A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.
A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.
A subclass of ADENOSINE RECEPTORS that are generally considered to be coupled to the GS, STIMULATORY G-PROTEIN which causes up regulation of CYCLIC AMP.
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Purine bases found in body tissues and fluids and in some plants.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)
A glycoprotein enzyme present in various organs and in many cells. The enzyme catalyzes the hydrolysis of a 5'-ribonucleotide to a ribonucleoside and orthophosphate in the presence of water. It is cation-dependent and exists in a membrane-bound and soluble form. EC 3.1.3.5.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
A group of enzymes which catalyze the hydrolysis of ATP. The hydrolysis reaction is usually coupled with another function such as transporting Ca(2+) across a membrane. These enzymes may be dependent on Ca(2+), Mg(2+), anions, H+, or DNA.
An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.
Catalyze the hydrolysis of nucleosides with the elimination of ammonia.
A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)
3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)
A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
5'-Adenylic acid, monoanhydride with sulfuric acid. The initial compound formed by the action of ATP sulfurylase on sulfate ions after sulfate uptake. Synonyms: adenosine sulfatophosphate; APS.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)
Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES.
A purine base and a fundamental unit of ADENINE NUCLEOTIDES.
Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
The rate dynamics in chemical or physical systems.
A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.
Drugs used to cause dilation of the blood vessels.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Proteins involved in the transport of NUCLEOSIDES across cellular membranes.
A purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.
A class of enzymes that catalyze the conversion of a nucleotide and water to a nucleoside and orthophosphate. EC 3.1.3.-.
Purine bases related to hypoxanthine, an intermediate product of uric acid synthesis and a breakdown product of adenine catabolism.
Purine or pyrimidine bases attached to a ribose or deoxyribose. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.
The circulation of blood through the CORONARY VESSELS of the HEART.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Nucleosides in which the purine or pyrimidine base is combined with ribose. (Dorland, 28th ed)
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
An enzyme which catalyzes the catabolism of S-ADENOSYLHOMOCYSTEINE to ADENOSINE and HOMOCYSTEINE. It may play a role in regulating the concentration of intracellular adenosylhomocysteine.
A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
The monomeric units from which DNA or RNA polymers are constructed. They consist of a purine or pyrimidine base, a pentose sugar, and a phosphate group. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).
A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Elements of limited time intervals, contributing to particular results or situations.
Treatment process involving the injection of fluid into an organ or tissue.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.
Purines with a RIBOSE attached that can be phosphorylated to PURINE NUCLEOTIDES.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A group of compounds which consist of a nucleotide molecule to which an additional nucleoside is attached through the phosphate molecule(s). The nucleotide can contain any number of phosphates.
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
A process that changes the nucleotide sequence of mRNA from that of the DNA template encoding it. Some major classes of RNA editing are as follows: 1, the conversion of cytosine to uracil in mRNA; 2, the addition of variable number of guanines at pre-determined sites; and 3, the addition and deletion of uracils, templated by guide-RNAs (RNA, GUIDE).
A subtype of equilibrative nucleoside transporter proteins that is sensitive to inhibition by 4-nitrobenzylthioinosine.
Inhibitor of phosphodiesterases.
Esters formed between the aldehydic carbon of sugars and the terminal phosphate of adenosine diphosphate.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
A purine nucleoside that has guanine linked by its N9 nitrogen to the C1 carbon of ribose. It is a component of ribonucleic acid and its nucleotides play important roles in metabolism. (From Dorland, 28th ed)
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The hollow, muscular organ that maintains the circulation of the blood.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
A subtype of equilibrative nucleoside transporter proteins that is insensitive to inhibition by 4-nitrobenzylthioinosine.
The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.
A rather large group of enzymes comprising not only those transferring phosphate but also diphosphate, nucleotidyl residues, and others. These have also been subdivided according to the acceptor group. (From Enzyme Nomenclature, 1992) EC 2.7.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
Established cell cultures that have the potential to propagate indefinitely.
Relatively complete absence of oxygen in one or more tissues.
Enzymes that catalyze the hydrolysis of CYCLIC AMP to form adenosine 5'-phosphate. The enzymes are widely distributed in animal tissue and control the level of intracellular cyclic AMP. Many specific enzymes classified under this heading demonstrate additional spcificity for 3',5'-cyclic IMP and CYCLIC GMP.
Pyrazolopyrimidine ribonucleosides isolated from Nocardia interforma. They are antineoplastic antibiotics with cytostatic properties.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
An enzyme that catalyzes the reaction between a purine nucleoside and orthophosphate to form a free purine plus ribose-5-phosphate. EC 2.4.2.1.
The veins and arteries of the HEART.
An enzyme that catalyzes the deamination of AMP to IMP. EC 3.5.4.6.
Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
Exposure of myocardial tissue to brief, repeated periods of vascular occlusion in order to render the myocardium resistant to the deleterious effects of ISCHEMIA or REPERFUSION. The period of pre-exposure and the number of times the tissue is exposed to ischemia and reperfusion vary, the average being 3 to 5 minutes.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
A pentose active in biological systems usually in its D-form.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Coronary vasodilator with some antiarrhythmic activity.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.
Analogs of those substrates or compounds which bind naturally at the active sites of proteins, enzymes, antibodies, steroids, or physiological receptors. These analogs form a stable covalent bond at the binding site, thereby acting as inhibitors of the proteins or steroids.
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is an inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal side effect is nephrotoxicity. In vivo, dideoxyadenosine is rapidly metabolized to DIDANOSINE (ddI) by enzymatic deamination; ddI is then converted to dideoxyinosine monophosphate and ultimately to dideoxyadenosine triphosphate, the putative active metabolite.
