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 ubiquitously-expressed cysteine protease that plays an enzymatic role in POST-TRANSLATIONAL PROTEIN PROCESSING of proteins within SECRETORY GRANULES.
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.
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
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.
The holly plant family of the order Celastrales, subclass Rosidae, class Magnoliopsida.
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.
Molecular cloning and characterization of an adenosine receptor: The A3 adenosine receptor. Proceedings of the National Academy ... Civelli's research in this period did not focus solely on dopamine receptors; he also discovered the adenosine A3 receptor. By ... ". "Molecular cloning and characterization of an adenosine receptor: the A3 adenosine receptor". "Chinese herbal compound ...
Björklund O, Shang M, Tonazzini I, Daré E, Fredholm BB (2008). "Adenosine A1 and A3 receptors protect astrocytes from hypoxic ... Once localized, the enzyme alternates between two conformations, E1 and E2, to transport ions across the membrane. The E1 ... It is a member of the P-type ATPases, also known as E1-E2 ATPases due to its two states. The gastric hydrogen potassium ATPase ... Like all P-type ATPases, a phosphate group is transferred from adenosine triphosphate (ATP) to the H+/K+ ATPase during the ...
... is a drug which acts as a selective antagonist for the adenosine A3 receptor (ki value at human A3 receptor is 0.44 nM ... The affinity towards adenosine A3 subtype was measured against the radioligand PSB-11. Ozola V, Thorand M, Diekmann M, Qurishi ... Müller CE (2003). "Medicinal chemistry of adenosine A3 receptor ligands". Current Topics in Medicinal Chemistry. 3 (4): 445-62 ... structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors ...
... is known to act as an antagonist of the adenosine A3 receptor. Reversine is a potent inhibitor of the mitotic kinase ...
On the other hand, nanomolar concentrations of adenosine activate A1 and A3 receptors, resulting in neutrophilic chemotaxis ... Formation of foam cells is inhibited by adenosine A2A receptors. Abnormal levels of ATP and adenosine are present in the ... Extracellular adenosine contributes to the regulation of GFR. Renal interstitial adenosine is mainly derived from ... In the airways of patients with asthma, the expression of adenosine receptors is upregulated. Adenosine receptors affect ...
Yamano K, Mori K, Nakano R, Kusunoki M, Inoue M, Satoh M (2007). "Identification of the functional expression of adenosine A3 ...
Mutations to the a3 isoform result in the human disease infantile malignant osteopetrosis, and mutations to the a4 isoform ... adenosine triphosphatase in a Japanese patient with infantile malignant osteopetrosis". Bone. 30 (2): 436-9. doi:10.1016/S8756- ... dRTA caused by mutations in the a4 subunit gene in some cases can be associated with deafness due to a failure to normally ... Inheritance of this type of RTA results from either mutations to V-ATPase subunit isoform B1 or isoform a4 or mutations of band ...
... adenosine may inhibit the function of these immune cells. In addition, the tumor cells may also express adenosine A1 and A3 ... Subsequently, cAMP signaling is triggered in T cell that express the adenosine A2A receptor. Adenosine receptor are also ... Free adenosine generated by NT5E inhibits cellular immune responses and thereby promotes immune escape of tumor cells. Due to ... Also described was adenosine generated by NT5E, which limits the inflammatory immune response by negative feedback in ...
... is a drug which acts as a potent and selective antagonist for the adenosine A3 receptor, with sub-nanomolar affinity ( ... A3 Ki=0.2nM) and high selectivity over the other three adenosine receptor subtypes. Simple xanthine derivatives such as ... a new potent and selective adenosine A3 receptor antagonist". European Journal of Pharmacology. 444 (3): 133-41. doi:10.1016/ ... low affinity for the A3 subtype and must be extended by expanding the ring system and adding an aromatic group to give high A3 ...
... adenosine receptor binding affinity (21 μM for A1, 32 μM for A2A, 4.5 μM for A2B, and >100 for μM for A3) is ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Progress in ... Müller, Christa E.; Jacobson, Kenneth A. (2011), Fredholm, Bertil B. (ed.), "Xanthines as Adenosine Receptor Antagonists", ... Studies indicate that, similar to caffeine, simultaneous antagonism of adenosine receptors is responsible for paraxanthine's ...
The E1-E2 notation highlights the selectivity of the enzyme. In E1, the pump has high affinity for the exported substrate and ... doi:10.1016/0968-0004(87)90071-5. SKOU JC (February 1957). "The influence of some cations on an adenosine triphosphatase from ... These are termed E1~P, E2P, E2-P*, and E1/E2. ATP hydrolysis occurs in the cytoplasmic headpiece at the interface between ... denoted by E1 and E2. The E1-E2 notation stems from the initial studies on this family of enzymes made on the Na+/K+-ATPase, ...
IPR008102 Adenosine receptor InterPro: IPR001634 A1 (ADORA1, AA1R) A2a (ADORA2A, AA2A) A2b (ADORA2B, AA2B) A3 (ADORA3, AA3R) ... Prostaglandin E1 receptor (PTGER1, PE21) Prostaglandin E2 receptor (PTGER2, PE22) Prostaglandin E3 receptor (PTGER3, PE23) ...
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Prog Clin Biol ... or rather its adenosine-antagonist behavior). Mandal, Ananya. "Caffeine Pharmacology". Website Medical News. Archived from the ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
... or adenosine A3. The exact effects of methoctramine still remain unknown. However, the few experiments conducted have led to ...
The following G protein-coupled receptors couple to Gi/o subunits: Acetylcholine M2 & M4 receptors Adenosine A1 & A3 receptors ...
5-TRIAZINE DERIVATIVES AS LIGANDS FOR HUMAN ADENOSINE-A3 RECEPTORS", published 2003-12-11 (Reagent number two: norephedrine, ... It is also employed the synthesis of an experimental adenosine receptor ligand.: Cyanuric chloride can also be used as an ...
... adenosine a2b MeSH D12.776.543.750.810.700.300 - receptor, adenosine a3 MeSH D12.776.543.750.810.720 - receptors, purinergic p2 ... adenosine a2b MeSH D12.776.543.750.100.700.700.300 - receptor, adenosine a3 MeSH D12.776.543.750.100.700.720 - receptors, ... adenosine a2b MeSH D12.776.543.750.720.700.700.300 - receptor, adenosine a3 MeSH D12.776.543.750.720.700.720 - receptors, ... adenosine a1 MeSH D12.776.543.750.100.700.700.200 - receptors, adenosine a2 MeSH D12.776.543.750.100.700.700.200.100 - receptor ...
"Novel mutations in the a3 subunit of vacuolar H+-adenosine triphosphatase in a Japanese patient with infantile malignant ... As mutacións na isoforma a3 orixinan a enfermidade humana infantil osteopetrose maligna, e as mutacións na isoforma a4 dan ... e vinte e catro mutacións na a4 que orixinan a acidose tubular renal distal.[42][45] Os estudos de PCR e transcrición inversa ... dos pacientes con osteopetrose maligna infantl recesiva teñen mutacións no xene da subunidade a isoforma a3 da ATPase V.[35][38 ...
Adenosine monophosphate (AMP) Adenosine triphosphate (ATP) Adenylate cyclase Adiponectin Adonitol Adrenaline, epinephrine ... C19H42BrN Chelerythrine Chromomycin A3 Chaparonin Chitin α-Chloralose Chlorophyll Cholecystokinin (CCK) Cholesterol Choline ... Abamectine Abietic acid Acetic acid Acetylcholine Actin Actinomycin D Adenine Adenosmeme Adenosine diphosphate (ADP) ... Cortisol Creatine Creatine kinase Crystallin Cyclic adenosine monophosphate (cAMP) α-Cyclodextrin Cyclodextrin ...
... e1 Terminology Relating to Fabrics and Fabric Test Methods D4851 - 07(2019)e1 Test Methods for Coated and Laminated Fabrics for ... 15 Test Method for Adenosine Triphosphate (ATP) Content of Microorganisms in Water D4014 - 03(2018) Specification for Plain and ... e1 Practice for Labeling Art Materials for Chronic Health Hazards D4239 - 18e1 Test Method for Sulfur in the Analysis Sample of ... e1 Test Method for Performing the Sieve Analysis of Coal and Designating Coal Size D4751 - 20b Test Methods for Determining ...
... paper, a paper size defined by ISO 216 A3 regulatory sequence, a sequence for the insulin gene Adenosine A3 receptor, a ... a band known as A3 in the U.S. to avoid confusion with the country group Alabama A-3, a Yamaha musical instrument product A3 ... a British Isles plants community Gibberellin A3, a plant hormone HLA-A3, a Human MHC Serotype HLA-A Subfamily A3, a rhodopsin- ... a 1980 racing car A3, a climbing Grade A-3 lifeboat, a 1947 lifeboat for carrying by the SB-29 Superfortress Abrial A-3 Oricou ...
Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ... All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... When adenosine enters the circulation, it is broken down by adenosine deaminase, which is present in red blood cells and the ... Adenosine is believed to be an anti-inflammatory agent at the A2A receptor. Topical treatment of adenosine to foot wounds in ...
As a result of the formation of this new iron-cyanide complex, the electrons that would situate themselves on the heme a3 group ... Cyanide prevents the cell from producing adenosine triphosphate (ATP) by binding to one of the proteins involved in the ... The cyanide component of Zyklon B can bind at one of these iron groups, heme a3, forming a more stabilized compound through ...
2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system.". J. Comp ... 2001). "Adenosine A2B receptors behave as an alternative anchoring protein for cell surface adenosine deaminase in lymphocytes ... Strohmeier GR, Reppert SM, Lencer WI, Madara JL (1995). "The A2b adenosine receptor mediates cAMP responses to adenosine ... cooperative interaction between A2B and A3 adenosine receptors.". Circ. Res. 92 (5): 485-92. PMID 12600879. doi:10.1161/01.RES. ...
... is an antagonist of all four adenosine receptor subtypes (A1, A2A, A2B, and A3), although with varying potencies. The ... When caffeine is consumed, it antagonizes adenosine receptors; in other words, caffeine prevents adenosine from activating the ... and 80 μM at A3. Antagonism of adenosine receptors by caffeine also stimulates the medullary vagal, vasomotor, and respiratory ... an agent that reduces the effects of adenosine). The caffeine molecule is structurally similar to adenosine, and is capable of ...
There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a different gene. The ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... "Entrez Gene: ADORA2A adenosine A2A receptor". Jacobson KA, Gao ZG (2006). "Adenosine receptors as therapeutic targets". Nature ... Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in ...
... and adenosine monophosphate (AMP) and signal transduction in the form of cyclic adenosine monophosphate (cAMP). A2B and A3 ... Caffeine acts as an antagonist of adenosine A1 and A2A receptors. Adenosine is a normal neuromodulator that activates adenosine ... There are four well-known adenosine receptors found in the body, A1, A2A, A2B, and A3. The endogenous agonist for these ... Adenosine acts on A1 receptors to decrease opening of N-type Ca2+ channels in some hippocampal neurons, and therefore decrease ...
January 2002). "7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor ... The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Entrez Gene: ADORA2A adenosine A2A receptor". Ohta A, Sitkovsky M (2001). "Role of G-protein-coupled adenosine receptors in ...
2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system". J. Comp ... The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human ... 2001). "Adenosine A2B receptors behave as an alternative anchoring protein for cell surface adenosine deaminase in lymphocytes ... Strohmeier GR, Reppert SM, Lencer WI, Madara JL (1995). "The A2b adenosine receptor mediates cAMP responses to adenosine ...
Wang Y, Macke JP, Abella BS, Andreasson K, Worley P, Gilbert DJ, Copeland NG, Jenkins NA, Nathans J (Jun 1996). "A large family of putative transmembrane receptors homologous to the product of the Drosophila tissue polarity gene frizzled". J Biol Chem. 271 (8): 4468-76. doi:10.1074/jbc.271.8.4468. PMID 8626800 ...
G-protein coupled receptor 120 is a protein that in humans is encoded by the GPR120 gene.[5][6] GPR120 is a member of the rhodopsin family of G protein-coupled receptors (GPRs).[5][6] GPR120 has also been shown to mediate the anti-inflammatory and insulin-sensitizing effects of omega 3 fatty acids.[7] Lack of GPR120 is responsible for reduced fat metabolism, thereby leading to obesity.[8] Additionally, GPR120 has been implicated to be involved in the ability to taste fats.[9] It is expressed in taste bud cells (specifically cell type II, which contain other G-protein coupled taste receptors), and its absence leads to reduced preference to two types of fatty acid (linoleic acid and oleic acid), as well as decreased neuronal response to oral fatty acids.[10] ...
Thalidomide has been shown to bind to cereblon, inhibiting the activity of the E3 ubiquitin ligase, resulting in accumulation ... In vitro, apremilast reduces PDE4 activity leading to an increase in cyclic-adenosine monophosphate (cAMP) concentrations in ... It acts as a component of the E3 ubiquitin ligase, regulating various developmental processes, including embryogenesis, ...
Hillier LD, Lennon G, Becker M, Bonaldo MF, Chiapelli B, Chissoe S, Dietrich N, DuBuque T, Favello A, Gish W, Hawkins M, Hultman M, Kucaba T, Lacy M, Le M, Le N, Mardis E, Moore B, Morris M, Parsons J, Prange C, Rifkin L, Rohlfing T, Schellenberg K, Bento Soares M, Tan F, Thierry-Meg J, Trevaskis E, Underwood K, Wohldman P, Waterston R, Wilson R, Marra M (September 1996). "Generation and analysis of 280,000 human expressed sequence tags". Genome Research. 6 (9): 807-28. doi:10.1101/gr.6.9.807. PMID 8889549 ...
It aminoacylates at the 2'-OH of a terminal adenosine nucleotide on tRNA, and it is usually monomeric or dimeric (one or two ... It aminoacylates at the 3'-OH of a terminal adenosine on tRNA, and is usually dimeric or tetrameric (two or four subunits, ... The amino acids are attached to the hydroxyl (-OH) group of the adenosine via the carboxyl (-COOH) group. ...
"for their elucidation of the enzymatic mechanism underlying the synthesis of adenosine triphosphate (ATP)"[96] ...
... leukotriene A4 LTA4, which is then either rapidly converted to leukotriene B4 (LTB4) by Leukotriene-A4 hydrolase (LTA4H) or to ... An Adenosine triphosphate (ATP) binding site; ATP is crucial for ALOX5's metabolic activity ... Leukotriene-A4 hydrolase, to form the dihydroxyl product, Leukotriene B4 (LTB4, i.e. 5S,12R-dihydroxy-5S,6Z,8E,10E,12R,14Z- ... In another pathway, ALOX5 may act in series with a second lipoxygenase enzyme, ALOX15, to metabolize AA to lipoxin A4 (LxA4) ...
141 (16): e1-23. doi:10.1161/CIR.0000000000000748. PMID 32148086.. *^ Oishi, ML; Xing, S (February 2013). "Atrial fibrillation ... Other medications that rarely increase the risk of developing atrial fibrillation include adenosine, aminophylline, ... 119 (5): 448.e1-19. doi:10.1016/j.amjmed.2005.10.057. PMID 16651058.. ...
Gajewski E, Steckler D, Goldberg R (1986). "Thermodynamics of the hydrolysis of adenosine 5'-triphosphate to adenosine 5'- ... Receptorji P1 imajo podtipe A1, A2a, A2b in A3 (A je ostalo od stare nomenklature, kot adenozinski receptor) in vsi so ... 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) ...
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: ...
... and low production of adenosine triphosphate (ATP), can cause myocardial depression, reducing cardiac contractility and causing ... 29 (1): 185.e1-7. doi:10.1016/j.jcrc.2013.09.031. PMID 24262273.. ...
Kotani M, Tanaka I, Ogawa Y, Usui T, Mori K, Ichikawa A, Narumiya S, Yoshimi T, Nakao K (November 1995). "Molecular cloning and expression of multiple isoforms of human prostaglandin E receptor EP3 subtype generated by alternative messenger RNA splicing: multiple second messenger systems and tissue-specific distributions". Molecular Pharmacology. 48 (5): 869-79. PMID 7476918 ...
18 E3,18 55.78 cM. Start. 82,392,496 bp[2]. End. 82,406,777 bp[2]. ...
The TAS2R38 protein also confers sensitivity to the bitter compound 6-n-propylthiouracil (PROP). Because perception of PROP bitterness has been associated with supertasting, and because TAS2R38 genotypes associate with PROP-tasting phenotypes, it has been proposed that TAS2R38 genotypes may have a role in supertasting capabilities. It appears that while TAS2R38 genotypes determine a threshold of PROP tasting abilities, the genotypes cannot account for the differences in tasting amongst each threshold group. For example, some PAV/PAV homozygotes perceive PROP to be more bitter than others, and TAS2R38 genotype cannot account for these differences. Furthermore, some heterozygotes may become PROP supertasters (despite a lack of two PAV alleles), indicating overlap between PROP bitterness levels and varying TAS2R38 genotypes. These results illustrate that a mechanism beyond TAS2R38 genotype contributes to supertasting capabilities.[13] Because fungiform papillae (FP) number varies with PROP ...
