Adenosine: 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.Receptor, Adenosine A2A: 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.Receptor, Adenosine A1: 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.Adenosine Deaminase: An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.Electrodiagnosis: Diagnosis of disease states by recording the spontaneous electrical activity of tissues or organs or by the response to stimulation of electrically excitable tissue.Receptor, Adenosine A2B: 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.Adenosine Kinase: 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.Receptors, Adenosine A2: 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.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Receptors, Purinergic P1: 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).Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Xanthines: Purine bases found in body tissues and fluids and in some plants.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Theophylline: 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.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Receptors, Purinergic: 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.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.2-Chloroadenosine: 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.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.Inosine: 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)5'-Nucleotidase: 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.Cyclic AMP: 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.Adenosine Triphosphatases: 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.Tubercidin: 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.Adenine NucleotidesNucleoside Deaminases: Catalyze the hydrolysis of nucleosides with the elimination of ammonia.Coformycin: A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.Dipyridamole: 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)Theobromine: 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)Pentostatin: 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.Adenosine Phosphosulfate: 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.Purines: 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.Thioinosine: 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)Triazines: 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.Adenine: A purine base and a fundamental unit of ADENINE NUCLEOTIDES.Deoxyadenosines: Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Kinetics: The rate dynamics in chemical or physical systems.Aminophylline: 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.Vasodilator Agents: Drugs used to cause dilation of the blood vessels.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Nucleoside Transport Proteins: Proteins involved in the transport of NUCLEOSIDES across cellular membranes.Hypoxanthine: A purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.Nucleotidases: A class of enzymes that catalyze the conversion of a nucleotide and water to a nucleoside and orthophosphate. EC 3.1.3.-.Hypoxanthines: Purine bases related to hypoxanthine, an intermediate product of uric acid synthesis and a breakdown product of adenine catabolism.TriazolesNucleosides: Purine or pyrimidine bases attached to a ribose or deoxyribose. (From King & Stansfield, A Dictionary of Genetics, 4th ed)Apyrase: 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.Coronary Circulation: The circulation of blood through the CORONARY VESSELS of the HEART.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Bucladesine: 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, Cultured: 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.Guinea Pigs: 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.Examination QuestionsRats, Sprague-Dawley: 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.Adenosylhomocysteinase: 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.Receptors, Purinergic P2: 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.Calcium: 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.Myocardium: 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.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Nucleotides: 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)Dogs: 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)8-Bromo Cyclic Adenosine Monophosphate: 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.Colforsin: 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.Magnesium: 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.Caffeine: 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.Extracellular Space: 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.Hyperemia: 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).1-Methyl-3-isobutylxanthine: 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 KINASESVasodilation: The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.Early Ambulation: Procedure to accelerate the ability of a patient to walk or move about by reducing the time to AMBULATION. It is characterized by a shorter period of hospitalization or recumbency than is normally practiced.NorbornanesTime Factors: Elements of limited time intervals, contributing to particular results or situations.Perfusion: Treatment process involving the injection of fluid into an organ or tissue.Isoproterenol: 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.S-Adenosylhomocysteine: 5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.Purine Nucleosides: Purines with a RIBOSE attached that can be phosphorylated to PURINE NUCLEOTIDES.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Dinucleoside Phosphates: 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.Phosphodiesterase Inhibitors: Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.RNA Editing: 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).Equilibrative Nucleoside Transporter 1: A subtype of equilibrative nucleoside transporter proteins that is sensitive to inhibition by 4-nitrobenzylthioinosine.4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone: Inhibitor of phosphodiesterases.Adenosine Diphosphate Sugars: Esters formed between the aldehydic carbon of sugars and the terminal phosphate of adenosine diphosphate.Thionucleotides: Nucleotides in which the base moiety is substituted with one or more sulfur atoms.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Guanosine: 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)Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Rats, Inbred Strains: 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.Heart: The hollow, muscular organ that maintains the circulation of the blood.Functional Laterality: Behavioral manifestations of cerebral dominance in which there is preferential use and superior functioning of either the left or the right side, as in the preferred use of the right hand or right foot.Equilibrative-Nucleoside Transporter 2: A subtype of equilibrative nucleoside transporter proteins that is insensitive to inhibition by 4-nitrobenzylthioinosine.Platelet Aggregation: 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.Phosphotransferases: 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.Enzyme Activation: 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.Glyburide: An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Suramin: 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.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Anoxia: Relatively complete absence of oxygen in one or more tissues.3',5'-Cyclic-AMP Phosphodiesterases: 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.Formycins: Pyrazolopyrimidine ribonucleosides isolated from Nocardia interforma. They are antineoplastic antibiotics with cytostatic properties.Cyclic AMP-Dependent Protein Kinases: 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.Glucose Solution, Hypertonic: Solution that is usually 10 percent glucose but may be higher. An isotonic solution of glucose is 5 percent.Purine-Nucleoside Phosphorylase: 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.Coronary Vessels: The veins and arteries of the HEART.AMP Deaminase: An enzyme that catalyzes the deamination of AMP to IMP. EC 3.5.4.6.Dental Staff: Personnel who provide dental service to patients in an organized facility, institution or agency.Cattle: 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.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Ischemic Preconditioning, Myocardial: 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.Potassium: 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.Ribose: A pentose active in biological systems usually in its D-form.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Dilazep: Coronary vasodilator with some antiarrhythmic activity.Hydrogen-Ion Concentration: 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 Triphosphate: Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.Affinity Labels: 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.Mice, Inbred C57BLDideoxyadenosine: 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.Isopentenyladenosine: N(6)-[delta(3)-isopentenyl]adenosine. Isopentenyl derivative of adenosine which is a member of the cytokinin family of plant growth regulators.Depression, Chemical: 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.

Control of glutamatergic neurotransmission in the rat spinal dorsal horn by the nucleoside transporter ENT1. (1/439)

Adenosine modulates nociceptive processing in the superficial dorsal horn of the spinal cord. In other tissues, membrane transporters influence profoundly the extracellular levels of adenosine. To investigate the putative role of nucleoside transporters in the regulation of excitatory synaptic transmission in the dorsal horn, we employed immunohistochemistry and whole-cell patch-clamp recording of substantia gelatinosa neurons in slices of rat spinal cord in vitro. The rat equilibrative nucleoside transporter (rENT1) was revealed by antibody staining to be abundant in neonatal and mature dorsal horn, especially within laminae I-III. This was confirmed by immunoblots of dorsal horn homogenate. Nitrobenzylthioinosine (NBMPR), a potent non-transportable inhibitor of rENT1, attenuated synaptically evoked EPSCs onto lamina II neurons in a concentration-dependent manner. Application of an adenosine A1 antagonist 1,3-dipropyl-8-cyclopentylxanthine produced a parallel rightward shift in the NBMPR concentration-effect curve. The effects of NBMPR were partially reversed by adenosine deaminase, which facilitates the metabolic degradation of adenosine. The modulation by NBMPR of evoked EPSCs was mimicked by exogenous adenosine or the selective A1 receptor agonist, 2-chloro-N6-cyclopentyl adenosine. NBMPR reduced the frequency but not the amplitude of spontaneous miniature EPSCs and increased the paired-pulse ratio of evoked currents, an effect that is consistent with presynaptic modulation. These data provide the first direct evidence that nucleoside transporters are able to critically modulate glutamatergic synaptic transmission.  (+info)