N(6)-[delta(3)-isopentenyl]adenosine. Isopentenyl derivative of adenosine which is a member of the cytokinin family of plant growth regulators.
The decrease in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
... adenosine diphosphate MeSH D13.695.667.138.124.070 - adenosine diphosphate sugars MeSH D13.695.667.138.124.070.075 - adenosine ... n-ethylcarboxamide) MeSH D13.570.583.138.240 - s-adenosylhomocysteine MeSH D13.570.583.138.264 - s-adenosylmethionine MeSH ... adenosine diphosphate MeSH D13.695.827.068.124.070 - adenosine diphosphate sugars MeSH D13.695.827.068.124.070.075 - adenosine ... adenosine monophosphate MeSH D13.695.667.138.180.080 - adenosine phosphosulfate MeSH D13.695.667.138.236 - adenosine ...
N-ethylcarboxamide induces IL-6 expression via MAPKs and NF-kappaB activation through Akt, Ca(2+)/PKC, cAMP signaling pathways ... 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 ...
2001). "Adenosine A2B receptors behave as an alternative anchoring protein for cell surface adenosine deaminase in lymphocytes ... N-ethylcarboxamide induces IL-6 expression via MAPKs and NF-kappaB activation through Akt, Ca(2+)/PKC, cAMP signaling pathways ... Strohmeier GR, Reppert SM, Lencer WI, Madara JL (1995). "The A2b adenosine receptor mediates cAMP responses to adenosine ... alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting ...
N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase ... N-ethylcarboxamide) A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase ... ethylcarboxamide-adenosine (NECA), N6-phenylisopropyladenosine (PIA) and N6-cyclohexyladenosine (CHA) induced dose dependent ... N-ethylcarboxamide) (NECA). Subscribe to New Research on Adenosine-5-( ...
3H-chlorocyclopentyladenosine bound to adenosine A1 receptors. The A1 receptors were ubiquitously distributed in the brain with ... N-ethylcarboxamide) * N(6)-cyclohexyladenosine * 2-chloro-N(6)cyclopentyladenosine ... The adenosine A2a receptors were not detectable in whole brain membranes of goldfish either using the specific agonist 3H-CGS ... Biochemical and pharmacological evidence for the presence of A1 but not A2a adenosine receptors in the brain of the low ...
This study was designed to test the hypothesis that blockade of central nervous system (CNS) adenosine receptors may explain ... N-ethylcarboxamide) / administration & dosage * Adenosine-5-(N-ethylcarboxamide) / pharmacology* * Animals ... Central nervous system effects of caffeine and adenosine on fatigue Am J Physiol Regul Integr Comp Physiol. 2003 Feb;284(2): ... Initial experiments were done to confirm an effect of CNS caffeine and/or the adenosine A(1)/A(2) receptor agonist 5-N- ...
N-ethylcarboxamide; LAD, left anterior descending; DPSPX, 1,3-dipropyl-8-sulfophenylxanthine; CCPA, 2-chloro-N6- ... A1 adenosine receptor (AR) antagonists are effective diuretic agents that may be useful for treating fluid retention disorders ... ABBREVIATIONS: AR, adenosine receptor; CPX, 1,3-dipropyl-8-cyclopentylxanthine; BG 9719, 1,3-dipropyl-8-[2-(5,6-epoxynorbornyl ... Comparison of Three Different A1 Adenosine Receptor Antagonists on Infarct Size and Multiple Cycle Ischemic Preconditioning in ...
Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently ... N-ethylcarboxamide); 37739-05-2/2-chloro-N(6)cyclopentyladenosine; 58-61-7/Adenosine; 96865-92-8/8-(4-((2-aminoethyl) ... Adenosine / analogs & derivatives, pharmacology. Adenosine-5-(N-ethylcarboxamide) / pharmacology. Animals. Base Composition. ... Previous Document: Source of extracellular brain adenosine during hypoxia in fetal sheep.. Next Document: The bovine ...
Adenosine analog, 3::Adenosine, N6-Ethyl-carboxamido::Adenosine-5-(N-ethylcarboxamide)::CHEMBL464859::N- ... G-protein activation in human adenosine Adenosine A2A receptor expressing CHO cells using cAMP assay. J Med Chem 45: 420-9 ( ... Adenosine A1 receptor. (GUINEA PIG). BDBM21220. ((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,...). Show SMILES CCNC(=O)[C ... Adenosine receptor A1. (Homo sapiens (Human)). BDBM21220. ((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,...). Show SMILES ...
N-ethylcarboxamide-adenosine (NECA; 0.1 or 0.3 mg/kg body weight) was intraperitoneally administered to mice that had been ... N-Ethylcarboxamide-Adenosine Increases Mouse Serum Total Homocysteine Levels, Which Is a Risk Factor for Cardiovascular ... KEYWORDS: Adenosine, 5-N-Ethylcarboxamide-Adenosine, Glutathione, Homocysteine JOURNAL NAME: Pharmacology & Pharmacy, Vol.6 No ... When the non-specific adenosine receptor agonist 5- ...
N-ethylcarboxamide adenosine. ... Adenosine A1 and A2 receptors of the substantia gelatinosa are ... Antinociception produced by interactions between intrathecally administered adenosine agonists and norepinephrine.. Aran S, ... Identification of A1 and A2 adenosine receptors in the rat spinal cord. ... 5.. Neurotensin activation of the NTR1 on spinally-projecting serotonergic neurons in the rostral ventromedial medulla is ...
N-ethylcarboxamide induces IL-6 expression via MAPKs and NF-kappaB activation through Akt, Ca(2+)/PKC, cAMP signaling pathways ... 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 ...