CySLTR2 mRNA is co-expressed along with CysLRR1 in human blood eosinophils and platelets, and tissue mast cells, macrophages, airway epithelial cells, and vascular endothelial cells. It is also expressed without CysLTR1 throughout the heart, including Purkinje cells, adrenal gland, and brain as well as some vascular endothelial, airway epithelial, and smooth muscle cells.[10][11][12][13] CysLTR2, similar to CysLTR1, is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq alpha subunit and/or Ga subunit of its coupled G protein, depending or the cell type. Acting through these G proteins and their subunits, ligand-bound CysLTR1 activates a series of pathways that lead to cell function (see Gq alpha subunit#function and Ga subunit#function for details); the order of potency of the cysLTs in stimulating CysLTR2 is LTD4=LTC4,LTE4 with LTE4 probably lacking sufficient potency to have much activity that operates through CysLTR1 in vivo. By comparison, the ...
"For their elucidation of the enzymatic mechanism underlying the synthesis of adenosine triphosphate (ATP)"[156] ... Trillat JJ (1926). "Rayons X et Composeés organiques à longe chaine. Recherches spectrographiques sue leurs structures et leurs ...
N-terminal ATPase domain - binds ATP (Adenosine triphosphate) and hydrolyzes it to ADP (Adenosine diphosphate). The NBD ... Interaction with CHIP (Carboxyl-terminus of Hsp70 Interacting Protein)-an E3 ubiquitin ligase-allows Hsp70 to pass proteins to ...
Text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization ...
Much ado about adenosine: adenosine synthesis and function in regulatory T cell biology. „J Immunol". 185 (4), s. 1993-1998, ... J Allergy Clin Immunol". 121 (6), s. 1460-1466, 1466.e1-7, czerwiec 2008. DOI: 10.1016/j.jaci.2008.03.025. PMID: 18455222. ... adenosine monophosphate to adenosine. „J Immunol". 177 (10), s. 6780-6786, listopad 2006. PMID: 17082591. ... J Allergy Clin Immunol". 121 (6), s. 1467-1472, 1472.e1, czerwiec 2008. DOI: 10.1016/j.jaci.2008.03.013. PMID: 18423565. ...
P-ATPases may be composed of one or two polypeptides, and can usually take two main conformations, E1 and E2. Na+/K+ ... Kielley, WW (1961). "Myosin adenosine triphosphatase". In Boyer, P. D.; Lardy, H.; Myrbäck, K. The Enzymes. 5 (2nd ed.). New ... P-ATPases (sometime known as E1-E2 ATPases) are found in bacteria and also in eukaryotic plasma membranes and organelles. Its ... Martin SS, Senior AE (November 1980). "Membrane adenosine triphosphatase activities in rat pancreas". Biochimica et Biophysica ...
Adams MD, Soares MB, Kerlavage AR, et al. (1993). "Rapid cDNA sequencing (expressed sequence tags) from a directionally cloned human infant brain cDNA library". Nat. Genet. 4 (4): 373-80. doi:10.1038/ng0893-373. PMID 8401585 ...
ADP受體/P2Y12(英語:P2Y12)抑制劑(英語:Adenosine diphosphate receptor inhibitor)類 ... Paul-Clark, Mark J.; Cao, Thong van; Moradi-Bidhendi, Niloufar; Cooper, Dianne & Gilroy, Derek W. 15-epi-lipoxin A4-mediated ...
The classical estrogen receptors first characterized in 1958[6] are water-soluble proteins located in the interior of cells that are activated by estrogenenic hormones such as estradiol and several of its metabolites such as estrone or estriol. These proteins belong to the nuclear hormone receptor class of transcription factors that regulate gene transcription. Since it takes time for genes to be transcribed into RNA and translated into protein, the effects of estrogens binding to these classical estrogen receptors is delayed. However, estrogens are also known to have effects that are too fast to be caused by regulation of gene transcription.[7] In 2005, it was discovered that a member of the G protein-coupled receptor (GPCR) family, GPR30 also binds with high affinity to estradiol and is responsible in part for the rapid non-genomic actions of estradiol. Based on its ability to bind estradiol, GPR30 was renamed as G protein-coupled estrogen receptor (GPER). Unlike the other members of the GPCR ...
This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B.[6] ...
Défhosfáit adanóisín Adenosine diphosphate (ADP). *Aonfhosfáit adanóisín Adenosine monophosphate (AMP). *Trífhosfáit adanóisín ...
The 5-HT1 receptors are a subfamily of the 5-HT serotonin receptors that bind to the endogenous neurotransmitter serotonin (also known as 5-hydroxytryptamine, or 5-HT).[1] The 5-HT1 subfamily consists of five G protein-coupled receptors (GPCRs) that are coupled to Gi/Go and mediate inhibitory neurotransmission, including 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor, as it was reclassified as the 5-HT2C receptor.[2] For more information, please see the respective main articles of the individual subtypes: ...
The ring domain is an important element of ubiquitin E3 ligases, which catalyze protein ubiquitination. Ubiquitin is a small ... "Adenosine nucleotide modulates the physical interaction between hMSH2 and BRCA1". Oncogene. 20 (34): 4640-9. doi:10.1038/sj.onc ... "Activation of the E3 ligase function of the BRCA1/BARD1 complex by polyubiquitin chains". EMBO J. 21 (24): 6755-62. doi ...
The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it. ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of ... Adenosine A3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular ...
Adenosine receptor A3. Details. Name. Adenosine receptor A3. Synonyms. Not Available. Gene Name. ADORA3. Organism. Humans. ... Sajjadi FG, Firestein GS: cDNA cloning and sequence analysis of the human A3 adenosine receptor. Biochim Biophys Acta. 1993 Oct ... Salvatore CA, Jacobson MA, Taylor HE, Linden J, Johnson RG: Molecular cloning and characterization of the human A3 adenosine ... G-protein coupled adenosine receptor activity. Specific Function. Receptor for adenosine. The activity of this receptor is ...
Buy our Recombinant Human Adenosine A3 Receptor protein. Ab114790 is a protein fragment produced in Wheat germ and has been ... Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. Possible role ...
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase (PubMed:8234299 ... Adenosine receptor A3Add BLAST. 318. Amino acid modifications. Feature key. Position(s). DescriptionActions. Graphical view. ... "Molecular cloning and characterization of the human A3 adenosine receptor.". Salvatore C.A., Jacobson M.A., Taylor H.E., Linden ... sp,P0DMS8,AA3R_HUMAN Adenosine receptor A3 OS=Homo sapiens OX=9606 GN=ADORA3 PE=1 SV=1 ...
... ; Adenosine Receptor A3 (ADORA3) pipeline Target... ... Adenosine Receptor A3 - Pipeline Review, H1 2020 SUMMARY According to the recently published report ... Adenosine Receptor A3 (ADORA3) - The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor. Adenosine A3 ... Adenosine Receptor A3 (ADORA3) - Dormant Products. Adenosine Receptor A3 (ADORA3) - Discontinued Products. Adenosine Receptor ...
The A3 adenosine receptor (A3AR) has emerged as a therapeutic target with A3AR agonists to tackle the global challenge of ... Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10. ... Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10. ...
Protein target information for Adenosine receptor A3 (rabbit). Find diseases associated with this biological target and ...
They have enabled my goal as editor to make A Adenosine Receptors from Cell Biology to Pharmacology and 3 Therapeutics an up ... documents the present state of knowledge of the adenosine A receptor. It covers a wide range of information, including data ... aspects and molecular biology of the A receptor provides a solid basis for its future development as a target for 3 adenosine- ... You are browsing: All A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics ...
Adenosine receptors in colon carcinoma tissues and colon tumoral cell lines: focus on the A3 adenosine subtype. J Cell Physiol ... Novel N6-substituted adenosine 5′-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic ... A3 adenosine receptor signaling contributes to airway inflammation and mucus production in adenosine deaminase-deficient mice. ... Activation of protein kinase B by adenosine A1 and A3 receptors in newborn rat cardiomyocytes. J Mol Cell Cardiol. 2004; 37: ...
... is an A3AR selective agonist containing multiple receptor affinity- and selectivity-enhancing modifications and a therapeutic ... These data will be useful to guide rational design of drugs targeting A3AR, considering efficacy, metabolic elimination, and ...
Adenosine acts through an A3 receptor to prevent the induction of murine anti-CD3-activated killer T cells.. Hoskin DW1, Butler ... Adenosine, therefore, acts through an A(3) receptor to prevent AK-T cell induction. Tumor-associated adenosine may act through ... Adenosine, a purine nucleoside found at high levels in solid tumors, is able to suppress the recognition/adhesion and effector ... Interleukin-2 and interferon-gamma synthesis by AK-T cells was also inhibited by adenosine. AK-T cells express mRNA coding for ...