Ischaemic tolerance in aged mouse myocardium: the role of adenosine and effects of A1 adenosine receptor overexpression. (2/439)

The genesis of the ischaemia intolerant phenotype in aged myocardium is poorly understood. We tested the hypothesis that impaired adenosine-mediated protection contributes to ischaemic intolerance, and examined whether this is countered by A1 adenosine receptor (A1AR) overexpression. Responses to 20 min ischaemia and 45 min reperfusion were assessed in perfused hearts from young (2-4 months) and moderately aged (16-18 months) mice. Post-ischaemic contractility was impaired by ageing with elevated ventricular diastolic (32 +/- 2 vs. 18 +/- 2 mmHg in young) and reduced developed (37 +/- 3 vs. 83 +/- 6 mmHg in young) pressures. Lactate dehydrogenase (LDH) loss was exaggerated (27 +/- 2 vs. 16 +/- 2 IU g-1 in young) whereas the incidence of tachyarrhythmias was similar in young (15 +/- 1 %) and aged hearts (16 +/- 1 %). Functional analysis confirmed equipotent effects of 50 micro M adenosine at A1 and A2 receptors in young and aged hearts. Nonetheless, while 50 micro M adenosine improved diastolic (5 +/- 1 mmHg) and developed pressures (134 +/- 7 mmHg) and LDH loss (6 +/- 2 IU g-1) in young hearts, it did not alter these variables in the aged group. Adenosine did attenuate arrhythmogenesis for both ages (to ~10 %). In contrast to adenosine, 50 micro M diazoxide reduced ischaemic damage and arrhythmogenesis for both ages. Contractile and anti-necrotic effects of adenosine were limited by 100 micro M 5-hydroxydecanoate (5-HD) and 3 micro M chelerythrine. Anti-arrhythmic effects were limited by 5-HD but not chelerythrine. Non-selective (100 micro M 8-sulfophenyltheophylline) and A1-selective (150 nM 8-cyclopentyl-1,3-dipropylxanthine) adenosine receptor antagonism impaired ischaemic tolerance in young but not aged hearts. Quantitative real-time PCR and radioligand analysis indicated that impaired protection is unrelated to changes in A1AR mRNA transcription, or receptor density (~8 fmol mg-1 protein in both age groups). However, A1AR overexpression improved tolerance for both ages, restoring adenosine-mediated protection. These data reveal impaired protection via exogenous and endogenous adenosine contributes to ischaemic intolerance with ageing. This is independent of A1AR expression, and involves ineffective activation of a 5-HD-/diazoxide-sensitive process. The effects of A1AR overexpression indicate that the age-related failure in signalling can be overcome.  (+info)

Hypersensitivity of pulmonary C fibers induced by adenosine in anesthetized rats. (3/439)

Compelling clinical evidence implicates the potential role of adenosine in development of airway hyperresponsiveness and suggests involvement of pulmonary sensory receptors. This study was carried out to determine the effect of a low dose of adenosine infusion on sensitivity of pulmonary C-fiber afferents in anesthetized open-chest rats. Infusion of adenosine (40 microg x kg-1x min-1 i.v. for 90 s) mildly elevated baseline activity of pulmonary C fibers. However, during adenosine infusion, pulmonary C-fiber responses to chemical stimulants and lung inflation (30 cmH2O tracheal pressure) were markedly potentiated; e.g., the response to right atrial injection of capsaicin (0.25 or 0.5 microg/kg) was increased by more than fivefold (change in fiber activity = 2.64 +/- 0.67 and 16.27 +/- 3.11 impulses/s at control and during adenosine infusion, n = 13, P < 0.05), and this enhanced response returned to control in approximately 10 min. The potentiating effect of adenosine infusion was completely blocked by pretreatment with 8-cyclopentyl-1,3-dipropylxanthine (100 microg/kg), a selective antagonist of the adenosine A1 receptor, but was not affected by 3,7-dimethyl-1-propargylxanthine (1 mg/kg), an A2-receptor antagonist, or 3-ethyl-5-benzyl-2-methyl-4-phenylethynyl-6-phenyl-1,4-(+/-)-dihydropyridine-3,5- dicarboxylate (2 mg/kg), an A3-receptor antagonist. This potentiating effect was also mimicked by N6-cyclopentyladenosine (0.25 microg x kg-1 x min-1 for 90 s), a selective agonist of the adenosine A1 receptor. In conclusion, our results showed that infusion of adenosine significantly elevated the sensitivity of pulmonary C-fiber afferents in rat lungs and that this potentiating effect is likely mediated through activation of the adenosine A1 receptor.  (+info)

A role of protein kinase C mu in signalling from the human adenosine A1 receptor to the nucleus. (4/439)

1 Stimulation of adenosine A(1) receptors produced a stimulation of c-fos promoter-regulated gene transcription in Chinese hamster ovary (CHO)-A1 cells expressing the human A(1) receptor. Gene transcription was monitored using a luciferase-based reporter gene (pGL3). 2 This response to the A(1) receptor agonist N(6)-cyclopentyladenosine (CPA) was sensitive to inhibition by pertussis toxin, the MEK-1 inhibitor PD 98059 and by the phosphatidylinositol-3-kinase inhibitors wortmannin and LY 294002. The response was also completely abolished by the protein kinase C (PKC) inhibitor Ro-31-8220. 3 Several isoforms of PKC can be detected in CHO-A1 cells (alpha, delta, epsilon, micro, iota, zeta), but only PKC alpha, PKC delta and PKC were downregulated by prolonged treatment with phorbol ester. The c-fos-regulated luciferase response to A(1) agonists was not, however, inhibited by 24 h pretreatment with the phorbol esters phorbol 12,13-dibutyrate (PDBu). This observation, together with the fact that a significant attenuation (40%) of the c-fos-luciferase response to PDBu and A(1) agonist was produced by low concentrations of the PKC inhibitor Go 6976 suggests a role for PKC micro. 4 Stimulation of CHO-A1 cells with CPA stimulated the activation of endogenous PKC micro as measured by autophosphorylation. This was rapid, occurred within 1-2 min, but returned to basal levels after 30 min. Furthermore, transient expression of a constitutively active form of PKC micro resulted in a significant increase in c-fos-regulated gene expression. 5 Taken together, these data suggest that PKC micro plays an important role in the ability of the adenosine A(1) receptor to signal to the nucleus.  (+info)

Diadenosine-5-phosphate exerts A1-receptor-mediated proarrhythmic effects in rabbit atrial myocardium. (5/439)