... ethylcarboxamide adenosine. Brain Res 1990; 519:287-93 ... Antinociception by adenosine analogs and an adenosine kinase ... 19 Adenosine receptors are present on intrinsic interneurons in the dorsal horn. 2 It is conceivable that these adenosine ... Poon A, Sawynok J: Antinociception by adenosine analogs and inhibitors of adenosine metabolism in an inflammatory thermal ... in which adenosine is inactive. The mechanisms of norepinephrine release by activation of spinal adenosine A1 receptors after ...
... adenosine diphosphate MeSH D13.695.667.138.124.070 - adenosine diphosphate sugars MeSH D13.695.667.138.124.070.075 - adenosine ... n-ethylcarboxamide) MeSH D13.570.583.138.240 - s-adenosylhomocysteine MeSH D13.570.583.138.264 - s-adenosylmethionine MeSH ... adenosine diphosphate MeSH D13.695.827.068.124.070 - adenosine diphosphate sugars MeSH D13.695.827.068.124.070.075 - adenosine ... adenosine monophosphate MeSH D13.695.667.138.180.080 - adenosine phosphosulfate MeSH D13.695.667.138.236 - adenosine ...
... hydroxyl group of the ribose on the ATL compounds is protected from phosphorylation by the addition of N-ethylcarboxamide. ... Maximal CF response after bolus of ATL-146e was greater and more sustained than with adenosine. Note that adenosine flow ... No pharmacodynamic half-life data were reported for the adenosine boluses owing to the fact that the adenosine response was ... because comparisons were made between the adenosine A2A receptor agonists and adenosine in the same anesthetized animal model. ...
N-ethyl-carboxamide-adenos ine (CGS21680), a selective adenosine A2A receptor agonist, enhanced taurine release, while ... Purinergic P2 receptors trigger adenosine release leading to adenosine A2A receptor activation and facilitation of long-term ... Purinergic P2 receptors trigger adenosine release leading to adenosine A2A receptor activation and facilitation of long-term ... Effects of an adenosine A2A receptor blockade in the nucleus accumbens on locomotion, feeding, and prepulse inhibition in rats. ...
N-ethylcarboxamide adenosine (NECA) greater than (S)-PIA, indicative of their interaction with A1 adenosine receptors. Agonist ... adenosine indicates that the A1 adenosine receptor binding subunit is a Mr 38,000 protein. Adenosine receptor agonists [(R)-PIA ... N-ethylcarboxamido adenosine (125I-PAPA-APEC), we have demonstrated the presence of A2 adenosine receptors in this cell line. ... Demonstration of both A1 and A2 adenosine receptors in DDT1 MF-2 smooth muscle cells.. V Ramkumar, W W Barrington, K A Jacobson ...
Fingerprint Dive into the research topics of Intravitreous Injection of Adenosine or Its Agonists Causes Breakdown of the ... Intravitreous Injection of Adenosine or Its Agonists Causes Breakdown of the Blood-Retinal Barrier. ...
Fingerprint Dive into the research topics where G. Haskó is active. These topic labels come from the works of this person. Together they form a unique fingerprint. ...
N-ethylcarboxamide (NECA) in the presence of AR subtype-selective antagonists. The concentrations of each antagonist chosen for ... adenosine uptake. HU 210 at 1 μM did not inhibit [3H]adenosine uptake (Fig. 3) . These data suggest an adenosine uptake ... Adenosine uptake inhibitors decrease TNF-α in LPS-treated mice by increasing the amount of endogenous adenosine available to ... CBD has been shown to competitively inhibit adenosine uptake by ENT1, which is NBMPR sensitive. 16 We determined that adenosine ...
However, this physiologically constitutive activator was inhibited by adenosine deaminase and by inhibitors of the adenosine A2 ... RDC8 codes for an adenosine A2 receptor with physiological constitutive activity.. Maenhaut C1, Van Sande J, Libert F, ... Moreover, RDC8 mRNA and adenosine A2 receptors display a very similar distribution in the brain. RDC8 therefore codes for an A2 ... Cos 7 cells transfected with RDC8 cDNA constructs acquired binding characteristics of an adenosine A2 receptor. ...
N-ethylcarboxamide). *Cyclic AMP. *Phosphotransferases (Alcohol Group Acceptor). *Inositol 1,4,5-trisphosphate 3-kinase ... Adenosine A1 receptor signaling stimulates calcium responses in HBSMC. (A) Agonists (100 nM) selective for adenosine receptor ... selective agonists at adenosine A(2A) receptors and adenosine A(3) receptors, respectively. Calcium responses to NECA and CPA ... N-ethylcarboxamido-adenosine (100 nM) or N(6)-(3-iodobenzyl)-adenosine-5-N-methyluronamide (100 nM), ...
Activation and desensitization of rat A3-adenosine receptors by selective adenosine derivatives and xanthine-7-ribosides. Park ... Activation of brain adenosine receptors evokes vasodilation in skin arterioles. Proctor, K. G., Stojanov, I. & Bealer, S. L., ... Actions of adenosine on nitro blue tetrazolium deposition and surface pH during intestinal reperfusion injury. Kaminski, P. M ... Parrish, F. W., Smith, E. E. & Whelan, W. J., Mar 1970, In : Archives of Biochemistry and Biophysics. 137, 1, p. 185-189 5 p.. ...
Fingerprint Dive into the research topics where Peter J Oldenburg is active. These topic labels come from the works of this person. Together they form a unique fingerprint. ...
Fingerprint Dive into the research topics of The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic ... The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells. ...
