators for myocardial perfusion imaging. (ahajournals.org)
  • 5 The discovery of highly selective and relatively short-acting adenosine receptor A 2A agonists 6-9 has opened the possibility of a strategy for eliciting the desired coronary vasodilatation without producing side effects. (ahajournals.org)
  • Recently, a new class of selective adenosine A 2A receptor agonists has been synthesized at the University of Virginia. (ahajournals.org)
  • The A1 and A2a adenosine receptor agonists could increase proliferation of NPCs. (deepdyve.com)
  • This analog thus bypassed a common side effect associated with adenosine receptor agonists. (painresearchforum.org)
  • Mice lacking the Adenosine A2A Receptor are hypoalgesic, and have altered analgesic responses to Receptor -selective opioid agonists. (idexlab.com)
  • NON-TECHNICAL SUMMARY: This is a phase I SBIR proposal by Adenosine Therapeutics for 6 months of support to synthesize and evaluate novel compounds as agonists of equine A2A adenosine receptors. (sbir.gov)
  • Conclusions and Clinical Relevance - Results indicated that activation of A 2A receptors exerted anti-inflammatory effects on equine neutrophils and that stable, highly selective adenosine A 2A receptor agonists may be developed for use in management of horses and other domestic animals with septic and nonseptic inflammatory diseases. (elsevier.com)
  • 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)
  • 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)
  • This work, we investigated the effect of low-dose of caffeine on the ectonucleotidase activities, adenosine receptors content, and paying particular attention to its pro-survival effect during aging. (springer.com)
  • The content of A1 receptors did not change in any groups of mice, but the content of A2A receptors was reduced in hippocampus of mice that consumed caffeine. (springer.com)
  • Dall'Igna OP, Porciúncula LO, Souza DO et al (2003) Neuroprotection by caffeine and adenosine A2A receptor blockade of beta-amyloid neurotoxicity. (springer.com)
  • Arousal effect of caffeine depends on adenosine A2A receptors in the shell of the nucleus accumbens. (proteopedia.org)
  • The present study is the first indication that heteromerization of different receptors for the same modulator constitutes a unique way to presynaptically regulate neurotransmission and also is the first indication that A 1 R-A 2A R heteromers may be involved in the acute and chronic effects of caffeine. (jneurosci.org)
  • The adenosine class of heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs) mediates the important role of extracellular adenosine in many physiological processes and is antagonized by caffeine. (sciencemag.org)
  • Consumption of caffeine, a non-selective adenosine A 2A receptor (A 2A R) antagonist, reduces the risk of developing Alzheimer's disease (AD) and mitigates both amyloid and Tau lesions in transgenic mouse models of the disease. (frontiersin.org)
  • We will explore whether this polymorphism is associated with a different vasodilating response to the administration of adenosine and caffeine into the brachial artery. (bioportfolio.com)
  • The A2A adenosine receptor is an important GPCR, well-known for binding caffeine. (fieldofscience.com)
  • Studies in mice revealed that the disruption of sleep after caffeine is mediated by blockade of adenosine A2A receptors. (uzh.ch)
  • Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine. (semanticscholar.org)
  • Heart rate (HR), body temperature (Temp), locomotor activity (LA), and oxygen consumption (O(2)C) were studied in awake mice lacking one or both of the adenosine A(1) or A(2A) receptors (A(1)R or A(2A)R, respectively) using telemetry and respirometry, before and after caffeine administration. (semanticscholar.org)
  • Caffeine reduces hypnotic effects of alcohol through adenosine A2A receptor blockade. (semanticscholar.org)
  • The mechanism by which caffeine contributes to its antiparkinsonian effects by acting as either an Adenosine A2A Receptor ( A2A R) neutral antagonist or an inverse agonist is unresolved. (idexlab.com)
  • Here we show that caffeine is an A2A R inverse agonist in cell-based functional studies and in experimental parkinsonism. (idexlab.com)
  • Thus, we observed that caffeine triggers a distinct mode, opposite to A2A R agonist, of the Receptor 's activation switch leading to suppression of its spontaneous activity. (idexlab.com)
  • Overall, caffeine A2A R inverse agonism may be behind some of the well-known physiological effects of this substance both in health and disease. (idexlab.com)
  • Finally, the non-selective adenosine receptor antagonist caffeine (25 mg/kg) reduced ethanol-induced hypnotic effects. (archives-ouvertes.fr)
  • 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)
  • Agonist-bound adenosine A(2A) receptor structures reveal common features of GPCR activation. (proteopedia.org)