(1) Diadenosine polyphosphates have been described to be present in the myocardium and exert purinergic- and nonreceptor-mediated effects. Since the electrophysiological properties of atrial myocardium are effectively regulated by A(1) receptors, we investigated the effect of diadenosine pentaphosphate (Ap(5)A) in rabbit myocardium. (2) Parameters of supraventricular electrophysiology and atrial vulnerability were measured in Langendorff-perfused rabbit hearts. Muscarinic potassium current (I(K(ACh/Ado))) and ATP-sensitive potassium current (I(K(ATP))) were measured by using the whole-cell voltage clamp method. (3) Ap(5)A prolonged the cycle length of spontaneously beating Langendorff perfused hearts from 225+/-14 (control) to 1823+/-400 ms (Ap(5)A 50 micro M; n=6; P<0.05). This effect was paralleled by higher degree of atrio-ventricular block. Atrial effective refractory period (AERP) in control hearts was 84+/-14 ms (n=6). Ap(5)A>/=1 micro M reduced AERP (100 micro M, 58+/-11 ms; n=6). (4) Extrastimuli delivered to hearts perfused with Ap(5)A- or adenosine (>/= micro M)-induced atrial fibrillation, the incidence of which correlated to the concentration added to the perfusate. The selective A(1)-receptor antagonist CPX (20 micro M) inhibited the Ap(5)A- and adenosine-induced decrease of AERP. Atrial fibrillation was no longer observed in the presence of CPX. (5) The described Ap(5)A-induced effects in the multicellular preparation were enhanced by dipyridamole (10 micro M), which is a cellular adenosine uptake inhibitor. Dipyridamole-induced enhancement was inhibited by CPX. (6) Ap(5)A (+info)

Comparison of effects of MgCl2 and Gpp(NH)p on antagonist and agonist radioligand binding to adenosine A1 receptors. (6/439)

AIM: To investigate modulation of antagonist and agonist binding to adenosine A1 receptors by MgCl2 and 5 -guanylimidodiphosphate (Gpp(NH)p) using rat brain membranes and the A1 antagonist [3H]-8-cyclopentyl-1,3-dipropylxanthine ([3H]DPCPX) and the A1 agonist [3H]-2-chloro-N6-cyclopentyladenosine ([3H]CCPA). METHODS: Parallel saturation and inhibition studies were performed using well-characterised radioligand binding assays and a Brandel Cell Harvester. RESULTS: MgCl2 produced a concentration-dependent decrease (44%), whereas Gpp(NH)p increased [3H]DPCPX binding (19%). In [3H]DPCPX competition studies, agonist affinity was 1.5-14.6-fold higher and 4.6-10-fold lower in the presence of 10 mmol/L MgCl2 and 10 micromol/L Gpp(NH)p respectively; antagonist affinity was unaffected. The decrease in agonist affinity with increasing Gpp(NH)p concentrations was due to a reduction in the proportion of binding to the high affinity receptor state. In contrast to [3H]DPCPX, MgCl2 produced a concentration-dependent increase (72%) and Gpp(NH)p a decrease (85%) in [3H]CCPA binding. Using [3H]CCPA, agonist affinities were 5-17-fold higher than those for [3H]DPCPX, consistent with binding only to the high affinity receptor state. Agonist affinity was 1.3-10.5-fold higher and 2.4-4.7-fold lower on adding MgCl2 or Gpp(NH)p respectively; antagonist affinities were as for [3H]DPCPX. CONCLUSION: The inconsistencies surrounding the effects of MgCl2 and guanine nucleotides on radioligand binding to adenosine A1 receptors were systematically examined. The effects of MgCl2 and Gpp(NH)p on agonist binding to A1 receptors are consistent with their roles in stimulating GTP-hydrolysis at the G-protein alpha-subunit and in blocking formation of the high affinity agonist-receptor-G protein complex.  (+info)

Adenosine A(1) receptor-mediated presynaptic inhibition at the calyx of Held of immature rats. (7/439)

At the calyx of Held synapse in brainstem slices of 5- to 7-day-old (P5-7) rats, adenosine, or the type 1 adenosine (A1) receptor agonist N6-cyclopentyladenosine (CPA), inhibited excitatory postsynaptic currents (EPSCs) without affecting the amplitude of miniature EPSCs. The A1 receptor antagonist 8-cyclopentyltheophylline (CPT) had no effect on the amplitude of EPSCs evoked at a low frequency, but significantly reduced the magnitude of synaptic depression caused by repetitive stimulation at 10 Hz, suggesting that endogenous adenosine is involved in the regulation of transmitter release. Adenosine inhibited presynaptic Ca(2+) currents (IpCa) recorded directly from calyceal terminals, but had no effect on presynaptic K+ currents. When EPSCs were evoked by IpCa during simultaneous pre- and postsynaptic recordings, the magnitude of the adenosine-induced inhibition of IpCa fully explained that of EPSCs, suggesting that the presynaptic Ca(2+) channel is the main target of A1 receptors. Whereas the N-type Ca(2+) channel blocker omega-conotoxin attenuated EPSCs, it had no effect on the magnitude of adenosine-induced inhibition of EPSCs. During postnatal development, in parallel with a decrease in the A1 receptor immunoreactivity at the calyceal terminal, the inhibitory effect of adenosine became weaker. We conclude that presynaptic A1 receptors at the immature calyx of Held synapse play a regulatory role in transmitter release during high frequency transmission, by inhibiting multiple types of presynaptic Ca(2+) channels.  (+info)

Brief, repeated, oxygen-glucose deprivation episodes protect neurotransmission from a longer ischemic episode in the in vitro hippocampus: role of adenosine receptors. (8/439)

1. Ischemic preconditioning in the brain consists of reducing the sensitivity of neuronal tissue to further, more severe, ischemic insults. We recorded field epsps (fepsps) extracellularly from hippocampal slices to develop a model of in vitro ischemic preconditioning and to evaluate the role of A1, A2A and A3 adenosine receptors in this phenomenon. 2. The application of an ischemic insult, obtained by glucose and oxygen deprivation for 7 min, produced an irreversible depression of synaptic transmission. Ischemic preconditioning was induced by four ischemic insults (2 min each) separated by 13 min of normoxic conditions. After 30 min, an ischemic insult of 7 min was applied. This protocol substantially protected the tissue from the irreversible depression of synaptic activity. 3. The selective adenosine A1 receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX, 100 nm), completely prevented the protective effect of preconditioning. The selective adenosine A2A receptor antagonist 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phe nol (ZM 241385, 100 nm) did not modify the magnitude of fepsp recovery compared to control slices. The selective A3 adenosine receptor antagonists, 3-propyl-6-ethyl-5[ethyl(thio)carbonyl]-2-phenyl-4-propyl-3-pyridinecarboxylate (MRS 1523, 100 nm) significantly improved the recovery of fepsps after 7 min of ischemia. 4. Our results show that in vitro ischemic preconditioning allows CA1 hippocampal neurons to become resistant to prolonged exposure to ischemia. Adenosine, by stimulating A1 receptors, plays a crucial role in eliciting the cell mechanisms underlying preconditioning; A2A receptors are not involved in this phenomenon, whereas A3 receptor activation is harmful to ischemic preconditioning.  (+info)

*Adenosine receptor

The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. This receptor has an inhibitory function ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as endogenous ... Adenosine receptors play a key role in the homeostasis of bone. The A1 receptor has been shown to stimulate osteoclast ... Br J Pharmacol 170(6):1167-1176 "Entrez Gene: ADORA2A adenosine A2A receptor". Jacobson KA, Gao ZG (2006). "Adenosine receptors ...