N-ethylcarboxamide) Oxidants Adenosine Diphosphate Ribose Interleukin-12 Cell Death ...
Adenosine receptor regulation of coronary blood flow in ossabaw miniature swine. Long, X., Mokelke, E. A., Neeb, Z. P., Alloosh ... Adenosine is not responsible for local metabolic control of coronary blood flow in dogs during exercise. Tune, J. D., Richmond ... Adenosine deaminase that acts on RNA 3 (adar3) binding to glutamate receptor subunit B Pre-mRNA Inhibits RNA editing in ... Adenosine receptor antagonists and retinal neovascularization in vivo. Mino, R. P., Spoerri, P. E., Caballero, S., Player, D., ...
Adenosine-activated mast cells induce IgE synthesis by B lymphocytes: An A2B-mediated process involving Th2 cytokines IL-4 and ... Lyashenko, I. A. & Popov, V. L., 1 мая 2020, В : Technical Physics. 65, 5, стр. 728-736 9 стр.. Результат исследований: ... 388-392 5 стр.. Результат исследований: Материалы для книги/типы отчетов › Материалы для конференции ... 5, стр. 944-951 8 стр.. Результат исследований: Материалы для журнала › Статья ...
N-ethylcarboxamide); Biological Transport, Active; Bronchi; *Calcium Signaling; Cells, Cultured; Cyclic AMP; GTP-Binding ... selective agonists at adenosine A(2A) receptors and adenosine A(3) receptors, respectively. Calcium responses to NECA and CPA ... N-ethylcarboxamido-adenosine (100 nM) or N(6)-(3-iodobenzyl)-adenosine-5-N-methyluronamide (100 nM), ... Adenosine A1 receptors mediate mobilization of calcium in human bronchial smooth muscle cells.. Citation data: American journal ...
N-ethylcarboxamide), cannabinoid, receptor, receptor, signal transduction",. author = "Touma, {Anja M.} and Malik, {Rabia U.} ... keywords = "CB1, GTP-binding proteins, N(6)-cyclopentyladenosine, SCH 442 416, adenosine A1, adenosine-5{\textquoteright}-( ... Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G-peptides. / Touma, Anja M.; Malik, Rabia U.; ... Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G-peptides. In: Pharmacology Research and ...
N-ethylcarboxamide). Animals. Brain Stem -- drug effects. Brain Stem -- metabolism. ... The role of spinal and brainstem adenosine receptors in the modulation of the volume-evoked micturition reflex in the ... The role of spinal and brainstem adenosine receptors in the modulation of the volume-evoked micturition reflex in the ... Assessment of the role of A1/A2 adenosine receptors mediating the purine antinociception, motor and autonomic function in the ...
Adenosine stimulates neuromedin U mRNA expression in the rat pars tuberalis. Aizawa, S., Gu, T., Kaminoda, A., Fujioka, R., ... Adrenomedullin 2 and 5 activate the calcitonin receptor-like receptor (clr) - Receptor activity-modifying protein 3 (ramp3) ... 15-19 5 p.. Research output: Contribution to journal › Article › peer-review ...
... we investigated the effect of adenosine on myeloid cells and explored a possible contribution of myeloid cells to adenosine ... Little, however, is known about the effect of adenosine on myeloid cells. Considering that tumor associated macrophages (TAM) ... tissues show abundant expression of the ectonucleotidases CD39 and CD73 which generate immunomodulatory adenosine, thereby ... N-ethylcarboxamide (NECA, Tocris) was employed at 100 nM. To control for effects of adenosine on chemokinesis, a control ...
  • In whole brain membranes of goldfish, 3H-chlorocyclopentyladenosine bound to adenosine A1 receptors. (nih.gov)
  • The adenosine A2a receptors were not detectable in whole brain membranes of goldfish either using the specific agonist 3H-CGS 21680 or 3H-5'-N-ethylcarboxamidoadenosine. (nih.gov)
  • This study was designed to test the hypothesis that blockade of central nervous system (CNS) adenosine receptors may explain the beneficial effect of caffeine on fatigue. (nih.gov)
  • Results suggest that caffeine can delay fatigue through CNS mechanisms, at least in part by blocking adenosine receptors. (nih.gov)
  • Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. (biomedsearch.com)
  • Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently known. (biomedsearch.com)
  • For A2A adenosine receptors CGS 21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadeno sine) and N-ethylcarboxamidoadenosine (NECA) were found to be the most potent agonists followed by R- and S-PIA with minor stereoselectivity. (biomedsearch.com)
  • The CHO cells with stably transfected adenosine receptors provide an identical cellular background for such a pharmacological characterization. (biomedsearch.com)
  • 1 Both A 1 andA 2 subtypes of adenosine receptors are present in the substantia gelationosa. (asahq.org)
  • 7 A common problem with administration of direct agonists, such as adenosine itself, is adverse effects caused by stimulation of all receptors, not just those involved in the therapeutic effect. (asahq.org)
  • Demonstration of both A1 and A2 adenosine receptors in DDT1 MF-2 smooth muscle cells. (aspetjournals.org)
  • Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. (aspetjournals.org)
  • These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. (aspetjournals.org)
  • Using a recently developed A2 adenosine receptor agonist radioligand 2-[4-(2-[( 4-aminophenyl]methylcarbonyl)ethyl) phenyl]ethylamino-5'-N-ethylcarboxamido adenosine (125I-PAPA-APEC), we have demonstrated the presence of A2 adenosine receptors in this cell line. (aspetjournals.org)
  • Finally, adenosine receptor agonists stimulated adenylate cyclase activity by approximately 2-3 fold with the following potency series: PAPA-APEC greater than or equal to NECA greater than (R)-PIA, indicative of their interaction at A2 receptors. (aspetjournals.org)