  • With an additional human GPCR structure, it is now possible to extend the analysis of structural differences as they pertain to receptor pharmacology, ligand recognition, and receptor activation across the members of the class A receptor family. (sciencemag.org)
  • We investigated the molecular basis of this process in the adenosine A 2A receptor (A 2A R), a prototypical G protein-coupled receptor (GPCR). (aspetjournals.org)
  • Here, we chose the human adenosine A 2A receptor (A 2A R), a prototypical GPCR, for such a mechanistic exploration. (aspetjournals.org)
  • 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)
  • Study reveals presence of adenosine A(2A) and A(2B (show ADRA2B ELISA Kits )) receptors as well as a role for them in lacrimal gland secretion, and especially in synergy with purinergic and cholinergic stimulation. (antibodies-online.com)
  • cardiovascular and neurohumoral effects by stimulation of specific adenosine receptors. (bioportfolio.com)
  • The endogenous nucleoside adenosine can induce various cardiovascular and neurohumoral effects by stimulation of specific adenosine receptors. (bioportfolio.com)
  • 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)
  • It was found that phosphorylation of the human A2AAR could be induced in HUVECs by treatment with PMA or by stimulation of endogenous histamine H1 receptors. (gla.ac.uk)
  • The aim of the present work is to investigate the effects of Adenosine A2A receptor stimulation on the expression of neutrophil activation markers and LFA-1 integrin-mediated adhesion to the ligand ICAM-1 using the agonist ATL313. (virginia.edu)
  • Pharmacological Preconditioning by Adenosine A2a Receptor Stimulation: Features of the Protected Liver Cell Phenotype. (sinobiological.com)
  • The sedative effects of ethanol are thought to result, in part, from the stimulation of inhibitory GABA receptors as well as the antagonism of glutamate's NMDA receptor subtype ( Roehrs and Roth, 2001 ). (nature.com)
  • Interestingly, A2AΔCTR did not show aggregation or clustering after agonist stimulation, a process readily occurring with the wild-type receptor. (cardiff.ac.uk)
  • Pretreatment strategy with adenosine A2A receptor agonist attenuates reperfusion injury in a preclinical porcine lung transplantation model. (antibodies-online.com)
  • Adenosine (Ado), a naturally occurring autacoid, exerts cardioprotective effects against myocardial ischemia and reperfusion injury, through activation of its receptors type 1 (A 1 ) and 2A (A 2A ). (elsevier.com)
  • A2A AR activation on BBB (show ALMS1 ELISA Kits ) endothelial cells offers a therapeutic window that can be fine-tuned for drug delivery to the brain and has potential as a CNS drug-delivery technology. (antibodies-online.com)
  • Lexiscan was designed to produce coronary vasodilation and increase coronary blood flow by activation of the A2A adenosine receptor. (bio-medicine.org)
  • The binding site highlights an integral role for the extracellular loops, together with the helical core, in ligand recognition by this class of GPCRs and suggests a role for ZM241385 in restricting the movement of a tryptophan residue important in the activation mechanism of the class A receptors. (sciencemag.org)
  • The A 2A adenosine subtype is linked to G s and G olf proteins, and upon receptor activation, the intracellular levels of cAMP increase. (sciencemag.org)
  • However, TCR-mediated IL-2 production ( 11 ), CD25 and CD69 expression ( 12 ), granule exocytosis, Fas ligand up-regulation ( 13 ), and cell proliferation ( 11 ) are modulated by the activation of cell surface adenosine receptors. (jimmunol.org)
  • Extracellular adenosine-triggered cAMP accumulation ( 14 ) and inhibition of activation-induced CD25 expression ( 15 ) were reported to be mediated by the A 2A AR. (jimmunol.org)
  • Inhibition of killer T cell activation by adenosine has been attributed to signaling through the A 3 AR ( 10 ). (jimmunol.org)
  • We found that macrophages engulfing apoptotic cells release adenosine in sufficient amount to trigger A2ARs, and simultaneously increase the expression of A2ARs, possibly via activation of activation of liver X receptor and peroxisome proliferators activated receptor δ. (pubmedcentralcanada.ca)
  • Although T cells express inhibitory adenosine A 2A receptors (A 2A R) that suppress their activation and inhibit immune killing of tumors, a role for myeloid cell A 2A Rs in suppressing the immune response to tumors has yet to be investigated. (aacrjournals.org)
  • Although extracellular ATP enhances immune cell chemotaxis and activation through engagement with P2 purinergic receptors, it is rapidly degraded to adenosine by ectonucleotidases. (aacrjournals.org)
  • Macrophages modulate their activation state by increasing the synthesis and secretion of ATP that in the tumor microenvironment is immunosuppressive due to its rapid catabolism into adenosine by CD39 and CD73 ( 6 ). (aacrjournals.org)
  • We found that activation of adenosine receptors affected the proliferation of NPCs. (deepdyve.com)