*Adenosine A2A receptor

"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This ...

*Adenosine A3 receptor

1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... adenosine receptor". Mol. Pharmacol. 63 (5): 1021-31. doi:10.1124/mol.63.5.1021. PMID 12695530. "Adenosine Receptors: A3". ...

*Adenosine A1 receptor

The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. Activation of the adenosine A1 receptor ... "Adenosine Receptors: A1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Adenosine A1 Receptor at the US National Library of Medicine Medical Subject Headings (MeSH) Human ADORA1 genome location and ...

*N6-Cyclopentyladenosine

... modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive ... "N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists". Bioorganic & ... N6-Cyclopentyladenosine (CPA) is a drug which acts as a selective adenosine A1 receptor agonist. It has mainly cardiovascular ... Elzein E, Zablocki J (December 2008). "A1 adenosine receptor agonists and their potential therapeutic applications". Expert ...

*Adams-Oliver syndrome

"Hypoxia induces cardiac malformations via A1 adenosine receptor activation in chicken embryos". Birth Defects Research. Part A ... "Haploinsufficiency of the NOTCH1 Receptor as a Cause of Adams-Oliver Syndrome With Variable Cardiac Anomalies". Circulation: ...

*Adenosine reuptake inhibitor

Bauman LA, Mahle CD, Boissard CG, Gribkoff VK (1992). "Age-dependence of effects of A1 adenosine receptor antagonism in rat ... Chaudary N, Naydenova Z, Shuralyova I, Coe IR (2004). "The adenosine transporter, mENT1, is a target for adenosine receptor ... "Adenosine and adenosine uptake inhibitors potentiate the neuromuscular blocking action of rocuronium mediated by adenosine A(1 ... York MJ, Davies LP (1982). "The effect of diazepam on adenosine uptake and adenosine-stimulated adenylate cyclase in guinea-pig ...

*Pharmacodynamics

Dhalla AK, Shryock JC, Shreeniwas R, Belardinelli L (2003). "Pharmacology and therapeutic applications of A1 adenosine receptor ... adenosine receptor antagonist, on the negative inotropic action of A(1) adenosine receptor full agonists in isolated guinea pig ... Hormone receptors Neuromodulator receptors Neurotransmitter receptors General anesthetics were once thought to work by ... More precisely, receptor reserve refers to a phenomenon whereby stimulation of only a fraction of the whole receptor population ...

*Acupuncture

The anti-nociceptive effect of acupuncture may be mediated by the adenosine A1 receptor. A 2014 review in Nature Reviews Cancer ... which then triggered nearby A1 receptors "caused more tissue damage and inflammation relative to the size of the animal in mice ... Mechanical deformation of the skin by acupuncture needles appears to result in the release of adenosine. ... such studies unnecessarily muddled a finding that local inflammation can result in the local release of adenosine with ...

*Dipropylcyclopentylxanthine

... is a drug which acts as a potent and selective antagonist for the adenosine A1 receptor. It has high selectivity for A1 over ... "Potent adenosine receptor antagonists that are selective for the A1 receptor subtype". Molecular Pharmacology. 31 (3): 247-52. ... It has been used to study the function of the adenosine A1 receptor in animals, which has been found to be involved in several ... De Sarro G, Donato Di Paola E, Falconi U, Ferreri G, De Sarro A (December 1996). "Repeated treatment with adenosine A1 receptor ...

*Bamifylline

... is a drug of the xanthine chemical class which acts as a selective adenosine A1 receptor antagonist. Theophylline ... "Effects of A1 adenosine receptor blockade by bamiphylline on ischaemic preconditioning during coronary angioplasty" (PDF). ...

*CCPA (biochemistry)

2-Chloro-N6-cyclopentyladenosine (CCPA) is a specific receptor agonist for the Adenosine A1 receptor. It is similar to N6- ... a high affinity agonist radioligand for A1 adenosine receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 340: 679-683. ...

*Rolofylline

Givertz MM, Massie BM, Fields TK, Pearson LL, Dittrich HC (October 2007). "The effects of KW-3902, an adenosine A1-receptor ... Rolofylline (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor antagonist. It was discovered ... dose-finding study of the adenosine A1 receptor antagonist rolofylline in patients with acute heart failure and renal ...

*Adenosine monophosphate deaminase deficiency type 1

... excess free adenosine down-regulates primary A1 adenosine receptors, leading to increased muscle pain. Secondary receptors (A3 ... Adenosine mediates pain through adenosine receptors. MADD causes an increase of free adenosine during heavy activity which may ... In the brain, excess adenosine decreases alertness and causes sleepiness. In this way, adenosine may play a role in fatigue ... Fatigue and sedation after heavy exertion can be caused by excess adenosine in the cells which signals muscle fiber to feel ...

*Basal ganglia

... muscarinic acetylcholine receptor M4, and adenosine receptor A1. The direct pathway has been proposed to facilitate motor ... This pathway consists of MSNs that express dopamine receptor D2, muscarinic acetylcholine receptor M1, and adenosine receptor ... "Adenosine-cannabinoid receptor interactions. Implications for striatal function". British Journal of Pharmacology. 160 (3): 443 ... This model of direct D1, and indirect D2 pathways explain why selective agonists of each receptor are not rewarding, as ...

*ATL-444

... is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A. It has ... "Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats". ... been used to study the role of the adenosine receptor system in the reinforcing action of cocaine. CGS-15943 Doyle, S. E.; ...

*Phosphodiesterase 2

"Adenosine deaminase inhibition enhances the inotropic response mediated by A1 adenosine receptor in hyperthyroid guinea pig ... Theoretically, this problem can be resolved if the effect of adenosine accumulated by EHNA, a result of adenosine deaminase ... EHNA is also a very potent adenosine deaminase inhibitor with an IC50 ~2 nM. This dual inhibition would lead to the ... Suvarna NU, O'Donnell JM (July 2002). "Hydrolysis of N-methyl-D-aspartate receptor-stimulated cAMP and cGMP by PDE4 and PDE2 ...

*Medium spiny neuron

... these neurons express D1-type dopamine receptors, adenosine A1 receptors, dynorphin peptides, and substance P peptides. ... Both types express glutamate receptors (NMDAR and AMPAR), cholinergic receptors (M1 and M4) and CB1 receptors are expressed on ... they also express adenosine A1 receptors), while dynorphinergic MSNs connect the striatum with the substantia nigra (pars ... and express the peptides dynorphin and substance P and dopamine D1 and adenosine A1 but not A2A receptors (Ferréet al., 1997; ...