  • Moreover, RDC8 mRNA and adenosine A2 receptors display a very similar distribution in the brain. (nih.gov)
  • Adenosine A1 receptors mediate mobilization of calcium in human bronchial smooth muscle cells. (plu.mx)
  • Adenosine A1 receptors mediate m. (plu.mx)
  • In contrast, there were no calcium responses to 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamido-adenosine (100 nM) or N(6)-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (100 nM), selective agonists at adenosine A(2A) receptors and adenosine A(3) receptors, respectively. (plu.mx)
  • Calcium responses were attenuated by xestospongin C and 2-aminoethoxydiphenylborane, inhibitors of inositol trisphosphate (IP(3)) receptors, and by U73122, an inhibitor of phospholipase C. It was concluded that stimulation of adenosine A(1) receptors on HBSMC rapidly mobilizes intracellular calcium stores by a mechanism dependent on PTX-sensitive G proteins, and IP(3) signaling. (plu.mx)
  • In this study, we examined the allosteric influence of native peptides derived from the C-terminus of the Gα subunit (G-peptides) on signaling from two Gi-coupled receptors, adenosine A1 receptor (A 1 R) and cannabinoid receptor 1 (CB 1 ). (elsevier.com)
  • DI-fusion The role of spinal and brainstem adenosine receptors in the. (ac.be)
  • The role of spinal and brainstem adenosine receptors in the modulation of the volume-evoked micturition reflex in the unanesthetized rat. (ac.be)
  • Assessment of the role of A1/A2 adenosine receptors mediating the purine antinociception, motor and autonomic function in the rat spinal cord. (ac.be)
  • Adenosine, a purine nucleoside, regulates a variety of physiological functions by stimulating specific extracellular receptors. (freedomwares.ca)
  • 12 Adenosine delivers potent suppressive effects on virtually all cells of the immune system by interacting with four subtypes of adenosine receptors (ARs), A1, A2A, A2B, and A3. (freedomwares.ca)
  • Growing evidence indicates that adenosine receptors could be promising therapeutic targets in autoimmune diseases. (researchwithrutgers.com)
  • Here we studied the role of adenosine receptors in controlling the course of type 1 diabetes. (researchwithrutgers.com)
  • NECA inhibited diabetes in A 2A receptor KO mice and the selective A 2A receptor agonist 2-p-(2-carboxyethyl)phenethyl-amino-5′-N-ethyl-carboxamidoadenosine (CGS21680) had no effect in normal mice, indicating a lack of role of A 2A receptors. (researchwithrutgers.com)
  • The vascular response to adenosine and its analogs is mediated by four adenosine receptors (ARs), namely, A 1 , A 2A , A 2B , and A 3 . (nebraska.edu)
  • We have recently demonstrated that adenosine controls the release of catecholamines (CA) from carotid body (CB) acting on AN receptors. (unl.pt)
  • Here, we have investigated the hypothesis that this control is exerted via an interaction between adenosine A(2B) and dopamine D-2 receptors present in chemoreceptor cells and if it is, the location of this interaction on the CB hypoxic transduction cascade. (unl.pt)
  • Role of cysteine residues of rat A2a adenosine receptors in agonist binding. (naver.com)
  • We found that cardiac fibroblasts produce cAMP in response to agonists for β-adrenergic (isoproterenol), prostaglandin EP2 (butaprost), adenosine (adenosine-5′-N-ethylcarboxamide, NECA), and prostacyclin (beraprost) receptors. (chapman.edu)
  • This site features trending Adenosine Receptors-linked items from the web for 5 of August 2019. (inpst.net)
  • Adenosine Receptors Adenosine is a purine nucleoside that serves as a link between energy metabolism and cell signaling. (inpst.net)
  • Adenosine is a physiologic regulator of all cell types that binds to G protein coupled receptors (GPCRs) that exist as four subtypes (A1, A2A, A2B, and A3). (inpst.net)
  • Naturally occurring xanthines are nonselective antagonists of adenosine receptors. (inpst.net)
  • Herein, we describe the expression and function of adenosine receptors (A1, A2A, A2B and A3) in neuroendocrine tumours. (cf.ac.uk)
  • Expression of adenosine receptors was investigated in archival human neuroendocrine tumour sections and in two human tumour cell lines, BON-1 (pancreatic) and KRJ-I (intestinal). (cf.ac.uk)
  • their activation leads to increased proliferation and secretion of chromogranin A. Targeting adenosine signal pathways, specifically inhibition of A2 receptors, may thus be a useful addition to the therapeutic management of neuroendocrine tumours. (cf.ac.uk)
  • These multiple physiologic functions controlled by adenosine receptors result in some undesirable side effects from direct adenosine receptor agonists, including headache, nausea, 5 motor weakness, 6,7 chest pain, and atrioventricular block, 8 which limit their clinical application. (asahq.org)
  • These actions occur via adenosine receptors which are widespread on the surface of cells in a living body [J. W. Daly, J. Med. (justia.com)
  • Therefore, diseases caused by physiological abnormality due to changes of interaction between adenosine and its receptors occur generally in the neurosecretion system, cardiovascular and gastro-intestinal tract system. (justia.com)
  • Use of an adenosine antagonist inhibiting the interaction between adenosine and its receptors is considered useful for the therapy and prophylaxis of these diseases [M. Williams et al. (justia.com)
  • Adenosine A2 receptors regulate the gene expression of striatopallidal and striatonigral neurons. (naver.com)
  • Initial experiments were done to confirm an effect of CNS caffeine and/or the adenosine A(1)/A(2) receptor agonist 5'-N-ethylcarboxamidoadenosine (NECA) on spontaneous locomotor activity. (nih.gov)