  • The majority of the anti-inflammatory effects of adenosine are mediated by signalling through the A2AAR and activation of the A2AAR has been shown to be protective in numerous models of inflammatory disease. (gla.ac.uk)
  • Effect of adenosine A2A receptor activation in murine models of respiratory disorders. (semanticscholar.org)
  • These presynaptic A2ARs heteromerize with A1 receptors (A1Rs) and their activation facilitates glutamate release. (ub.edu)
  • Activation did not require hydrolysis of AMP to adenosine by ectonucleotidases. (painresearchforum.org)
  • Our research unexpectedly suggested that some of the physiological effects of AMP (and AMP analogs) might be due to direct activation of adenosine receptors and independent of ectonucleotidases. (painresearchforum.org)
  • Flögel and colleagues reported that the anti-inflammatory effects of chet-AMP were due to hydrolysis to chet-adenosine by ecto-5'-nucleotidase (NT5E, also known as CD73) followed by activation of the adenosine A2A receptor. (painresearchforum.org)
  • In addition to TGF-β, macrophages engulfing apoptotic cells release adenosine in sufficient amount to trigger A2ARs, and simultaneously increase the expression of A2ARs, as a result of possible activation of LXR and PPARδ. (unideb.hu)
  • A(2A) receptors contribute to coronary vasodilation in response to cardiac ischemia via activation of K(V) and K(ATP) channels. (cusabio.com)
  • These results indicate that the activation of A(2A) receptors that follows an increase in extracellular adenosine levels caused by the administration of high doses of ethanol plays a role in its hypnotic effects. (archives-ouvertes.fr)
  • their activation leads to increased proliferation and secretion of chromogranin A. Targeting adenosine signal pathways, specifically inhibition of A2 receptors, may thus be a useful addition to the therapeutic management of neuroendocrine tumours. (cf.ac.uk)
  • The pharmacological profile and anatomical distribution of this receptor indicate that it is of the A2a subtype. (nih.gov)
  • The A2A adenosine receptor is the adenosine receptor subtype responsible for coronary vasodilation. (bio-medicine.org)
  • We have determined the crystal structure of the human A 2A adenosine receptor, in complex with a high-affinity subtype-selective antagonist, ZM241385, to 2.6 angstrom resolution. (sciencemag.org)
  • This protein, an adenosine receptor of A2A subtype, uses adenosine as the preferred endogenous agonist and preferentially interacts with the G(s) and G(olf) family of G proteins to increase intracellular cAMP levels. (sinobiological.com)
  • Finally, repeated l -DOPA treatment reversed the 6-OHDA-induced reduction of striatal dynorphin mRNA in WT but not A 2A KO mice, raising the possibility that the A 2A receptor may contribute to l -DOPA-induced behavioral sensitization by facilitating adaptations within the dynorphin-expressing striatonigral pathway. (jneurosci.org)
  • Conditional genetic removal of these receptors enhanced long-term memory in young and aging mice and increased the levels of Arc (also known as Arg3.1), an immediate-early gene that is required for long-term memory. (nih.gov)
  • Like humans with AD, aging mice expressing human amyloid precursor protein (hAPP) showed increased levels of astrocytic A2A receptors. (nih.gov)
  • Conditional genetic removal of these receptors enhanced memory in aging hAPP mice. (nih.gov)
  • Here we investigate the role of the A2a receptor by disrupting the gene in mice. (nih.gov)
  • In this study, the researchers used mice where the A2A adenosine receptor was knocked out and then infused those mice with normal immune cells from wild-type mice expressing the A2A adenosine receptor. (scitechdaily.com)
  • This produced chimeric mice expressing the A2A receptor on immune cells, but not on blood-brain barrier cells. (scitechdaily.com)
  • Without A2A receptor on blood-brain barrier cells, the normal immune cells failed to effectively infiltrate the central nervous system, and thus, these mice were protected and developed less severe symptoms of MS-like disease. (scitechdaily.com)
  • Depletion of CD8 + T cells or NK cells in tumor-bearing mice indicates that both cell types initially contribute to slowing melanoma growth in mice lacking myeloid A 2A receptors, but tumor suppression mediated by CD8 + T cells is more persistent. (aacrjournals.org)
  • Mice lacking the adenosine A2A receptor are hypoalgesic and a role for the A2A receptor in sensitizing afferent fibres projecting to the spinal cord has been suggested. (surrey.ac.uk)
  • To test this hypothesis adenosine A2A receptor knockout mice and wildtype controls were used in behavioural and autoradiographic experiments. (surrey.ac.uk)
  • Adenosine A2A receptor knockout mice had substantially reduced spinal cord NMDA glutamate binding whereas spinal cord AMPA glutamate receptor binding was increased, spinal cord substance P receptor binding was unaffected. (surrey.ac.uk)