... and A3 adenosine receptors in lymphoid organs.. Lukashev DE1, Smith PT, Caldwell CC, Ohta A, Apasov SG, Sitkovsky MV. ... No significant changes were observed in A2b, A1, and A3 mRNA levels in the thymus or lymph nodes of A2a receptor-deficient mice ... Here, we show that most of the cAMP response to adenosine is abolished in lymphoid tissues of A2a receptor-deficient mice, ... These data suggest that regulation of the expression of A2b, A1, and A3 receptors is not affected significantly by the absence ...
When appropriately modified, they show selectivity toward A1 or A3 receptors, which results in a variety of therapeutic ... Thiazole and thiadiazole analogues have been recently proposed as a novel promising class of adenosine A1 and A3 receptor ... QSAR study on thiazole and thiadiazole analogues as antagonists for the adenosine A1 and A3 receptors Bioorg Med Chem. 2005 Sep ... In this work, we carried out a QSAR study on thiazole and thiadiazole analogues as antagonists for adenosine A1 and A3 ...
... highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. ... CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential ... CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential ...
A2B and A3, which belong to the G protein-coupled receptor (GPCR) superfamily. The human A3AR (hA3AR) subtype is implicated in ... Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, ... Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, ... Expression of Adenosine A2B Receptor and Adenosine Deaminase in Rabbit Gastric Mucosa ECL Cells ...
A way to block a pain pathway in animal models of chronic neuropathic pain including pain caused by chemotherapeutic agents and bone cancer pain suggesting a promising new approach to pain r... Read more ...
Required for the formation of a threonylcarbamoyl group on adenosine at position 37 (t(6)A37) in tRNAs that read codons ... sp,O86793,TSAD_STRCO tRNA N6-adenosine threonylcarbamoyltransferase OS=Streptomyces coelicolor (strain ATCC BAA-471 / A3(2) / ... tRNA N6-adenosine threonylcarbamoyltransferaseUniRule annotation. ,p>Manual validated information which has been generated by ... Required for the formation of a threonylcarbamoyl group on adenosine at position 37 (t6A37) in tRNAs that read codons beginning ...
... simple luminescent calcium flux assays using irradiated AequoScreen cells tranfected with human adenosine A3 receptor - no cell ... Frozen Cells validated for calcium testing: Adenosine A3 receptor, human recombinant, in CHO-K1 host cell. We provide one vial ...
News Targeting the A3 Adenosine Receptor Activates "Off Signals" for Pain Targeting the A3 Adenosine Receptor Activates "Off ... reports the discovery of drugs targeting the A3 adenosine receptor (A3AR) that can "turn off" pain signals in the spinal cord ...
... simple binding and functional assays using irradiated cells transfected with human adenosine A3 receptor - no cell culture ... Frozen Cells validated for cAMP testing: Adenosine A3 receptor, human recombinant, in CHO-K1 host cell. We provide one vial of ...
7. U.S. Provisional Application 62/033,723, filed August 6, 2014, titled "A3 Adenosine Receptor Agonists" [HHS Ref. No. E-210- ... 1. U.S. Patent 8,735,407, issued May 27, 2014, titled "Purine Derivatives As A3 Adenosine Receptor-Selective Agonists" [HHS Ref ... 6. U.S. Provisional Application 61/909,742, filed November 27, 2013, titled "A3 Adenosine Receptor Agonists" [HHS Ref. No. E- ... The subject inventions describe selective A3 Adenosine Receptor (A3AR) agonists, and their in vivo activity reducing or ...
To investigate the expression of adenosine A3 receptor (A3AR) in human colonic epithelial cells and the effects of A3AR ... and A3 receptor [1, 2]. Adenosine A3 receptor (A3AR) is a Gi-protein-coupled receptor that, when being activated, decreases ... Activation of Adenosine A3 Receptor Alleviates TNF-α-Induced Inflammation through Inhibition of the NF-κB Signaling Pathway in ... Activation of Adenosine A3 Receptor Alleviates TNF-α-Induced Inflammation through Inhibition of the NF-κB Signaling Pathway in ...
N)-Methanocarba Adenosine Derivatives and Their Dendrimer Conjugates as A3 Receptor Agonists (U.S. Patent Application Number 61 ... N)-Methanocarba Adenosine Derivatives and Their Dendrimer Conjugates as A3 Receptor Agonists (U.S. Patent Application Number 61 ... Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A3 adenosine receptor agonists, pharmaceutical ... https://www.google.com/patents/WO2011068978A1?cl=en&dq=methanocarba+Adenosine+Derivatives&hl=en&sa=X&ved=0ahUKEwjPo- ...
Adenosine A3 receptor agonist inhibits retinal ganglion cell apoptosis in vivo Joana Galvao; Li Guo; Ana Raquel Santiago; ... Adenosine A3 receptor agonist inhibits retinal ganglion cell apoptosis in vivo You will receive an email whenever this article ... Joana Galvao, Li Guo, Ana Raquel Santiago, Antonio Ambrosio, M Francesca Cordeiro; Adenosine A3 receptor agonist inhibits ... Adenosine and three of its four receptors have been identified at the level of retinal ganglion cell (RGC) layer. Our previous ...
This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide ... ... 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 range ... They have enabled my goal as editor to make "A Adenosine Receptors from Cell Biology to Pharmacology and 3 Therapeutics" an up ...
Three A3 adenosine receptor (AR) antagonists (1-3) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously ... Three A3 adenosine receptor (AR) antagonists (1-3) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously ... on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine ... on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine ...
Immunohistology confirmed the presence of the A3 adenosine receptor in RGC layer. However, the expression of A3 adenosine ... The Activation Of A3 Adenosine Receptor Inhibits Retinal Ganglion Cell Apoptosis Joana M. Galvao; Eduardo M. Normando; Li Guo; ... The Activation Of A3 Adenosine Receptor Inhibits Retinal Ganglion Cell Apoptosis You will receive an email whenever this ... Immunohistological analysis of A3 adenosine receptor expression was performed in 5 µm thick paraffin sections from enucleated ...
Chronic Morphine-Induced Changes in Signaling at the A3 Adenosine Receptor Contribute to Morphine-Induced Hyperalgesia, ... A3 Adenosine Receptor and Morphine-Induced Adverse Effects. Timothy M. Doyle, Tally M. Largent-Milnes, Zhoumou Chen, Vasiliki ... A3 Adenosine Receptor and Morphine-Induced Adverse Effects. Timothy M. Doyle, Tally M. Largent-Milnes, Zhoumou Chen, Vasiliki ... Chronic Morphine-Induced Changes in Signaling at the A3 Adenosine Receptor Contribute to Morphine-Induced Hyperalgesia, ...
NECA from human recombinant adenosine A3 receptor expressed in human HeLa cell membrane at 10 uM. ...
The A3 adenosine receptor (A3AR) is highly expressed in tumors and was suggested as a target for cancer treatment. In this ... The A3 adenosine receptor agonist CF102 induces apoptosis of hepatocellular carcinoma via de-regulation of the Wnt and NF-κB ... Bar-Yehuda, S., Stemmer, S.M., Madi, L., Castel, D., Ochaion, A., Cohen, S. ... Fishman, P. (2008). The A3 adenosine receptor ... The A3 adenosine receptor agonist CF102 induces apoptosis of hepatocellular carcinoma via de-regulation of the Wnt and NF-κB ...