  • Adenosine receptor agonists [(R)-PIA, NECA, and (S)-PIA] inhibited isoproterenol-stimulated adenylate cyclase activity in DDT1 MF-2 cell membranes with IC50 values of 62, 538, and 750 nM, respectively. (aspetjournals.org)
  • The nonselective adenosine receptor agonist, 5'-N-ethylcarboxamidoadenosine (NECA), and the adenosine A(1) receptor agonist, N(6)-cyclopentyladenosine (CPA), both stimulated rapid, transient increases in [Ca(2+)](i). (plu.mx)
  • Calcium responses to NECA and CPA were inhibited by 8-cyclopentyl-1,3-dipropylxanthine, an adenosine A(1) receptor antagonist, and by pertussis toxin (PTX). (plu.mx)
  • We used agonists N 6 -Cyclopentyladenosine (CPA) and 5'-N-Ethylcarboxamidoadenosine (NECA) for A 1 R and 2-Arachidonoylglycerol (2-AG) and WIN 55,212-2 mesylate (WN) for CB 1 . (elsevier.com)
  • The nonselective adenosine receptor agonist 5′-N-ethylcarboxamidoadenosine (NECA) prevented diabetes development in both MLDS-challenged mice and in cyclophosphamide- treated NOD mice. (researchwithrutgers.com)
  • Previously, we indirectly showed that relaxation of porcine coronary artery by adenosine and its analogs are linked to modulation of phospholipase C and protein kinase C. In the present investigation, we assessed if the relaxant responses to the adenosine analogs CAD and NECA are associated with inhibition of inositol 1,4,5-trisphosphate (IP 3 ) formation. (elsevier.com)
  • Adenosine and NECA (0.1 μM) caused small contractions of 13.9 ± 3.0 and 16.4 ± 6.4%, respectively, and CCPA at 0.1 and 1.0 μM caused contractions of 30.8 ± 4.3 and 28.1 ± 3.9%, respectively, in A 1 AR (+/+) rings. (nebraska.edu)
  • Adenosine, NECA, and CGS-21680 produced an increase in maximal relaxation in A 1 AR (-/-) compared with A 1 AR (+/+) rings, whereas Cl-IBMECA did not produce contraction in either A 1 AR (+/+) or A 1 A 1 R (-/-) rings. (nebraska.edu)
  • Adenosine receptor agonist NECA increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation Conventional methods for therapeutic blood-brain barrier (BBB) disruption facilitate drug delivery but are cumbersome to perform. (inpst.net)
  • A previous study demonstrated that adenosine receptor (AR) stimulation by 5′-N-ethylcarboxamide adenosine (NECA) increased the extravasation of intravascular tracers into the brain and proposed that AR agonism may be an effective method for therapeutic BBB disruption. (inpst.net)
  • The non-selective adenosine receptor agonist (adenosine-5′N-ethylcarboxamide, NECA) and the A2AR agonist (CGS21680) stimulated cell proliferation by up to 20-40% which was attenuated by A2B (PSB603 and MRS1754) and A2A (SCH442416) receptor selective antagonists but not by the A1 receptor antagonist (PSB36). (cf.ac.uk)
  • Adenosine and NECA stimulated a twofold increase in chromogranin A secretion in BON-1 cells. (cf.ac.uk)
  • Effect of fluoxetine or adenosine receptor NECA agonist on G-proteins of C6 glioma cells or NK immunocytes. (nel.edu)
  • Kovárů H, Kovaru F, Ondráčkova P, Lisá V, Fiserová A. Effect of fluoxetine or adenosine receptor NECA agonist on G-proteins of C6 glioma cells or NK immunocytes. (nel.edu)
  • The relative potencies of agonists for the A2B adenosine receptor could only be tested by measurement of receptor-stimulated adenylyl cyclase activity. (biomedsearch.com)
  • The N6-benzyl substituted derivatives of adenosine-5'-N-methyluronamide (MECA) turned out to be the most potent agonists. (biomedsearch.com)
  • 5 The discovery of highly selective and relatively short-acting adenosine receptor A 2A agonists 6-9 has opened the possibility of a strategy for eliciting the desired coronary vasodilatation without producing side effects. (ahajournals.org)
  • Recently, a new class of selective adenosine A 2A receptor agonists has been synthesized at the University of Virginia. (ahajournals.org)
  • Microglial cells or rats were treated with or without lipopolysaccharide (LPS) in the presence or absence of adenosine, adenosine receptor agonists/antagonists, or CBD. (arvojournals.org)
  • Adenosine stimulates contraction of airway smooth muscle, but the mechanism is widely considered indirect, depending on release of contractile agonists from mast cells and nerves. (plu.mx)
  • A ) Agonists (100 nM) selective for adenosine receptor subtypes were added to HBSMC and calcium responses recorded. (nih.gov)
  • The effect of adenosine A(2B) and dopamine D-2 receptor agonists applied alone or conjunctly, was studied on the basal and evoked release (10% 02 and ionomycin) of CA from CB. (unl.pt)
  • In light of the clear therapeutic potential of selective adenosine receptor subtypeselective agonists or antagonists, new therapeutic candidates are being intensely pursued by the pharmaceutical industry. (inpst.net)
  • Among several novel approaches that seem promising in relief of neuropathic pain, adenosine receptor agonists have attracted considerable attention. (asahq.org)
  • Although adenosine agonists were shown to attenuate pain behaviors in a variety of animal models, adenosine agonists are also implicated in the regulation of many physiologic processes, especially cardiovascular and neurologic, which either reduce the activity of excitable tissues ( e.g. , by slowing heart rate) or increase the delivery of metabolic substrates ( e.g. , inducing vasodilation). (asahq.org)
  • A 1 adenosine receptor (AR) antagonists are effective diuretic agents that may be useful for treating fluid retention disorders including congestive heart failure. (aspetjournals.org)
  • 11,14,15 Thus, the effects of adenosine or T62 after nerve injury are totally abolished by destruction of noradrenergic terminals or administration of α 2 -adrenoceptor antagonists. (asahq.org)