  • Additionally, there was reduced uptake of [14C]-2-deoxyglucose into spinal cord sections from adenosine A2A receptor knockout mice. (surrey.ac.uk)
  • In the formalin test there was a significant reduction in nociceptive behaviour displayed by adenosine A2A receptor knockout mice during both phases of the test. (surrey.ac.uk)
  • The selective adenosine A2A antagonist SCH58261 also antagonized both phases of the formalin test in wildtype mice. (surrey.ac.uk)
  • Spinal cord NMDA glutamate receptor binding was significantly reduced following formalin injection in wildtype mice whereas AMPA glutamate receptor binding and uptake of [14C]-2-deoxyglucose were significantly increased following formalin injection in wildtype mice. (surrey.ac.uk)
  • There were no significant changes in any of the measures examined in spinal cords from adenosine A2A receptor knockout mice. (surrey.ac.uk)
  • Following repeated PGE2 injection and mechanical paw pressure, spinal cord NMDA glutamate receptor binding and uptake of [14C]-2-deoxyglucose into the spinal cord was significantly greater in adenosine A2A receptor knockout mice compared to wildtype mice. (surrey.ac.uk)
  • The reduced response to formalin injection and decrease in NMDA glutamate receptor binding could reflect reduced peripheral sensory input to the spinal cord and be responsible for the hypoalgesia in adenosine A2A receptor knockout mice. (surrey.ac.uk)
  • Using A2A-deficient mice, our results demonstrate that the A2A receptor is required for the proper formation of new lymphatic vessels following LPS and IFA administration. (springer.com)
  • Furthermore, our results also indicate that CD73-derived adenosine has a minor involvement in this process as CD73-deficient mice only display a slight alteration in the recruitment of lymphatic endothelial cell in the LPS-peritonitis model. (springer.com)
  • An adenosine A 2A antagonist, istradefylline, which rescued abnormal excitatory synaptic function in the CS indirect pathway medium spiny neurons (MSNs) of sensitized mice, alleviated both of the QNP-induced abnormal behaviors with only short-term administration. (eneuro.org)
  • Reduced response to the formalin test and lowered spinal NMDA glutamate Receptor binding in Adenosine A2A Receptor knockout mice. (idexlab.com)
  • To test this hypothesis formalin (20 microl, 5%) was injected into the paw and nociceptive responses were measured in wildtype and Adenosine A2A Receptor knockout mice. (idexlab.com)
  • The role of the adenosine A(2A) receptor in the hypnotic effects of ethanol was assessed in mice. (archives-ouvertes.fr)
  • The duration of the loss of righting reflex following acute ethanol administration was shorter for A(2A) receptor-deficient mice (A(2A)R KO) than for wild-type mice (A(2A)R WT), whereas the fall in body temperature was not different between the two phenotypes. (archives-ouvertes.fr)
  • Dipyridamole, an inhibitor of adenosine uptake, increased the sleep time observed following administration of ethanol in CD1 mice and in A(2A)R WT but not in A(2A)R KO mice. (archives-ouvertes.fr)
  • SCH 58261, a selective A(2A) receptor antagonist, unlike DPCPX, a selective A(1) receptor antagonist, shortened the duration of the loss of righting reflex induced by ethanol, thus mimicking the lack of receptor in deficient mice. (archives-ouvertes.fr)
  • Several lines of evidence suggest an involvement of adenosine A2a receptor (A2aAR) mediated adenosinergic neuromodulation in the etiopathogenesis of schizophrenia. (garvan.org.au)
  • We detected one rare naturally occurring receptor variant (Gly-340-Ser) and two silent mutations (405C/T and 1083C/T). To our knowledge the Gly-340-Ser substitution is the first naturally occurring molecular variant of the A2aAR identified. (garvan.org.au)
  • 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 activity of this receptor is mediated by G proteins which activate adenylyl cyclase. (abcam.com)
  • Additionally we are shipping Adenosine A2a Receptor Antibodies (160) and Adenosine A2a Receptor Proteins (7) and many more products for this protein. (antibodies-online.com)
  • The receptors are seven-pass transmembrane proteins that respond to extracellular cues and activate intracellular signal transduction pathways. (sinobiological.com)
  • Recently, evidence has emerged that heptaspanning membrane or G protein-coupled receptors may be linked to intracellular proteins identified as regulators of receptor anchoring and signaling. (cardiff.ac.uk)
  • Cells + Anti-Human Adenosine A 2A Receptor (extracellular)-FITC Antibody (#AAR-007-F), (2.5 µg). (alomone.com)
  • Of the four known adenosine receptors (A 1 , A 2A , A 2B , and A 3 ), A 1 receptor (A 1 R) and A 2A receptor (A 2A R) are primarily responsible for the central effects of adenosine ( Dunwiddie and Masino, 2001 ). (jneurosci.org)
  • In this study, we aim to determine the functional effects of two frequent genetic polymorphisms in the adenosine receptor and AMPdeaminase (involved in the formation of adenosine) on the vascular effects of adenosine. (bioportfolio.com)