*Valerian (herb)

Valerian also contains isovaltrate, which has been shown to be an inverse agonist for adenosine A1 receptor sites. This action ... Holzl J, Godau P (1989). "Receptor binding studies with Valeriana officinalis on the benzodiazepine receptor". Planta Medica. ... Identification of isovaltrate as an inverse agonist at A1 receptors". Biochemical Pharmacology. 73 (2): 248-58. doi:10.1016/j. ... generally are believed to have some affinity for the GABAA receptor, a class of receptors on which benzodiazepines are known to ...

*Pre-Bötzinger complex

Adenosine modulates the preBötC output via activation of the A1 and A2A receptor subtypes. An adenosine A1 receptor agonist has ... Effects of adenosine A1 receptor activation". BMC Neuroscience. 9: 95. doi:10.1186/1471-2202-9-95. PMC 2567986 . PMID 18826652 ... Another synthetic drug specific to the adenosine A2A receptor subtype is CGS-21680 that has been shown to cause apneas in 14- ... Since many of these neurons express GABA, glutamate, serotonin and adenosine receptors, chemicals custom tailored to bind at ...

*Subthalamic nucleus

... a precursor to adenosine (through a catabolic process). In turn, adenosine A1 receptor activation depresses excitatory ... However, it has been shown in thalamic slices from mice, that the stimulus also causes nearby astrocytes to release adenosine ... "Adenosine is crucial for deep brain stimulation-mediated attenuation of tremor". Nature Medicine. 14 (1): 75-80. doi:10.1038/ ...

*EPB41L2

2004). "Cytoskeletal protein 4.1G binds to the third intracellular loop of the A1 adenosine receptor and inhibits receptor ... Shen, L; Liang F; Walensky L D; Huganir R L (November 2000). "Regulation of AMPA receptor GluR1 subunit surface expression by a ... Shen L, Liang F, Walensky LD, Huganir RL (2001). "Regulation of AMPA receptor GluR1 subunit surface expression by a 4. 1N- ... Binda AV, Kabbani N, Lin R, Levenson R (2002). "D2 and D3 dopamine receptor cell surface localization mediated by interaction ...

*RNF5

Liu AM, Wong YH (2005). "G16-mediated activation of nuclear factor kappaB by the adenosine A1 receptor involves c-Src, protein ...

*Cardiorenal syndrome

Givertz, M. M.; Massie B. M.; Fields T. K.; Pearson L. L. (2007). "The effects of KW-3902 an adenosine A1-receptor antagonist, ... It was found that an adenosine A1-receptor antagonist called KW-3902 was able to improve kidney function in CRS patients. ... Adenosine antagonists Adenosine is responsible for constriction of afferent arteriole and reduction in GFR. ...

*Diprophylline

Schwabe, U; Ukena, D; Lohse, MJ (September 1985). "Xanthine Derivatives as Antagonists at A1 and A2 Adenosine Receptors". ... It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. Xanthine "International Non-Proprietary Names. ...