  • and A is an optionally substituted divalent hydrocarbon chain having 2 to 4 carbon atoms and salts thereof are strong adenosine antagonists and activate cerebral functions and metabolisms, thus being useful as therapeutic or prophylactic agents for neurological or psychic changes caused by cerebral apoplexy, brain injury or cerebral atrophy. (justia.com)
  • Addition of guanosine 5'-[beta, alpha-imido]triphosphate (100 microM) shifted the (R)-PIA competition curves to the right to lower affinities. (aspetjournals.org)
  • Adenosine, FORMATION: Adenosine is a purine nucleoside that is formed within cells from the breakdown of adenosine monophosphate (AMP), which, in turn, is formed from adenosine triphosphate (ATP) and adenosine diphosphate (ADP) in the course of utilizing energy for cellular functions. (inpst.net)
  • In the cerebral tissue, it is considered that, under conditions of hypoxia or when cerebral blood circulation is blocked, adenosine triphosphate (ATP) of a high-energy compound is decreased to increase the adenosine concentration, and the adenosine acts on the adenosine receptor (A.sub.1) on nerve terminals to cause decrease of intracellular cyclic AMP concentration, opening of K.sup. (justia.com)
  • In superfused goldfish cerebellar slices, cyclohexyladenosine inhibited the cyclic AMP accumulation stimulated by forskolin and the selective adenosine A1 receptor antagonist, 8-cyclopentyltheophylline, reversed this effect. (nih.gov)
  • iTeos Therapeutics Initiates Phase 1/1b Trial with Differentiated Adenosine A2A Antagonist in Patients with Advanced Cancer Gosselies, Belgium and Cambridge, MA - April 17, 2019 - iTeos Therapeutics SA, a privately-held biotechnology company developing novel cancer immunotherapies, announced today the first cohort of patients has been dosed in its Phase 1/1b study with EOS100850, the Company's investigational A2A receptor antagonist and lead program candidate. (inpst.net)
  • Neither the change in [Ca 2+ ] i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2-aminoethyl)carbamoylmethoxy]-phenyl}-1,3-dipropylxanthine (XAC). (elsevier.com)
  • Theophylline having an adenosine antagonist activity, for example, has various pharmacological activities including stimulation of the central nervous system and heart muscle, diuretic action and relaxation of smooth muscle, especially bronchial smooth muscle, and has been widely used clinically. (justia.com)
  • ATL193 and ATL146e are 2-propynylcyclohexyl-5′- N -ethylcarboxamido derivatives of Ado. (ahajournals.org)
  • Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. (uchicago.edu)
  • The present invention provides novel tricyclic pyrimidine derivatives which are useful for the therapy and prophylaxis, by the action of ameliorating cerebral function based on a strong adenosine-antagonism, of mental disorders, neurological symptoms, etc. including symptoms of dementia, caused by cerebral apoplexy, brain injury or cerebral atrophy. (justia.com)
  • In this study we present for the first time the comparative pharmacology of all known human adenosine receptor subtypes. (biomedsearch.com)
  • More specifically, adenosine displays a variety of physiological actions in most of the organs and tissues, for example inhibition of cerebral function, vasodilation, cardiac depression, renal vasoconstriction, inhibition of platelet aggregation, modulation of insulin secretion, dysfunction of lymphocytes and modulation of renin release. (justia.com)
  • 3-5 The spinal administration of adenosine itself does not produce analgesia in normal rats to acute noxious stimulation. (asahq.org)
  • Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A 2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A 1 , A 2B , and A 3 . (ahajournals.org)
  • Fibroblasts are activated by factors such as transforming growth factor β and inhibited by agents that elevate 3′,5′-cyclic adenosine monophosphate (cAMP) levels. (chapman.edu)
  • In contrast to the adenosine A 2 receptor agonist 5′-N-ethylcarboxamidoadenosine, nucleotide analogues had no discernible effect on cytosolic adenosine 3′,5′-cyclic monophosphate levels or adenylyl cyclase activity. (elsevier.com)
  • In ovarian cancer, high levels of adenosine are due to tumor-specific expression of the ectonucleotidases CD39/ENTPD1 and CD73/ecto-5′-nucleotidase [ 7 ] which synergistically catalyze the degradation of extracellular immune-stimulatory ATP to immune-inhibitory adenosine. (springer.com)
  • BACKGROUND AND PURPOSE: The increased levels of extracellular adenosine in inflamed tissues down-regulate activated immune cells via the A(2A) adenosine receptor. (isharonline.org)
  • The aim of this study was to test whether the negative selection of T cells will produce T cells that are resistant to inhibition by extracellular adenosine. (isharonline.org)
  • The goal of this study is to determine the role of adenosine signaling in retinal inflammation and its potential modulation by CBD. (arvojournals.org)
  • Functional effects of adenosine were investigated in proliferation-experiments with CD4 + T cells and specific inhibitors. (springer.com)
  • These results suggest that the activated A 2A AR in the retinal microglial cells plays a major anti-inflammatory role in the retina and that CBD's anti-inflammatory effects are linked to the inhibition of adenosine uptake. (arvojournals.org)
  • To avoid these undesirable effects, indirect approaches, such as allosteric adenosine receptor modulation or inhibition of adenosine kinase 9,10 or adenosine deaminase, 11 have been examined and show antinociceptive effects in neuropathic rats. (asahq.org)