  • Report effects of adenosine and a selective A2A adenosine receptor agonist on hemodynamic and thallium-201 and technetium-99m-sestaMIBI biodistribution and kinetics. (cusabio.com)
  • Structure-based discovery of A2A adenosine receptor ligands. (nih.gov)
  • A number of selective A2A ligands have been developed, with several possible therapeutic applications. (wikipedia.org)
  • It was clear that ligands of adenosine receptors and inhibitors for phosphodiesterase were targets for drug development. (wikipedia.org)
  • These labeled ligands may facilitate the positron emission tomographic (PET) investigation of adenosine A 2a receptors. (springer.com)
  • Adenosine receptors are emerging as relevant drug targets for a variety of disorders including Parkinson's disease, and there is interest in discovering new ligands that bind to them. (fieldofscience.com)
  • In the present report, a team of researchers from NIH and UCSF led by Brian Shoichet, John Irwin and Kenneth Jacobson use virtual screening to discover new ligands for the A2A. (fieldofscience.com)
  • While the compounds formed the same kinds of interactions as some other A2A ligands, they were also relatively diverse in structure. (fieldofscience.com)
  • Accordingly, our approach allowed immediate 'real-time' readout of the ligand-receptor interaction, thus allowing kinetic binding experiments, a feature impossible to achieve using conventional radioisotope-labelled ligands. (bio-protocol.org)
  • Understanding how ligands bind to G-protein-coupled receptors and how binding changes receptor structure to affect signaling is critical for developing a complete picture of the signal transduction process. (jpt.com)
  • Effects of CGS 21680, a selective adenosine A2A receptor agonist, on allergic airways inflammation in the rat. (semanticscholar.org)
  • In addition, A2A receptor can suppress immune cells, thereby protecting tissue from inflammation. (wikipedia.org)
  • Adenosine levels are elevated during conditions of hypoxia ( 6 ), muscle exercise ( 7 ), inflammation, or adenosine deaminase (ADA) 3 deficiency. (jimmunol.org)
  • Extracellular adenosine has an important role in regulating the severity of inflammation during an immune response. (jimmunol.org)
  • During inflammation, increases in extracellular adenosine levels effectively turn off the local inflammatory response to protect against excessive cellular damage to the surrounding tissue ( 2 ). (jimmunol.org)
  • 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)
  • Altogether our data indicate that adenosine is one of the soluble mediators released by macrophages that mediate engulfment-dependent apoptotic cell suppression of inflammation. (pubmedcentralcanada.ca)
  • PTX alone, or in combination with ZM-241385 (an adenosine receptor A2A antagonist) or CGS-21680 (an A2A agonist), was pre-administered to rats 1 h prior to IAC, and the severity of lung injury and inflammation were examined. (pubmedcentralcanada.ca)
  • The study indicates PTX plays a protective role in IAC-induced ALI in rats by inhibiting pulmonary inflammation through A2A signaling pathways. (pubmedcentralcanada.ca)
  • The release of adenosine at sites of inflammation represents an endogenous mechanism for limiting excessive inflammation and tissue damage. (gla.ac.uk)
  • The goal of this study is to determine the role of adenosine signaling in retinal inflammation and its potential modulation by CBD. (arvojournals.org)
  • We have investigated the effect of 2(4-((2-carboxymethyl)phenyl)ethylamino)-5'-N-ethylcarboxamidoadenosine (CGS 21680), a potent and selective agonist at adenosine A2A receptors, on pulmonary inflammation induced by allergen challenge in the ovalbumin-sensitised, Brown Norway rat. (semanticscholar.org)
  • Adenosine and inflammation: what's new on the horizon? (semanticscholar.org)
  • Adenosine A2A receptors have been shown to exert anti-inflammatory effects in animal models of inflammation, however their effect on neutrophils is unknown. (virginia.edu)
  • Altogether, our data indicate that adenosine is one of the soluble mediators released by macrophages that mediate engulfment-dependent apoptotic cell suppression of inflammation, and TG2 is anti-inflammatory by both promoting active TGF-β formation and regulating integrin signaling. (unideb.hu)
  • 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)
  • 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)
  • As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. (wikipedia.org)
  • This effect has been linked to caffeine's interaction with the A 2A adenosine receptor, which controls locomotor behavior in basal ganglia, together with dopamine D 2 and metabotropic glutamate receptors (mGluRs) ( 11 , 12 ). (sciencemag.org)
  • In this study, we showed that repeated injection of dopamine D 2 receptor agonist, quinpirole (QNP) elicited two distinct OCD-related behaviors: cognitive inflexibility (SSRI-responsive) and repetitive behavior (SSRI-resistant). (eneuro.org)