*Methoxy arachidonyl fluorophosphonate

... evidence against constitutive activity of rat brain adenosine A1 and cannabinoid CB1 receptors". Br. J. Pharmacol. 140 (8): ... In addition, it binds to the CB1 receptor in rat brain membrane preparations (IC50 = 20 nM), but does not appear to agonize or ... antagonize the receptor. DIFP - diisopropyl fluorophosphate, a related inhibitor IDFP - isopropyl dodecylfluorophosphonate, ...
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2-Chlorophenyl cyclopentyl ketone | C12H13ClO | CID 81223 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
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BioAssay record AID 581576 submitted by ChEMBL: Displacement of [3H]3-methoxy-PEPy from rat mGluR5 receptor allosteric binding site at 30 uM.
Adenosine is an important mediator of the endogenous defense against ischemia-induced injury in the heart. Adenosine can achieve cardioprotection by mediating the effect of ischemic preconditioning and by protecting against myocyte injury when it is present during the infarct-producing ischemia. A novel adenosine A3 receptor can mediate this protective function. One approach to achieve cardioprotection is to enhance myocardial sensitivity to the endogenous adenosine by increasing the number of adenosine receptors instead of administering an adenosine receptor agonist. The objective of the present study was to investigate whether genetic manipulation of the cardiac myocyte, achieved by gene transfer and overexpression of the human A3 receptor cDNA, renders the myocytes resistant to the deleterious effect of ischemia. Prolonged hypoxia with glucose deprivation, causing myocyte injury and adenosine release, was used to simulate ischemia in cultured chick embryo ventricular myocytes. During simulated
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Adenosine mediates many physiological functions via activation of extracellular receptors. The modulation of cell growth by adenosine was found to be receptor-mediated. In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. When both A1 and A2 receptors were blocked, colony formation or growth was not inhibited at low concentrations of adenosine but was inhibited at high adenosine concentrations ...
Cyclic 3, 5-[14C]AMP was measured in platelets that had first been incubated with [14C]adenine. Maximum increases of 2-4-fold were observed 0.5 min after addition of 10-40 µM adenosine. Smaller increases were obtained with higher concentrations of adenosine. In 0.5-min incubations 2-chloroadenosine was less effective than adenosine at concentrations below 20 µM and more effective at concentrations above 100 µM. Incorporation of 1-10 µM adenosine into platelets was inhibited at least 96% by p-nitrobenzylthioguanosine without any effect on the increase in cyclic [14C]AMP caused by these concentrations of adenosine, suggesting that adenosine acts at an extracellular site. With higher adenosine concentrations, p-nitrobenzylthioguanosine was less effective in inhibiting incorporation of adenosine but blocked the decline in cyclic [14C]AMP levels observed on increasing the adenosine concentration above 40 µM. This inhibitory effect of high adenosine concentrations on the accumulation of cyclic ...
Synonyms for adenosine 5'-diphosphate in Free Thesaurus. Antonyms for adenosine 5'-diphosphate. 1 synonym for adenosine diphosphate: ADP. What are synonyms for adenosine 5'-diphosphate?
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Breakdown of excessive amounts of adenosine triphosphate (ATP), the main energy source of a cell, leads to the formation of extracellular adenosine, an important signaling molecule involved in multiple pathways that regulate neuronal and immunological function. Adenosine is either actively produced by certain cells or is released from damaged tissue, particularly when cells are starved of oxygen. Adenosine levels are tightly regulated at all points throughout its production, release, uptake and degradation, and disruptions in control that result in excessively high levels are associated with a number of human pathologies, including severe combined immunodeficiency (SCID).. The diversity in the regulation and function of adenosine (both of which differ in a tissue- and cell-specific manner) means that it has been difficult to unravel its exact role at the molecular level. In addition, data obtained in vitro, or in tissue culture, might not be relevant to whole organisms, and mammalian model ...
symbol: AdoPP[CH2]P or p[CH2]ppA; the recommended name for β, γ‐methyleneadenosine 5′‐triphosphate (abbr.: ATP[β,γ‐CH2]); 5′‐adenylyl methylenediphosphonate (abbr.: AMP‐PCP); adenosine (5′→O1)‐1,2‐μ‐methylenetriphosphate; a synthetic analogue of adenosine 5′‐triphosphate, ATP, in which the oxy ... ...
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德國康佳強力脈通 Asekivex 60粒, 強力脈通Heibuken Strong Maton 100粒, 心腦素 Adenosine Triphospat 100粒, 血脈素 Adenosine Triphosphat 100粒, 高樂
A concise synthesis of a series of N6-substituted adenosines with bicyclo[3.2.1]octan-6-yl and polycyclic N6-substituents has been developed. The adenosine A1 receptor (A1R) affinity and potency of these compounds was initially assessed using competitive binding assays and cyclic adenosine monophosphate (cAMP) accumulation assays in DDT1 MF-2 cells. The potency and receptor subtype selectivity of selected examples was further evaluated by measuring their effects on cAMP accumulation at all human adenosine receptor subtypes expressed in CHO cells. The results of these assays indicated that all of the synthesised N6-substituted adenosines are full agonists at A1R and activate this receptor selectively over the other adenosine receptor subtypes. The two standout compounds in terms of potency were N6-(3-thiabicyclo[3.2.1]octan-6-yl)adenosine and N6-(cubanylmethyl)adenosine with EC50 values at human A1R of 2.3 nM and 1.1 nM, respectively. The cubanylmethyl derivative in particular proved to be highly ...
Persantine is a drug that is routinely used to determine blood flow to the heart in the diagnosis of coronary heart disease. Persantine causes an increase in the adenosine level in the blood. Adenosine is a naturally occurring substance in the body that can increase blood flow. Adenosine is normally removed from the bloodstream by an adenosine transporter, which is a protein that takes up adenosine from the blood into cells. The increase in adenosine levels in the blood is variable, and the cause for this variability is unknown. A mutation for this transporter gene may contribute to this variability, and may alter its function. Thus, the purpose of this study is to determine the relationship between the mutation and the transporter function ...
The importance of adenosine in blood flow control during exercise in normoxia and hypoxia was examined in the present study by femoral arterial infusion of the nonspecific adenosine receptor blocker aminophylline as previously applied in the studies of forearm blood flow in systemic hypoxia at rest (29) and in normoxic (32) and hypoxic (8) forearm exercise. These studies showed that aminophylline is effectively delivered from luminal to muscle interstitial spaces and that it not only inhibited the normal flow increase with contractions (32) but also effectively inhibited intraluminal adenosine acting on the endothelium, since resting hypoxic vasodilation was abolished (29). As mentioned, in the present study, blood flow was enhanced substantially from rest and was significantly higher in hypoxic exercise compared with normoxia. Aminophylline did not affect blood flow in exercising QF, suggesting no contribution of adenosine to capillary blood flow in normoxic or hypoxic exercise in the ...
Adenosine is a candidate sleep substance. It can be both a distress signal of importance in pathology and a physiological regulator. Key factors in determining which of these possibilities pertain are: (i) the number of receptors expressed, and (ii) the mechanisms that establish extracellular adenosine levels. The roles of adenosine are studied by means of antagonists and/or animals (mostly mice) with targeted deletions of receptors or enzymes involved in adenosine metabolism. Whereas adaptive changes in the genetically modified mice can occur for the physiologically important effects, such adaptive changes are less likely to occur in situations where adenosine acts as a distress signal. The relevance to sleep will be covered only in general terms in this review and will be covered in other contributions to this volume.
Intra- and extracellular adenosine levels rise in response to physiological stimuli and with metabolic/energetic perturbations, inflammatory challenge and tissue injury. Extracellular adenosine engages members of the G-protein coupled adenosine receptor (AR) family to mediate generally beneficial acute and adaptive responses within all constituent cells of the heart. In this way the four AR sub-types - A1, A2A, A2B, and A 3Rs - regulate myocardial contraction, heart rate and conduction, adrenergic control, coronary vascular tone, cardiac and vascular growth, inflammatory-vascular cell interactions, and cellular stress-resistance, injury and death. The AR sub-types exert both distinct and overlapping effects, and may interact in mediating these cardiovascular responses. The roles of the ARs in beneficial modulation of cardiac and vascular function, growth and stress-resistance render them attractive therapeutic targets. However, interactions between ARs and with other receptors, and their ubiquitous