  • However, this physiologically constitutive activator was inhibited by adenosine deaminase and by inhibitors of the adenosine A2 receptor. (nih.gov)
  • T62 (2-amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophen) is an allosteric adenosine receptor modulator that enhances adenosine binding to the A1 receptor through a conformation change. (asahq.org)
  • Among these indirect approaches, allosteric adenosine receptor modulation represents a novel drug development direction to potentiate A1 receptor function and agonist binding via a conformation change. (asahq.org)
  • ADENOSINE is recognized to play a role in modulation of nociceptive transmission in the spinal cord. (asahq.org)
  • This integral membrane protein stimulates adenylate cyclase activity in the presence of adenosine. (wikipedia.org)
  • Adenosine A 1 receptor signaling stimulates calcium responses in HBSMC. (nih.gov)
  • CBD inhibited adenosine uptake via equilibrative nucleoside transporter 1 and synergistically enhanced adenosine's TNF-α suppression after treatment with LPS. (arvojournals.org)
  • CBD inhibited adenosine uptake via equilibrative nucleoside transporter 1 and synergistically enhanced adenosine's TNF-α suppression upon LPS treatment. (freedomwares.ca)
  • Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase r. (bindingdb.org)
  • Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 m. (bindingdb.org)
  • The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it. (wikipedia.org)
  • Adenosine generated by OvCA cells likely contributes to the recruitment of TAMs which further amplify adenosine-dependent immunosuppression via additional ectonucleotidase activity. (springer.com)
  • This A(2A) adenosine receptor-mediated immunosuppression is a disqualifying obstacle in cancer immunotherapy as it protects cancerous tissues from adoptively transferred anti-tumour T cells. (isharonline.org)
  • Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. (ahajournals.org)
  • These results suggest that adenosine receptor activation in porcine coronary artery inhibits agonist-induced production of IP 3 , and the magnitude of inhibition appears to depend on the type of adenosine analog used and on the presence and absence of endothelium. (elsevier.com)
  • A 2A ARs and/or A 2B ARs are involved in adenosine-mediated vascular relaxation of coronary and aortic beds. (nebraska.edu)
  • Adenosine uptake and tumor necrosis factor (TNF)-α release in cells or in retinas were determined. (arvojournals.org)
  • Adenosine" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uchicago.edu)
  • ASP5854 ameliorated A(2A) agonist 2-[p-(2-carboxyethyl) phenethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680)- and haloperidol-induced catalepsy in mice, with the minimum effective doses of 0.32 and 0.1 mg/kg, respectively, and it also improved haloperidol-induced catalepsy in rats at doses higher than 0.1 mg/kg. (curehunter.com)
  • Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients. (ahajournals.org)
  • Corticosteroids regulate brain hippocampal 5-HT1A receptor mRNA expression. (naver.com)
  • Photoaffinity labeling with the agonist photoprobe [125I]N6-[2-(4-amino-3-iodophenyl) ethyl]adenosine indicates that the A1 adenosine receptor binding subunit is a Mr 38,000 protein. (aspetjournals.org)
  • 11 Under adverse conditions such as inflammation, adenosine production by damaged neurons is increased and helps to protect tissue against excessive damage. (freedomwares.ca)
  • An obligatory interaction between adenosine or T62 and spinal noradrenergic function has been postulated in a rat model of neuropathic pain. (asahq.org)
  • We speculated that this adenosine-α 2 adrenoceptor interaction would also be present in the efficacy of T62 after surgery. (asahq.org)
  • The selective A 1 receptor agonist 2-chloro-N 6 -cyclopentyladenosine (CCPA) and A 3 receptor agonist N 6 -(3-iodobenzyl)- adenosine-5′-N-methyluronamide (IB-MECA) were less efficacious in ameliorating the course of diabetes. (researchwithrutgers.com)
  • The adenosine receptor (AR) subtypes expressed in rat retinal microglial cells were assessed by quantitative real-time RT-PCR. (arvojournals.org)
  • Considering that tumor associated macrophages (TAM) and myeloid-derived suppressor cells (MDSC) constitute up to 20 % of OvCA tissue, we investigated the effect of adenosine on myeloid cells and explored a possible contribution of myeloid cells to adenosine generation in vitro and ex vivo. (springer.com)
  • Generation of biologically active adenosine by TAM-like macrophages was measured in luciferase-based reporter assays. (springer.com)
  • In addition, adenosine A1 receptor regulation after chronic oral T62 administration was examined. (asahq.org)
  • It is concluded that conservation of BM proteins other than laminin-5 either by inhibiting degradation by MMPs or by preserving epidermal cell protein production is critical in therapeutic treatment of HD-induced microvesication in an ex vivo human skin model. (tudelft.nl)
  • RDC8 codes for an adenosine A2 receptor with physiological constitutive activity. (nih.gov)
  • On the other hand, adenosine, as one of the important constituents of a living body, plays an important role for appearance, maintenance and control of various physiological functions intra- and extracellularly. (justia.com)
  • Increased energy utilization or hypoxia enhances the cellular formation of AMP, which is dephosphorylated by a 50-nucleotidase in the ratelimiting step for adenosine production. (inpst.net)
  • Adenosine, released during cellular stress, damage and hypoxia, is a major regulator of angiogenesis. (cf.ac.uk)
  • 6 In contrast, adenosine does produce long-lasting analgesia in a model of neuropathic pain. (asahq.org)