  • In this localization A2ARs establish reciprocal antagonistic interactions with dopamine D2 receptors (D2Rs). (ub.edu)
  • From the discovery of adenosine A2A receptor-dopamine D2 receptor heteromers and the antagonistic interaction between these receptors, the basis of a new therapeutic approach towards the treatment of PD emerged. (nwu.ac.za)
  • The adenosine A 2A receptors (A 2A Rs) are highly enriched in the striatopallidal neurons where they integrate dopamine and glutamate signals to modulate several cognitive behaviors, but their contribution to cognitive flexibility control is unclear. (abo.fi)
  • The protein uses adenosine as the preferred endogenous agonist and is involved in increasing intracellular cAMP levels. (proteopedia.org)
  • Adenosine is an endogenous purine nucleoside that modulates a wide range of physiological functions ( 1 ). (jimmunol.org)
  • This provides a switch mechanism by which low and high concentrations of adenosine inhibit and stimulate, respectively, glutamate release. (jneurosci.org)
  • We also labelled NMDA glutamate and NK1 Receptor s in spinal cord sections as an indirect measure of nociceptive transmission from peripheral sites to the spinal cord. (idexlab.com)
  • These results suggest that the activated A 2A AR in the retinal microglial cells plays a major anti-inflammatory role in the retina and that CBD's anti-inflammatory effects are linked to the inhibition of adenosine uptake. (arvojournals.org)
  • Occupancy of A2A receptors with drugs such as ATL313 may exert their anti-inflammatory effects on neutrophils through inhibition of LFA-1-mediated adhesion and migration. (virginia.edu)
  • And related, are the anti-inflammatory effects seen in vivo A1 and/or A2A mediated? (painresearchforum.org)
  • 2] Interestingly, evidence is growing for a certain role of adenosine receptors in the field of oncology . (axonmedchem.com)
  • Belongs to the G-protein coupled receptor 1 family. (abcam.com)
  • Hydrophobicity analysis of the deduced protein sequence reveals seven hydrophobic regions, characteristic of a member of the G-protein-coupled receptor superfamily. (nih.gov)
  • For details see G protein-coupled receptor . (proteopedia.org)
  • A G-protein coupled receptor. (mybiosource.com)
  • The blockade of A2A receptors has potentially shown to be protective in several tumor models, through pharmacological inhibition or genetic deletion. (wikipedia.org)
  • High concentrations of adenosine in tumor microenvironments inhibit antitumor cytotoxic lymphocyte responses. (aacrjournals.org)
  • The results indicate that tumor-associated myeloid cells, including macrophages, DCs, and MDSCs all express immunosuppressive A 2A Rs that are potential targets of adenosine receptor blockers to enhance immune killing of tumors. (aacrjournals.org)
  • PTX has hemorheologic effects and vasodilating properties for peripheral blood vessels, displays anti-inflammatory activities by inhibiting the production of tumor necrosis factor (TNF)-α, and improves the recovery of adenosine triphosphate (ATP) [ 5 , 6 ]. (pubmedcentralcanada.ca)
  • Our group recently identified a role for the CD73-adenosine pathway in tumor angiogenesis. (springer.com)
  • As angiogenesis and lymphangiogenesis are similar processes, often occurring in parallel, we suspect that the CD73-adenosine pathway could have a role in the regulation of lymphangiogenesis during inflammatory reactions and in the tumor microenvironment. (springer.com)
  • In the B16 melanoma model, host-A2A deficiency impaired tumor-associated lymphangiogenesis which resulted in a reduced number of tumor cells disseminating to the tumor-draining lymph node. (springer.com)
  • Collectively, our results demonstrate that the A2A receptor promotes inflammatory and tumor-associated lymphangiogenesis. (springer.com)
  • Adenosine uptake and tumor necrosis factor (TNF)-α release in cells or in retinas were determined. (arvojournals.org)
  • Although adenosine is typically produced inside a cell, extracellular levels of adenosine rise as a consequence of the catabolism of ATP that is released from stressed or damaged cells ( 3 , 4 ). (jimmunol.org)
  • Conditions of inflammatory tissue distress are associated with high extracellular levels of adenosine, due to increased adenosine triphosphate (ATP) degradation upon cellular stress or the release of extracellular ATP upon cell death, which can be degraded to adenosine by membrane-bound ecto-enzymes like CD39 and CD73. (biomedcentral.com)
  • Conditions of tissue injury are associated with high extracellular levels of adenosine. (biomedcentral.com)
  • Enhanced extracellular concentrations of adenosine can be considered as a general damage signal [ 2 ], contributing to a 'damage-associated molecular pattern (DAMP)' [ 3 ]. (biomedcentral.com)
  • 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)
  • The functional role of heteromers of G-protein-coupled receptors is a matter of debate. (jneurosci.org)