The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of ...
In this study and previously (24), we have demonstrated that blockade of the A2AAR with an A2A-specific AR antagonist protected mice from EAE by hindering lymphocyte entry into the brain and spinal cord of wild-type mice. This finding was unexpected, as this function of adenosine, that is, mediating lymphocyte migration into the CNS, was previously unknown. Furthermore, the facts that adenosine suppresses the immune response and resolves inflammation (2) are at odds with the finding that blockade of the A2AAR, which mediates the preponderance of adenosines suppressive and anti-inflammatory functions (2), protects mice from EAE (24). The purpose of this study was to delineate adenosines role in the immune response from its function in mediating immune cell migration into the CNS via the A2A receptor.. We show that A2AAR−/− mice developed more severe EAE than did their wild-type counterparts. This severe disease was characterized in the CNS by increased numbers of lymphocytes and activated ...
Synonyms for adenosine triphosphatase test in Free Thesaurus. Antonyms for adenosine triphosphatase test. 2 words related to adenosine: biochemistry, nucleoside. What are synonyms for adenosine triphosphatase test?
Abstract BACKGROUND: In view of the multiple effects of adenosine on kidney function, this study aimed to determine the expression of adenosine receptors (AR) along the rat and mou..
Action adenosinergic funds due to a direct interaction with adenozinovymi (purine) receptors and indirect effect on the disintegration and accumulation of adenosine (one of the purine neuromodulators). Specialized purine receptors (post - and presynaptic), divided into the P1 receptors (highly sensitive to adenosine) and P2 receptors (more sensitive to ATP). Both types are found in the Central nervous system, cardiovascular and respiratory system, lymph and platelets, etc.. It is known that adenosine has mainly cardiovascular effects, manifested by vasodilatation (with improvement of microcirculation and reduction of platelet aggregation) and negative Ino-, Chrono and dromotropony effects on the heart associated with inhibition of intracellular transport of calcium ions. A number of drugs (dipyridamole, papaverine, etc.) affect the metabolism of adenosine, contribute to its accumulation in the myocardium or potentiate the effect; used as koronarolitikov the disease ...
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 ...
Researchers used a variety of methods to demonstrate that reducing adenosine or blocking the A1 adenosine receptor that is essential to the chemical messengers function changed how adult mice responded to sound.. Much as young children pick up language simply by hearing it spoken, researchers showed that when adenosine was reduced or the A1 receptor blocked in the auditory thalamus, adult mice passively exposed to a tone responded to the same tone stronger when it was played weeks or months later. These adult mice also gained an ability to distinguish between very close tones (or tones with similar frequencies).. Mice usually lack this "perfect pitch" ability. ...
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.
... contains 100mg of adenosine. Orthoplex Adenosine plays a major role in the production of cellular energy ATP
Adenosine myoview stress test - How much does adenosine nuclear stress test cost? Adenosine stress $$$. The cost depends on where you live and whether test is being done in a hospital facility or cardiologist office the cost can vary from 800$ to 2000$.
The data presented in this study demonstrate that activation of PKC-ε on stimulation of the A1R in the rat or mouse heart elicits the translocation of the kinase to a RACK2 protein of the cardiomyocyte. Previously, we reported A1R activation promotes the translocation of PKC-ε, but not PKC-δ, to the t-tubules of the cardiomyocyte (30). The present data indicate that RACK2 was the target protein for this translocation. Our present observations include the measurement of contractile activity of isolated cardiomyocytes and the visualization with imaging (rat) and coimmunoprecipitation of the kinase and RACK2 (rat and mouse). Translocation of PKC-ε to RACK2 occurred whether the PKC-ε was activated nonspecifically by a phorbol ester, or by A1R activation with PIA, or with the selective agonist CCPA. The action induced by CCPA was selective for the A1R, as indicated by the inhibition elicited by the A1R antagonist DPCPX. Furthermore, PKC-ε translocation most likely results from an A1R-induced ...
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Find patient medical information for Adenosine Triphosphate Oral on WebMD including its uses, side effects and safety, interactions, pictures, warnings and user ratings.
Adenosine is so readily formed in the brain that for some time its quantity there was overestimated by a factor of 20 or more (Berne et al. 1974; Newman and McIlwain, 1977). Now, rapid fixation...
Author: Allen Loyd V Jr, Year: 2013, Abstract: A formulation for preparing Adenosine 3-mg/mL Injection. Includes ingredients, method of preparation, discussion, and references for the compounding pharmacist.
You are viewing an interactive 3D depiction of the molecule 5-o-(4,6-dihydroxy-2,4,6-trioxido-1,3,5,2,4,6-trioxatriphosphinan-2-yl)adenosine (C10H14N5O12P3) from the PQR.
Detailed drug Information for adenosine Intravenous. Includes common brand names, drug descriptions, warnings, side effects and dosing information.
View mouse Adora1 Chr1:134199225-134235431 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
View mouse Adora2a Chr10:75316877-75334784 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
Genetic information processingProtein synthesistRNA and rRNA base modificationtRNA threonylcarbamoyl adenosine modification protein YeaZ (TIGR03725; HMM-score: 178.6) ...
AKI 1 is an adenosine regulating agent. It was undergoing preclinical studies in the USA with Gensia Sicor for the treatment of inflammatory disorders, however
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as endogenous ligand. In humans, there are four types of adenosine receptors. Each is encoded by a separate gene and has different functions, although with some overlap. For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader anti-inflammatory effects throughout the body. These two receptors also have important roles in the brain, regulating the release of other neurotransmitters such as dopamine and glutamate, while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses. Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in hospitals as treatment for severe tachycardia (rapid heart beat), and acting directly to slow the heart through ...
Adenosine is 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. For instance, adenosine plays an important role in energy transfer - as adenosine triphosphate (ATP) and adenosine diphosphate (ADP). It also plays a role in signal transduction as cyclic adenosine monophosphate, cAMP. Adenosine itself is both a neurotransmitter and potent vasodilator. When administered intravenously, adenosine causes transient heart block in the AV node. Because of the effects of adenosine on AV node-dependent supraventricular tachycardia, adenosine is considered a class V antiarrhythmic agent ...
METHODS AND RESULTS In this study, we tested whether the protection could be achieved by intravenous administration of the A1-selective adenosine agonists N6-(phenyl-2R-isopropyl)-adenosine (PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA). Nine groups of open-chest anesthetized rabbits were subjected to 30 minutes of regional coronary ischemia and 3 hours of reperfusion. Infarct size was determined by tetrazolium staining. Control hearts receiving no treatment had 38 +/- 4% of the risk zone infarcted. Preconditioning with 5 minutes of ischemia and 10 minutes of reperfusion before ischemia limited the infarct to 8 +/- 4%. Intravenous PIA 15 minutes before 30-minute ischemia also limited infarct size to 6 +/- 2% at the highest dose. CCPA offered similar protection. When the PIA was given at reperfusion, infarct size was 46 +/- 6%, indicating that receptor activation must precede ischemia to protect. Pretreatment with CGS 21680, a selective A2-receptor agonist, caused identical hypotension but ...