  • Adenosine A3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. (wikipedia.org)
  • Adenosine A3 receptors are G protein-coupled receptors that mediates a sustained cardioprotective function during cardiac ischemia. (marketpublishers.com)
  • They have enabled my goal as editor to make "A Adenosine Receptors from Cell Biology to Pharmacology and 3 Therapeutics" an up to date, scientifically excellent, reference source, attractive to basic and clinical scientists alike, a reality. (foyles.co.uk)
  • Background- Endogenous adenosine can protect the overloaded heart against the development of hypertrophy and heart failure, but the contribution of A 1 receptors (A 1 R) and A 3 receptors (A 3 R) is not known. (ahajournals.org)
  • 2-5 A 1 receptors (A 1 R) and A 3 receptors (A 3 R) are expressed in cardiomyocytes, and a substantial body of evidence indicates that adenosine can protect the heart during and after an ischemic insult. (ahajournals.org)
  • 6,7 Liao et al 8 demonstrated that the adenosine analogue 2-chloroadenosine (CADO) also attenuated pressure overload-induced LV hypertrophy through activation of the A 1 R. Similar to A 1 R, the A 3 R are Gi protein-coupled receptors that have been shown to activate similar downstream signaling pathways. (ahajournals.org)
  • Analysis of A2a receptor-deficient mice reveals no significant compensatory increases in the expression of A2b, A1, and A3 adenosine receptors in l. (nih.gov)
  • No significant changes were observed in A2b, A1, and A3 mRNA levels in the thymus or lymph nodes of A2a receptor-deficient mice, but small increases in mRNA expression of these receptors were detected in the spleen. (nih.gov)
  • These data suggest that regulation of the expression of A2b, A1, and A3 receptors is not affected significantly by the absence of A2a receptors and may provide further explanation of earlier in vivo observations of increased tissue damage and of longer persistence of proinflammatory cytokines in animals with inactivated A2a receptors. (nih.gov)
  • When appropriately modified, they show selectivity toward A1 or A3 receptors, which results in a variety of therapeutic potentialities of these ligands. (nih.gov)
  • In this work, we carried out a QSAR study on thiazole and thiadiazole analogues as antagonists for adenosine A1 and A3 receptors. (nih.gov)
  • Adenosine is released from a variety of cells in response to inflammatory and metabolic stress and exerts its physiological functions by interacting with 4 subtypes of adenosine receptors, including A1, A2A, A2B, and A3 receptor [ 1 , 2 ]. (hindawi.com)
  • Adenosine receptors (AR) have been considered as potential therapeutic targets in neurodegenerative diseases, such as glaucoma. (arvojournals.org)
  • Adenosine and three of its four receptors have been identified at the level of retinal ganglion cell (RGC) layer. (arvojournals.org)
  • This gene encodes a protein that belongs to the family of adenosine receptors, which are G-protein-coupled receptors that are involved in a variety of intracellular signaling pathways and physiological functions. (creativebiomart.net)
  • We selected most pathways adora3 participated on our site, such as Adenosine P1 receptors, Class A/1 (Rhodopsin-like receptors), G alpha (i) signalling events, which may be useful for your reference. (creativebiomart.net)
  • 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. (garvan.org.au)
  • Although activation of A 3 adenosine receptors attenuates reperfusion lung injury and associated apoptosis, the signaling pathway that mediates this protection remains unclear. (springer.com)
  • In this study we therefore compared the phosphorylation of extracellular-regulated kinase 1/2 (ERK1/2) via the four known human adenosine receptors A 1 , A 2A , A 2B , and A 3 , stably transfected into Chinese hamster ovary (CHO) cells. (aspetjournals.org)
  • The adenosine analog 5′- N -ethylcarboxamidoadenosine (NECA), known to act on all subtypes, had no effect on untransfected CHO cells, but did cause a substantial time- and dose-dependent phosphorylation in CHO cells transfected with each of the receptors. (aspetjournals.org)
  • NECA acting on adenosine A 2B receptors was much more potent in stimulating ERK1/2 phosphorylation (EC 50 = 19 nM) than cAMP formation (EC 50 = 1.4 μM). (aspetjournals.org)
  • Concentrations of adenosine that occur physiologically caused an increased phosphorylation after 5 min in CHO cells transfected with any one of the four adenosine receptors. (aspetjournals.org)
  • In conclusion, this study shows that all the human adenosine receptors transfected into CHO cells are able to activate ERK1/2 at physiologically relevant concentrations of the endogenous agonist. (aspetjournals.org)
  • they've got enabled my aim as editor to make "A Adenosine Receptors from mobile Biology to Pharmacology and three Therapeutics" an up to the moment, scientifically very good, reference resource, beautiful to simple and medical scientists alike, a truth. (b-construction.ru)
  • Adenosine is an endogenous and ubiquitous nucleoside that exerts many biological functions through interaction with 4 distinct subtypes of G protein-coupled receptors divided into A1, A2A, A2B, and A3. (unife.it)
  • Recent studies have shown the presence of A3 receptors on neutrophils, which represent the majority of circulating leukocytes and are the first cells to be recruited into a site of tissue inflammation in defending the body against infection. (unife.it)
  • Adenosine released from cells interacts with membrane receptors (adenosine receptors, ARs). (mybiosource.com)
  • cell sorting at adenosine A 1 / A 2A / A 3 receptors use solutions up to 100 nM. (hellobio.com)
  • To date adenosine receptors have been classified into three main classes: (A 1 , A 2 and A 3 . (russianpatents.com)
  • The sequence of the receptors of adenosine A 3 was recently identified from a cDNA library of rat testis. (russianpatents.com)
  • Adenosine receptors were found in several organs and regulate their functions. (russianpatents.com)
  • In the CNS, adenosine inhibits synaptic release of neurotransmitters, and this effect is mediated by receptors And 1 . (russianpatents.com)
  • In the heart of the receptors And 1 mediate negative inotropic, chronotropic and dromotropic effects of adenosine. (russianpatents.com)
  • Receptors of adenosine A 2a that are localized in a relatively higher number in the striatum, show functional interaction with dopamine receptors in the regulation of synaptic conduction. (russianpatents.com)
  • Adenosine receptors A 2a on endothelial and gladkomyshechne the x cells responsible for induced by the adenosine vasodilation (P.G. Baraldi et al. (russianpatents.com)
  • Based on the identification of mRNA receptors adenosine A 2b widely distributed in various tissues. (russianpatents.com)
  • The levels of expression of receptors of adenosine A 3 are relatively low compared with other subtypes, and depend greatly on the species. (russianpatents.com)
  • Receptors of adenosine A 3 expressed primarily in the Central nervous system, testis and the immune system and, apparently, involved in the modulation of release of mediators of mast cells in allergic reactions of immediate type and migration of neutrophilic granulocytes (Y.Chen et al. (russianpatents.com)
  • The adenosine receptors (or P1 receptors [1] ) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand . (wikipedia.org)
  • The adenosine receptors are commonly known for their antagonists caffeine and theophylline , whose action on the receptors produces the stimulating effects of coffee , tea and chocolate . (wikipedia.org)
  • Caffeine keeps you awake by blocking adenosine receptors. (wikipedia.org)
  • Xanthine derivatives such as caffeine and theophylline act as non-selective antagonists at A 1 and A 2A receptors in both heart and brain and so have the opposite effect to adenosine, producing a stimulant effect and rapid heart rate. (wikipedia.org)
  • We tested a panel of naturally occurring nucleosides for their affinity towards adenosine receptors. (duhnnae.com)
  • A3 Adenosine Receptors from Cell Biology to Pharmacology and by John R. Fozard (auth. (stainlessqa.com)
  • This booklet "A3 Adenosine Receptors from telephone Biology to Pharmacology and Therapeutics " files the current country of information of the adenosine A3 receptor. (stainlessqa.com)
  • Adenosine A3 receptors are G protein-linked receptors that functionality in body structure and intracellular signaling and are inquisitive about inflammatory responses and mediating cellphone proliferation and mobilephone demise. (stainlessqa.com)
  • A3 Adenosine Receptors from mobile Biology to Pharmacology and Therapeutics" is an up to the moment and scientifically very good resource of knowledge, beautiful to simple and medical scientists alike. (stainlessqa.com)
  • A central role of A 2A and A 3 adenosine receptors (ARs) in mechanisms of inflammation has been reported in different pathologies. (biomedcentral.com)
  • Several papers report a central role of adenosine receptors (ARs) in mechanisms of inflammation associated to various pathologies suggesting that their stimulation has a different effect on the release of several pro-inflammatory cytokines [ 16 - 18 ]. (biomedcentral.com)
  • The purpose of this study was to examine what role adenosine receptors may play in the generation of the ERG. (hi.is)
  • Adenosine agonist CGS21680 and antagonist ZM241385 for A2A receptors, and adenosine agonist 2-CI-IB-MECA and antagonist VUF5574 for A3 receptors along with exogenous adenosine were injected into the vitreous and their effects on the ERG components were examined, along with ERG flicker responses. (hi.is)