  • For example, preincubation of macrophages with apoptotic cells strongly suppresses the inflammatory response induced via Toll-like receptor 4 by lipopolysaccharide, a component of the cell wall of Gram-negative bacteria ( 4 - 6 ). (pubmedcentralcanada.ca)
  • Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes. (semanticscholar.org)
  • This extracellular ATP is converted to ADP and AMP by CD39 and then to adenosine by CD73 ( 5 ). (jimmunol.org)
  • CD73, which converts AMP to adenosine, is highly expressed by some tumors including ER − breast tumors, endothelial cells, regulatory T cells, and most B cells ( 4, 5 ). (aacrjournals.org)
  • Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. (semanticscholar.org)
  • The source of adenosine can either be intracellular adenosine triphosphate (ATP) degradation upon cellular stress, particularly under high energy demand, and subsequent transportation to the extracellular space via specialised nucleoside transporters or the appearance of large amounts of extracellular ATP due to tissue damage and cell death, which can be degraded to adenosine by membrane-bound ecto-enzymes like CD39 and CD73 [ 1 ]. (biomedcentral.com)
  • This work represents the first cloning of an A2a receptor in a rodent species, offers a complete pharmacological characterization of the receptor and provides an anatomical comparison between binding profile and gene expression of the receptor. (nih.gov)
  • In 100 healthy young volunteers, we will determine the genotype of the adenosine A2A receptor gene. (bioportfolio.com)
  • p1 mRNA levels were highest in 12 and 21-month-old animals in both ventricles (LV: p2A gene expression was lower in the aged LV (p1 receptor mRNA may partially explain the stronger antiadrenergic effects of Ado in the senescent heart. (elsevier.com)
  • Since ageing involves a complex change in these effects, we evaluated A1 and A2A gene expression in left (LV) and right ventricle (RV) from 2-, 5-, 12-, and 21-month-old Sprague-Dawley rats. (elsevier.com)
  • All Adenosine Receptor A2a reagents are produced in house and quality controlled, including 27 Adenosine Receptor A2a Gene, 2 Adenosine Receptor A2a qPCR. (sinobiological.com)
  • The study goals were to evaluate the potency and selectivity of these new compounds on recombinant canine Ado receptors and to evaluate their hemodynamic properties in dogs to assess their usefulness as vasodilators for myocardial perfusion imaging. (ahajournals.org)
  • The authors use the ZINC library of drug like molecules to dock about a million and a half compounds into the binding pocket of the A2A crystal structure. (fieldofscience.com)
  • A radioligand binding protocol described in literature was employed to investigate the binding of the compounds to the adenosine A2A and A1 receptors. (nwu.ac.za)
  • A very significant density of adenosine A2A receptors (A2ARs) is present in the striatum, where they are preferentially localized postsynaptically in striatopallidal medium spiny neurons (MSNs). (ub.edu)
  • 11C-preladenant was developed as a novel PET ligand for the adenosine A2A receptors (A2ARs). (vumc.nl)
  • The purine nucleoside adenosine is released by various cells, including fibroblasts, epithelial cells, endothelial cells, platelets, and muscle cells ( 1 , 2 , 3 , 4 ) or is derived from the extracellular metabolism of released purine nucleotides ( 5 ). (jimmunol.org)
  • The purine nucleoside adenosine is a modulatory messenger that is implicated in many physiological and pathological functions of both the immune system and the central nervous system (CNS). (biomedcentral.com)
  • It is well established that some areas of solid tumors often have transient or chronic hypoxia ( 19 , 20 ), which is conducive to extracellular adenosine accumulation ( 21 ). (pnas.org)
  • Extracellular adenosine gathers in response to cellular stress and breakdown through interactions with hypoxia induced HIF-1α. (wikipedia.org)
  • Interplay of hypoxia and A2B adenosine receptors in tissue protection. (semanticscholar.org)
  • A2B adenosine receptor dampens hypoxia-induced vascular leak. (semanticscholar.org)
  • Adenosine, released during cellular stress, damage and hypoxia, is a major regulator of angiogenesis. (cf.ac.uk)
  • Each of these four receptors plays an essential role in responding to adenosine in the central nervous system ( 3 , 4 ), regulating pain ( 5 ), cerebral blood flow ( 6 ), basal ganglia functions ( 7 ), respiration ( 8 ), and sleep ( 9 ). (sciencemag.org)
  • This may reflect loss of inhibitory adenosine A2A receptors located on inflammatory cells. (surrey.ac.uk)
  • In the present study, we demonstrate that heteromerization of adenosine A 1 receptors (A 1 Rs) and A 2A receptors (A 2A Rs) allows adenosine to exert a fine-tuning modulation of glutamatergic neurotransmission. (jneurosci.org)
  • The implications of these findings are that, potentially, modulation of this receptor can be beneficial for future treatment of MS," she added. (scitechdaily.com)
  • Adenosine A2A receptor locations in the body could help us to understand the possible therapeutic applications in the future. (wikipedia.org)
  • Methods and Results - In assays of recombinant canine Ado receptors, ATL-193 and ATL-146e were highly selective for the A 2A over the A 1 and A 3 receptors and were more potent than MRE-0470 and CGS-21680. (ahajournals.org)
  • 50 times more potent than CGS-21680 at human A 2A receptors and have half-lives of several minutes in human blood. (ahajournals.org)
  • Comparison of the adenosine A2A affinity of the most potent derivative (1h, Ki = 28.7 μM) from this study with that of the previously synthesised dihydropyridine derivatives (Van Rhee et al. (nwu.ac.za)
  • 1996, most potent compound had a Ki = 2.74 mM) reveals that an approximate 100-fold increase in binding affinity for A2A receptors occurred. (nwu.ac.za)
  • The same trend was observed for adenosine A1 affinity, where the most potent compound (1b) of this study exhibited a Ki-value of 7.39 μM compared to 2.75 mM determined for the most potent dihydropyridine derivatives (Van Rhee et al. (nwu.ac.za)
  • A1 and A2A receptors are believed to regulate myocardial oxygen demand and to increase coronary circulation by vasodilation. (wikipedia.org)
  • CVTX ) and Astellas Pharma US, Inc. today announced that the U.S. Food and Drug Administration (FDA) has approved Lexiscan(TM) (regadenoson) injection, an A2A adenosine receptor agonist, for use as a pharmacologic stress agent in radionuclide myocardial perfusion imaging (MPI) -- a test that detects and characterizes coronary artery disease -- in patients unable to undergo adequate exercise stress. (bio-medicine.org)
  • Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. (ahajournals.org)
  • Regadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans. (biomedsearch.com)
  • BACKGROUND: Regadenoson is a selective A2A adenosine receptor agonist and vasodilator used to increase the heterogeneity of distribution of coronary blood flow during myocardial perfusion imaging. (biomedsearch.com)
  • More specifically, A1 and A2A receptors play a role in regulating myocardial oxygen consumption and coronary blood flow . (axonmedchem.com)
  • Adenosine is a neuromodulator with complex effects on nociceptive pathways. (surrey.ac.uk)
  • These results support a key role for adenosine A2A receptors in peripheral nociceptive pathways. (surrey.ac.uk)
  • A full-length complementary DNA (cDNA) clone encoding the guinea pig brain A2 adenosine receptor has been isolated by polymerase chain reaction (PCR) and low-stringency-hybridization screening of a guinea pig brain cDNA library. (nih.gov)
  • This cDNA contains a long open reading frame encoding a 409-amino acid-residue protein which is highly homologous to the A2 adenosine receptors previously cloned from other species. (nih.gov)
  • In the subsequent receptor traffic from the cell surface, the role of actin organization was shown to be crucial in transiently transfected HEK-293 cells, as actin depolymerization by cytochalasin D prevented its agonist-induced internalization. (cardiff.ac.uk)
  • Part of its action in reducing incidence or delaying Alzheimer's and Parkinson's diseases symptoms in human is credited to the adenosine receptors properties. (springer.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)
  • 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)
  • Four disulfide bridges in the extracellular domain, combined with a subtle repacking of the transmembrane helices relative to the adrenergic and rhodopsin receptor structures, define a pocket distinct from that of other structurally determined GPCRs. (sciencemag.org)
  • Our results also suggest that ZM241385 follows a multistep dissociation pathway, consecutively interacting with distinct receptor regions, a mechanism that may also be common to many other GPCRs. (aspetjournals.org)
  • The large-scale production of G-protein coupled receptors (GPCRs) for functional and structural studies remains a challenge. (biomedcentral.com)
  • G-protein-coupled receptors (GPCRs) form a large superfamily of cell-surface receptors that mediate cellular responses to a wide range of biologically active molecules including hormones, neurotransmitters and drugs. (biomedcentral.com)
  • 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)
  • Adenosine and NECA stimulated a twofold increase in chromogranin A secretion in BON-1 cells. (cf.ac.uk)
  • The presence of heterodimeric complexes has progressed in suggesting new ways to regulate neuronal activity by targeting the A2A receptor. (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 adenosine A 2A receptor (A 2A R) modulates normal vascularization and pathologic angiogenesis in many tissues and may contribute to the pathogenesis of retinopathy of prematurity (ROP) characterized by abnormal retinal vascularization in surviving premature infants. (arvojournals.org)