  • The results show that the ERG is influenced by both adenosine receptors to varying degrees. (hi.is)
  • Retinal neurons that contain A2A and/or A3 adenosine receptors contribute to the generation of the ERG b-wave and oscillatory potentials. (hi.is)
  • 1,2,4]Triazolo[1,5-c]pyrimidine Nucleus as Adenosine Receptor Antagonists: Shift in Selectivity from A2A to A3 Adenosine Receptors. (units.it)
  • The role of adenosine A3 receptors in synaptic transmission under severe (7 min) and shorter (2-5 min) ischemic conditions, obtained by oxygen and glucose deprivation (OGD), was investigated in rat hippocampal slices. (ewha.ac.kr)
  • This indicates that A3 receptors, stimulated by selective A3 agonists, undergo desensitization during OGD. (ewha.ac.kr)
  • It is inferred that CA1 hippocampal A3 receptors stimulated by adenosine released during brief ischemia (2 and 5 min) might exert A1-like protective effects on neurotransmission. (ewha.ac.kr)
  • Ohta, A. & Sitkovsky, M. Role of G-protein-coupled adenosine receptors in downregulation of inflammation and protection from tissue damage. (nature.com)
  • Such immunometabolic modulation has shown to be a promising therapeutic target through blockade of adenosine receptors which mediate adenosine's immunosuppressive function, or cancer-associated ectonucleotidases CD39 and CD73 that catalyze the synthesis of adenosine. (springer.com)
  • A3 adenosine receptor (A3AR) is the only adenosine subtype to be over expressed in inflammatory and cancer cells, thus making it a potential target for therapy. (marketpublishers.com)
  • CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. (adooq.com)
  • New research undertaken at Saint Louis University, in concert with researchers from the National Institutes of Health, the University of Arizona, and 2 institutes in Quebec, reports the discovery of drugs targeting the A3 adenosine receptor (A3AR) that can "turn off" pain signals in the spinal cord to provide relief from chronic pain. (painweek.org)
  • Adenosine A3 receptor (A3AR) is a G i -protein-coupled receptor that, when being activated, decreases intracellular cAMP levels [ 3 ]. (hindawi.com)
  • The A3 adenosine receptor (A3AR) is highly expressed in tumors and was suggested as a target for cancer treatment. (spandidos-publications.com)
  • The A3‐adenosine receptor (A3AR) has recently emerged as a key regulator of neutrophil behaviour. (nottingham.ac.uk)
  • 1,3] We decided to develop a fluorescent-ligand for the A3AR (A3 adenosine receptor) subtype using the pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine (PTP) as active scaffold at the hA3AR. (units.it)
  • The A3 adenosine receptor (A3AR) is attributed with multiple beneficial actions in ischemic-reperfused myocardium, including modulation of oncotic and apoptotic cell death and enhancement of contractile function. (edu.au)
  • Available evidence indicates that this receptor sub-type is minimally activated by endogenous adenosine during ischemia (A3AR antagonists exerting no effects on ischemic outcome), and is thus amenable to activation with exogenous agonists. (edu.au)
  • Nonetheless, A3ARs may be more promising as therapeutic "anti-ischemic" targets compared with other adenosine receptor subtypes, since A3AR agonists elicit fewer and less significant side-effects. (edu.au)
  • Our findings suggest that this goal may be achieved by focusing future work on the A3 adenosine receptor (A3AR) pathway, in particular, as its activation provides robust pain reduction across several types of pain. (medicalnewstoday.com)
  • A recent study reported that an A3 adenosine receptor (A3AR) antagonist attenuated the progression of renal fibrosis . (bvsalud.org)
  • The adenosine A3 receptor (A3AR) regulates SERT via protein kinase G (PKG) and other signaling pathways leading to enhanced SERT surface expression and catalytic activity. (biomedcentral.com)
  • The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it. (wikipedia.org)
  • Adenosine Receptor A3 (ADORA3) pipeline Target constitutes close to 16 molecules. (marketpublishers.com)
  • Adenosine Receptor A3 (ADORA3) - The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor. (marketpublishers.com)
  • It also reviews key players involved in Adenosine Receptor A3 (ADORA3) targeted therapeutics development with respective active and dormant or discontinued projects. (marketpublishers.com)
  • adora3 has several biochemical functions, for example, G-protein coupled adenosine receptor activity. (creativebiomart.net)
  • 70 Adenosine A3 Receptor (ADORA3) 抗体 from 18 manufacturers are available on www.antibodies-online.cn. (antibodies-online.cn)
  • Adenosine Receptor A3 (ADORA3) - Pipeline Review, H2 2018 Summary Adenosine Receptor A3 (ADORA3) pipeline Target constitutes close to 17 molecules. (reportbuyer.com)
  • Progressive activation of M2-related program was characterized by induction of tissue remodeling and immunoregulatory genes such as matrix metalloproteinase ( MMP ) 2 , MMP7 , and adenosine A3 receptor ( ADORA3 ). (jimmunol.org)
  • abstract = "The A3 adenosine receptor has been implicated in modulation of cell growth. (elsevier.com)
  • abstract = "To examine the cardiovascular response to prostaglandin E1 infusion, we observed hemodynamic changes including left ventricular diameter (an ultrasonic crystal pair) during PGE1-induced hypotension in anesthetized open-chest dogs. (elsevier.com)
  • Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein A, a, R2, and R3 are as defined in the specification. (nih.gov)
  • Thus, increasing the receptor level improves the myocyte sensitivity to the endogenous adenosine, which in turn causes all of the cardioprotective effects found for exogenously administered adenosine agonists. (garvan.org.au)
  • The selective A 3 adenosine receptor agonists IB-MECA (0.05 mg/kg, 0.1 mg/kg, or 0.3 mg/kg) and MRS3558 (0.05 mg/kg or 0.1 mg/kg) were administered before reperfusion. (springer.com)
  • We set out to characterize the effect of this mutation on the efficacy of two agonists at multiple signalling pathways downstream of the adenosine A3 receptor. (worktribe.com)
  • Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive research into the effects of blocking or stimulating the individual adenosine receptor subtypes, which is now resulting in a new generation of more selective drugs with many potential medical uses. (wikipedia.org)
  • At micromolar concentrations, the A 3 agonists N 6 -(3-iodobenzyl)-adenosine-5'-N- methyluronamide (IB-MECA) and its 2-chloro derivative Cl-IB-MECA reduced cell number, with no effects on either parental CHO cells (not expressing any adenosine receptor), or CHO cells transfected with the human A 1 receptor. (elsevier.com)
  • The effects of selective A3 agonists or antagonists were examined on field excitatory postsynaptic potentials (fEPSPs) extracellularly recorded at the dendritic level of the CA1 pyramidal region. (ewha.ac.kr)
  • Similar results were obtained when severe OGD was carried out with a long, receptor-desensitizing exposure to various selective A3 agonists: 5′-N-methylcarboxamidoadenosine derivatives Cl-IB-MECA (N6-(3-iodobenzyl)-2-chloro), VT72 (N6-methoxy-2-phenylethynyl), VT158 (N6-methoxy-2-phenylethynyl), VT160 (N6-methoxy-2-(2-pyridinyl)-ethynyl), and VT163 (N6-methoxy-2-p-acetylphenylethynyl) and AR132 (N6-methyl-2-phenylethynyladenosine). (ewha.ac.kr)
  • Similar results were obtained for 2- or 5-min OGD applied in the presence of each of the A3 agonists tested. (ewha.ac.kr)
  • Shorter exposure to A3 agonists significantly delayed the recovery of fEPSP amplitude after 5-min OGD. (ewha.ac.kr)
  • Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18). (wikipedia.org)
  • Thiazole and thiadiazole analogues have been recently proposed as a novel promising class of adenosine A1 and A3 receptor antagonists. (nih.gov)
  • Three A 3 adenosine receptor (AR) antagonists ( 1-3 ) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously investigated by us were modified by inserting a methyl group on their ether or thioether side chains. (rsc.org)
  • Finally, in lymphocytes, activation of A3 receptor subtype would result in a reduction of the accession of killer T cells to tumor cells by exerting an immunosuppressive effect and suggesting a role for antagonists of this receptor as anti-tumoral drugs. (unife.it)
  • 1,2,4]Triazolo[1,5-c]pyrimidine derivatives are reported in literature as A2A adenosine receptor (AR) antagonists useful for the treatment of Parkinson's disease (PD), senile dementia and depression (1). (units.it)
  • A number of selective A3 ligands are available. (wikipedia.org)
  • Application of datasets by using CODESSA software led to QSAR equations based on three and four descriptors for the adenosine A1 and A3 receptor ligands, respectively. (nih.gov)
  • Fluorescent ligands for the A3 adenosine receptor. (units.it)
  • methods of their production, new intermediate compounds of described methods of production, a pharmaceutical composition containing these compounds, and application of compounds of common formula (I) and their pharmaceutical acceptable salts as ligands of adenosine A3 receptor in treatment of different diseases. (russianpatents.com)
  • Identification of an increasing number of physiological functions mediated by adenosine, and the opening of new adenosine receptor subtypes provides opportunities for therapeutic application of certain ligands (Poulse S.A. and R.J. Quinn Bioorganic and Medicinal Chemistry 6:619, 1998). (russianpatents.com)
  • Some of these compounds are still derived from adenosine or from the xanthine family, but researchers in this area have also discovered many selective adenosine receptor ligands that are entirely structurally distinct, giving a wide range of possible directions for future research. (wikipedia.org)
  • Both N-2-isopentenyladenosine IPA and racemic zeatin riboside were shown to be selective human adenosine A3 receptor hA3R ligands with affinities in the high nanomolar range Ki values of 159 and 649 nM, respectively. (duhnnae.com)
  • All the ligands tested along with exogenous adenosine had a significant statistical effect on one ERG component or another. (hi.is)
  • Jacobson, K.A. Recent developments in adenosine receptor ligands and their potential as novel drugs. (units.it)
  • A novel class of adenosine A3 receptor ligands.Structure affinity profile of a series of isoquinoline and quinazoline compounds. (vu.nl)
  • The CellAura fluorescent adenosine A 3 antagonist [XAC] ligand was shown to antagonize the activity of the adenosine receptor agonist, NECA, in three separate recombinant CHO cell lines expressing the human A 1 , A 2A or A 3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene. (hellobio.com)
  • Addition of CellAura fluorescent adenosine A 3 antagonist [XAC] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent adenosine A 3 antagonist [XAC] has no intrinsic agonist activity. (hellobio.com)
  • To determine the apparent KD for CellAura fluorescent adenosine A 3 antagonist [XAC], cells were treated with varying concentrations of NECA alone, or in the presence of 1µM CellAura fluorescent adenosine A 3 antagonist [XAC], and the cyclic AMP-induced expression of SPAP measured. (hellobio.com)
  • The following papers have cited the use of CA200645 CellAura fluorescent adenosine A 3 antagonist [XAC] (HB7812) from Hello Bio. (hellobio.com)
  • Both A 3 agonist 2-CI-IB-MECA and antagonist VUF5574 along with exogenously applied adenosine caused a significant statistical increase in the amplitude of the a-wave, while the A 2A agonist CGS21680 and antagonist ZM241385 did not. (hi.is)
  • Blocking the A3 adenosine receptor with an antagonist caused an increase in the scotopic ERG a- and b-wave. (hi.is)
  • On the basis of obtained results, the optimization of substitutions allow us, after 4 series (147compounds) of [1,2,4]triazolo[1,5-c]pyrimidine derivatives, to discover a potent and selective A3 AR antagonist, with a Ki of 0.47 nM. (units.it)
  • The novel, selective A3 antagonist LJ1251 ((2R,3R,4S)-2-(2-chloro-6-(3-iodobenzylamino)-9H-purin-9-yl)tetrahydrothiophene-3,4-diol, 0.1-10 nM) protected hippocampal slices from irreversible fEPSP depression induced by severe OGD and prevented or delayed the appearance of anoxic depolarization. (ewha.ac.kr)
  • The selective A3 antagonist MRS1523 (3-propyl-6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-3-pyridine carboxylate, 100 nM) reduced fEPSP depression evoked by 2-min OGD and induced a faster recovery of fEPSP amplitude after 5-min OGD. (ewha.ac.kr)
  • Adenosine exerts multiple functions through activation of individual adenosine receptor subtypes. (ahajournals.org)
  • Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A 1 , A 2A , A 2B and A 3 , which belong to the G protein-coupled receptor (GPCR) superfamily. (mdpi.com)
  • For therapeutic use, it is important to ensure that the molecules are selective to other adenosine receptor, so do not contact, or be contacted only in case of very high concentrations, with subtypes And 1 , A 2a and A 2b adenosine receptor. (russianpatents.com)
  • In the past most of the anti-inflammatory effects of this nucleoside were thought to be due to the activation of the A2A subtype, however more recently, the involvement of the A3 subtype has been also considered relevant for the outcome of inflammation. (unife.it)
  • AequoScreen® Double Transfected Cell Lines: Adenosine, A3 subtype. (perkinelmer.co.uk)
  • Hence, activation of the human A 3 receptor in A 3 R-CHO results in markedly impaired cell cycle progression, suggesting an important role for this adenosine receptor subtype in cell cycle regulation and cell growth. (elsevier.com)
  • Adenosine, a purine nucleoside found at high levels in solid tumors, is able to suppress the recognition/adhesion and effector phases of killer lymphocyte-mediated tumor cell destruction. (nih.gov)
  • The purine nucleoside adenosine modulates diverse physiological functions including induction of sedation, vasodilatation, suppression of cardiac rate and contractility, neurotransmitter release, inhibition of platelet aggregation and lipolysis. (mybiosource.com)
  • KeywordsAdenosine A3 receptor N-2-isopentenyladenosine IPA Antitumor agent Modified nucleoside HPLC Zeatin riboside Electronic supplementary materialThe online version of this article doi:10.1007-s11302-011-9244-9 contains supplementary material, which is available to authorized users. (duhnnae.com)
  • Frozen Cells validated for calcium testing: Adenosine A3 receptor, human recombinant, in CHO-K1 host cell. (perkinelmer.com)
  • Frozen Cells validated for cAMP testing: Adenosine A3 receptor, human recombinant, in CHO-K1 host cell. (perkinelmer.com)
  • In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury. (wikipedia.org)
  • Adenosine is an important mediator of the endogenous defense against ischemia-induced injury in the heart. (garvan.org.au)
  • 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. (garvan.org.au)
  • 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. (garvan.org.au)
  • Prolonged hypoxia with glucose deprivation, causing myocyte injury and adenosine release, was used to simulate ischemia in cultured chick embryo ventricular myocytes. (garvan.org.au)
  • During simulated ischemia, cultured myocytes with enhanced expression of the human A3 receptor and showed significantly higher ATP content, fewer cells killed, and less creatine kinase released into the medium than either control or mock-transfected myocytes. (garvan.org.au)
  • Also, increased expression of the A3 receptor caused an enhanced cardioprotective effect by the preconditioning ischemia. (garvan.org.au)
  • Overexpressing the adenosine A1 receptor also led to increased protection against ischemia-induced myocyte injury as well as an enhanced preconditioning effect. (garvan.org.au)
  • Adenosine at levels reached during ischemia (3 μM) induced a more pronounced, but still transient, activation of ERK1/2. (aspetjournals.org)
  • The concentration of adenosine in the normal kidney increases markedly during renal hypoxia , ischemia , and inflammation . (bvsalud.org)
  • Severe ischemia would transform the A3 receptor-mediated effects from protective to injurious. (ewha.ac.kr)
  • The aim of our study was to analyze and compare preventive influences of ischemic preconditioning , adenosine and prostaglandin E1 in the experimental model of hepatic ischemia / reperfusion injury . (bvsalud.org)
  • Conclusions- Adenosine exerts protective effects on the overloaded heart, but the A 3 R acts counter to the protective effect of adenosine. (ahajournals.org)
  • The effect of adenosine on cardiac function was discovered already in 1929 (Drury and Szentgyörgyi, J Physiol 68:213, 1929). (russianpatents.com)
  • Our results show that Engrailed/ephrin A5 synergy in growth cone collapse involves adenosine A1 receptor activation after Engrailed-dependent ATP synthesis, followed by ATP secretion and hydrolysis to adenosine. (biologists.org)
  • Engrailed/ATP enhancement of growth cone collapse occurs via activation of the adenosine A1 receptor (A1R), which is present at higher concentrations in temporal than nasal growth cones. (biologists.org)
  • The protective effects of A 3 adenosine receptor activation are mediated in part through upregulation of phosphorylated ERK. (springer.com)
  • In particular, the activation of the A3 receptor on this cellular type leads to the inhibition of degranulation and superoxide anion production with consequent anti-inflammatory effects. (unife.it)
  • The results of this study, obtained by using real time RT-PCR and Western blotting, show that adenosine is able to increase both MMP9 mRNA and protein levels through the activation of the A3 adenosine receptor. (unife.it)
  • The A3 receptor activation also led to an increase in extracellular levels of MMP9 in the supernatants of glioblastoma cells as evaluated by ELISA and gelatine zymography assays. (unife.it)
  • Overall, these results suggest that adenosine, through activation of the A3 receptor, modulates MMP9 protein levels and plays a role in the invasion of U87MG cells. (unife.it)
  • Abbracchio, Maria P. / Activation of the A3 adenosine receptor affects cell cycle progression and cell growth . (elsevier.com)
  • Fig. 3: Effects of adenosine receptor A2 A signalling on pathways involved in T cell activation. (nature.com)
  • Evaluation of the anticoagulants EDTA and citrate, theophylline, adenosine, and dipyridamole (CTAD) for assessing platelet activation on the ADVIA 120 hematology system. (thefreelibrary.com)
  • Experimental Approach: Residue W6.48 in the human adenosine A3 receptor fused to yellow fluorescent protein was mutated to phenylalanine and expressed in CHO-K1 cells containing a cAMP response element reporter gene. (worktribe.com)
  • The protein product of this gene, adenosine deaminase 2 (ADA2), is an extracellular enzyme that breaks down adenosine and may also serve as a growth factor. (wikipedia.org)
  • In this study, we focused on assessing the A3 receptor and its modulation using the A3 agonist, 2-Cl-IB-MECA, in a rat model of RGC apoptosis. (arvojournals.org)
  • The potential neuroprotective effect of the A3 adenosine receptor agonist 2-Cl-IB-MECA was assessed using three different concentrations (1.2 µM, 6 µM and 12 µM) in a model of chemical induced RGC apoptosis (intravitreal injection of 8% DMSO was used in Dark Agouti rats). (arvojournals.org)
  • Modulation of apoptosis by adenosine in the central nervous system: A possible role for the A3 receptor. (elsevier.com)
  • The A3 adenosine receptor as multifaceted therapeutic target: pharmacology, medicinal chemistry and in silico approaches. (units.it)
  • Conclusions and Implications: Investigation of the pharmacology of the W6.48F mutant of the adenosine A3 receptor confirms that this region is important in forming the active conformation of the receptor for stimulating a number of different signalling pathways and that mutations in this residue can lead to changes in agonist efficacy and signalling bias. (worktribe.com)
  • In mice in which extracellular adenosine production was impaired by CD73 KO, TAC caused greater hypertrophy and dysfunction and increased myocardial 3′-nitrotyrosine. (ahajournals.org)
  • Recently, we demonstrated that genetic deletion of CD73 (an ectonucleotidase that produces extracellular adenosine) exacerbated myocardial hypertrophy and heart failure resulting from left ventricular (LV) pressure overload produced by transverse aortic constriction (TAC), 1 suggesting that endogenous extracellular adenosine can protect against maladaptive hypertrophy. (ahajournals.org)
  • Over the past decade, remarkable progress has been made in the development of 'next-generation' therapeutics in immuno-oncology, with inhibitors of extracellular adenosine (eADO) signalling constituting an expanding class of agents. (nature.com)
  • Abundant evidence indicates that the conversion of pro-inflammatory extracellular ATP into immunosuppressive extracellular adenosine (eADO) favours tumour progression and escape from antitumour immunity. (nature.com)
  • Hypoxia-driven accumulation of extracellular adenosine results in the generation of an immunosuppressive niche that fuels tumor development. (springer.com)
  • T-cell proliferation in response to mitogenic anti-CD3 antibody was impaired in the presence of 10 microM adenosine (plus coformycin to inhibit endogenous adenosine deaminase). (nih.gov)
  • Deficiency of Adenosine deaminase 2 (DADA2) is a monogenic disease associated with systemic inflammation and vasculopathy that affects a wide variety of organs in different patients. (wikipedia.org)
  • Earlier function from our lab shows that mRNA degrees of a3 and a4 are up-regulated within the intrusive MDA-MB-231 breasts cancer cell range weighed against the non-invasive MCF7 range (24). (pyr-41.com)
  • Likewise, the intrusive MCF10CA1a breasts cancer cell range displays increased degrees of a3 mRNA in accordance with the parental MCF10a cell range, and knockdown of a3 reduced migration and invasion of MCF10CA1a cells (21). (pyr-41.com)
  • Our lab also demonstrated that a3 mRNA can be overexpressed in 43 of 43 human being breasts tumor samples in accordance with normal breasts cells by 2.5C50-fold which expression from the a3 protein is certainly highest in intrusive human being breast carcinoma in accordance with both non-invasive solid tumors and ALLO-2 regular breast tissue (25). (pyr-41.com)
  • Here, we demonstrate that adenosine, at concentrations that are typically present in the extracellular fluid of solid tumors, exerts a profound inhibitory effect on the induction of mouse cytotoxic T cells, without substantially affecting T-cell viability. (nih.gov)
  • The G i -coupled A 3 adenosine receptor (A 3 AR) mediates anti-inflammatory, anticancer and anti-ischemic protective effects. (uconn.edu)
  • There are currently no images for Adenosine A2a R Antibody (NBP1-39474FR). (novusbio.com)
  • Truncated N 6 -substituted-(N)-methanocarba-adenosine derivatives with 2-hexynyl substitution were synthesized to examine parallels with corresponding 4′-thioadenosines. (elsevier.com)
  • Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. (drugbank.ca)
  • Past studies have shown that a drug called adenosine may be effective for pain relief in humans, but the medication activates an array of circuits, or "pathways," causing a number of side effects. (medicalnewstoday.com)
  • however, alternative pathways involve the enzymatic activity of tissue-non-specific alkaline phosphatases and the NAD + ectohydrolase CD38 as well as cellular export of cytosolic adenosine. (nature.com)
  • These data were used to construct a computational model that describes how the physiological interaction between Engrailed, ephrin A5 and adenosine may enhance retino-tectal map precision. (biologists.org)
  • The figurative elements of blood are important substrates on which adenosine plays multiple physiological functions. (unife.it)
  • Finally, as for the physiological relevance of the A3 receptor-mediated stimulation of MMP-9 we found that the A3 agonist was responsible for an increase of the invasive ability of U87MG cells. (unife.it)
  • Here, we show that most of the cAMP response to adenosine is abolished in lymphoid tissues of A2a receptor-deficient mice, although some response remains in splenocytes. (nih.gov)
  • Sajjadi FG, Firestein GS: cDNA cloning and sequence analysis of the human A3 adenosine receptor. (drugbank.ca)
  • Salvatore CA, Jacobson MA, Taylor HE, Linden J, Johnson RG: Molecular cloning and characterization of the human A3 adenosine receptor. (drugbank.ca)
  • The study provides the first proof for the new concept that an increased expression of the human A3 receptor in the cardiac myocyte can be an important cardioprotective therapeutic approach. (garvan.org.au)
  • The Boehringer Ingelheim compound collection was screened for inhibitors of the ATPase activity of human papillomavirus E1 helicase to develop antiviral agents that inhibit human papillomavirus (HPV) DNA replication. (nih.gov)
  • Hoskin DW, Mader JS, Furlong SJ et al (2008) Inhibition of T cell and natural killer cell function by adenosine and its contribution to immune evasion by tumor cells (review). (springer.com)
  • The cardiovascular effects of induced hypotension by infusions of trinitroglycerin and adenosine triphosphate were also examined at the equivalent magnitude of hypotension. (elsevier.com)
  • Similar changes were also observed during adenosine triphosphate-induced hypotension. (elsevier.com)
  • Lately, a3-including V-ATPases had been localized towards the plasma membrane of a variety of intrusive breasts cancers cell lines using isoform-specific antibodies against a3 (25). (pyr-41.com)
  • Blay, J., White, T. D. & Hoskin, D. W. The extracellular fluid of solid carcinomas contains immunosuppressive concentrations of adenosine. (nature.com)
  • the purpose of this study was therefore to determine whether A 3 adenosine receptor stimulation with reperfusion modulates expression of the different mitogen-activated protein kinases. (springer.com)
  • The known diverse effects of adenosine on mitogenesis may be related to changes in mitogen-activated protein kinases. (aspetjournals.org)
  • The A 3 adenosine receptor (A 3 AR) contributes to several cardiovascular effects of adenosine, including antihypertensive and cardioprotective effects. (aspetjournals.org)
  • Mutation of W6.48F therefore resulted in differential effects on agonist efficacy, and introduced signalling pathway bias for HEMADO at the adenosine A3 receptor. (worktribe.com)
  • It has been unclear as to which specific pathway mediates the pain-relieving effects of adenosine, so Prof. Salvemini and her team wanted to find out. (medicalnewstoday.com)
  • It has long been appreciated that harnessing the potent pain-killing effects of adenosine could provide a breakthrough step towards an effective treatment for chronic pain. (medicalnewstoday.com)
  • Several physiologic effects of adenosine may be seen during infusion, including atrioventricular (AV) block, hypotension, sinus tachycardia (as a reflex mechanism), and sinus bradycardia. (springer.com)
  • Stimulation with the endogenous ligand adenosine resulted in the same pattern of ERK1/2 phosphorylation as NECA. (aspetjournals.org)
  • Antagonizes the activity of NECA, an adenosine receptor agonist. (hellobio.com)
  • We also noted that the A3 receptor stimulation led to increased levels of MMP9 protein in cellular extracts of U87MG cells, through phosphorylation of ERK1 / 2, JNK, Akt / PKB and the transcription factor AP-1. (unife.it)
  • Stimulation of both A3 and A2A causes reduction in the scotopic ERG b-wave. (hi.is)
  • with disrupted a4 exhibited decreased V-ATPase manifestation at the best edge, suggesting how the a4 ALLO-2 isoform can be primarily in charge of focusing on the V-ATPase towards the plasma membrane in 4T1-12B cells. (pyr-41.com)
  • Mammals communicate four different subunit a-isoforms, a1Ca4, where a3 and a4 are recognized to focus on the V-ATPase towards the plasma membrane of osteoclasts and renal intercalated cells, (7 respectively, 8, 11, 13). (pyr-41.com)
  • Significantly, overexpression of a3 in non-invasive MCF10a cells improved their invasiveness and localization from the V-ATPase towards the plasma membrane (21). (pyr-41.com)
  • Kumar V, Sharma A (2009) Adenosine: an endogenous modulator of innate immune system with therapeutic potential. (springer.com)
  • An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. (wikipedia.org)
  • Can-Fite is developing A3 agonist, CF101 for rheumatoid arthritis and psoriasis. (blogspot.co.uk)
  • Initially, we introduced on the bicyclic scaffold the same substituents those give affinity and selectivity at the A3 AR in the PTP nucleus. (units.it)