Adenosine was coupled to human serum albumin by two different procedures that preserved the purine and ribose rings. The conjugates were evaluated for antigenicity in rabbits and guinea pigs. A conjugate containing 2′(3′)-O-succinoyladenosine failed to elicit antibodies, whereas one containing laevulinic acid (O2′, 3′-adenosine-acetal) elicited antibodies in all animals injected. The affinity and specificity of binding of adenosine to three selected antisera were evaluated. Dissociation constants of 31-187 nM were observed. Displacement of adenosine binding to all antisera by adenine 5′-nucleotides, adenine, inosine and hypoxanthine required more than 1000-fold higher concentrations than of adenosine itself. Similar affinities for adenosine and 2′-deoxyadenosine were observed. By exploiting the high specificity of the antisera, a radioimmunoassay method was established that was capable of detecting down to 1 pmol of adenosine (20 nM) in unfractionated heart perfusates and cell ...
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Recombinant Mouse PAP Has pH-Dependent Ectonucleotidase Activity and Acts through A1-Adenosine Receptors to Mediate Antinociception. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Adenosine is the endogenous agonist at all adenosine receptors. Under resting physiological conditions, adenosine levels in the interstitial fluid are between 30 and 300 nM (7). This is sufficient to activate A1, A2A, and A3 adenosine receptors whenever these proteins are abundantly expressed on the cell surface. The local adenosine level increases 10-fold during hypoxia and 100- to 1,000-fold in ischemia (7, 18, 34, 72), allowing cell responses mediated via A2BR in these settings. The pharmacological and functional studies presented here have been conducted using parietal cells obtained from normal rabbit gastric mucosa, which are representative populations of native, nontransformed primary cells at rest. They provide evidence that A2B is the adenosine receptor that is preferentially, if not exclusively, expressed on the parietal cell membrane and mediates acid production via Gs activation. Moreover, activation kinetics indicate that the A2BR might act at full power to activate acid production ...
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Adenosine Receptor A2a小鼠单克隆抗体[7FG-G5-A2](ab79714)可与小鼠, 人样本反应并经WB实验严格验证,被2篇文献引用并得到2个独立的用户反馈。中国75%以上现货。
Cyclic AMP; 35-cyclic AMP; 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide; Acrasin; Adenosine 3,5-cyclic monophosphate; Adenosine 3,5-cyclic phosphate; Adenosine 3,5-cyclophosphate; Adenosine 3,5-monophosphate; Adenosine 3,5-cyclic monophosphorate; Adenosine 3,5-cyclic monophosphoric acid; Adenosine cyclic monophosphate; Cyclic 3,5-AMP; Cyclic 3,5-adenylate; Cyclic 3,5-adenylic acid; Cyclic adenosine 3,5-phosphate; adenosine cyclic-monophosphate; adenosine-cyclic-phosphate; adenosine-cyclic-phosphoric-acid; ...
Cyclic AMP; 35-cyclic AMP; 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide; Acrasin; Adenosine 3,5-cyclic monophosphate; Adenosine 3,5-cyclic phosphate; Adenosine 3,5-cyclophosphate; Adenosine 3,5-monophosphate; Adenosine 3,5-cyclic monophosphorate; Adenosine 3,5-cyclic monophosphoric acid; Adenosine cyclic monophosphate; Cyclic 3,5-AMP; Cyclic 3,5-adenylate; Cyclic 3,5-adenylic acid; Cyclic adenosine 3,5-phosphate; adenosine cyclic-monophosphate; adenosine-cyclic-phosphate; adenosine-cyclic-phosphoric-acid; ...
Adenosine acts as a break in biological systems, having inhibiting effects, but caffeine doesnt just stop this break, it also makes other neurotransmitters more active. For instance, it prevents breakdown of acetylcholine (ACh), so ACh sticks around longer, increasing its effect ...
Burke, Ruth M., Pearce, Julie K., Boxford, William E., Bruckmann, Angelika and Dessent, Caroline E. H. (2005) Stabilization of excess charge in isolated adenosine 5 -triphosphate and adenosine 5 -diphosphate multiply and singly charged anions. Journal of Physical Chemistry a, 109 43: 9775-9785. doi:10.1021/jp052937y ...
methyl 2-cyclopentyl-2-(methoxycarbonylamino)acetate - chemical structural formula, chemical names, chemical properties, synthesis references
Definition of adenosine monophosphate in US English - a compound consisting of an adenosine molecule bonded to one acidic phosphate group, present in most DNA and RNA. It
Adenosine Diphosphate: Adenosine 5-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5-position.
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[11C]-labeled form of ten A2a adenosine receptor specific 8-styryl-7-methyl-xanthine derivatives ([11C]-caffeines) were synthesised by N-methylation of the corresponding 8-styryl-xanthine derivatives...
Mechanisms involved in increased sensitivity to adenosine A2A receptor activation and hypoxia-induced vasodilatation in porcine coronary ...
A photosensitive resin composition comprising: (a) at least one polybenzoxazole precursor polymer; (b) at least one compound having Structure VI wherein, V is CH or N, Y is O or NR 3 wherein R 3 is H, CH 3 or C 2 H 5 , R 1 and R 2 each independently are H, C 1 -C 4 alkyl group, C 1 -C 4 alkoxy group, cyclopentyl or cyclohexyl, or alternatively, R 1 and R 2 can be fused to produce a substituted or unsubstituted benzene ring; and (c) at least one solvent; wherein the amount of the compound of Structure VI present in the composition is effective to inhibit residue from forming when the composition is coated on a substrate and the coated substrate is subsequently processed to form an image on the substrate, and with the proviso that if the polybenzoxazole precursor polymer solely consists of polybenzoxazole precursor
Quantitative in vivo Imaging of Adenosine A2A Receptors in the Human Brain Using 11C-SCH442416 PET: A Pilot Study. This pilot PET study demonstrates that A2A receptor binding can be quantified in striatal regions of the human brain by using 11C-SCH442416
Adenosine Triphosphate (ATP) is an excellent biomarker present in all living cells. During the past several years, several ATP test methods have been
Page contains details about glucose oxidase- & horseradish peroxidase-loaded Zn-linked adenosine 5-monophosphate . It has composition images, properties, Characterization methods, synthesis, applications and reference articles : nano.nature.com
20816-58-4 - ZZVDSVGETAFWNA-QYVSTXNMSA-N - Adenosine 5-phosphoroimidazolide - Similar structures search, synonyms, formulas, resource links, and other chemical information.
ウサギ・ポリクローナル抗体 ab106143 交差種: Hu 適用: WB,IHC-P,ICC/IF…Adenosine Receptor A2a抗体一覧…画像、プロトコール、文献などWeb上の情報が満載のアブカムの Antibody…
Here youll read about the definition and chemical structure of ATP and the different ways it can be produced and how it functions in the human body.
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DNA, Magnetic, Permit, Proteins, Adenosine, Base Pair, Behavior, Cancer, Concentrations, Genome, Growth, Human, Maintenance, Nucleoprotein, Polymerization, Recombinase, Time, Adenosine Triphosphate, ATP, Atpase
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Genetic information processingProtein synthesistRNA and rRNA base modificationtRNA threonylcarbamoyl adenosine modification protein, Sua5/YciO/YrdC/YwlC family (TIGR00057; HMM-score: 194.3) ...
Previous in vitro studies have shown biphasic effects of adenosine on mast cell activity; however, the receptor subtypes that mediate the inhibitory effects of adenosine are still controversial (Peachell et al., 1991; Yip et al., 2009). Mast cells express two distinct Gs-coupled adenosine receptors; their biologic roles have not been comprehensively defined, especially in vivo. Since activation of Gs-coupled adenosine receptors increases intracellular cAMP, we hypothesized that the inhibitory effects of adenosine on mast cells are mediated by the Gs-coupled adenosine receptors. In this study, we used both genetically modified animal models and mast cell cultures to comprehensively investigate the role of Gs-coupled adenosine receptors on mast cells both in vitro and in vivo. First, our data demonstrate a potent inhibitory effect of the nonhydrolyzable adenosine analog NECA on IgE-induced mast cell degranulation; this inhibitory effect of NECA was abolished by the genetic deletion of the A2B but ...
We performed experiments to test the hypothesis that endogenous adenosine acts as an essential cofactor required for eliciting angiotensin II (Ang II)-induced afferent and/or efferent arteriolar vasoconstriction. Enalaprilat (2 mg IV) was administered to anesthetized rats to reduce endogenous Ang II levels. Kidneys and blood were harvested from these animals and used for study of renal microvascular function using the in vitro blood-perfused juxtamedullary nephron technique. Arteriolar inside diameter was monitored videomicroscopically in (1) normal kidneys, (2) kidneys subjected to adenosine receptor blockade (100 mumol/L 1,3-dipropyl-8-p-sulfophenylxanthine), and (3) kidneys continuously exposed to 1 mumol/L adenosine. Under resting conditions, arteriolar diameters were similar in all three groups of kidneys, averaging 24.8 +/- 1.0 microns (n = 23) in afferent arterioles and 24.0 +/- 0.9 microns (n = 16) in efferent arterioles. In normal kidneys, adenosine (10 mumol/L) decreased both afferent ...
A series of 5-carbamoyl and 5-thionocarbamoyl derivatives of 2-C-methyl analogues of the A(1) adenosine receptor (A(1)AR) full agonists N(6)-cyclopentyladenosine (CPA), 2-chloro-N(6)-cyclopentyladenosine (CCPA), N(6)-[3-(R)-tetrahydrofuranyl]adenosine (tecadenoson), and 2-chloro analogue (2-Cl-tecadenoson) was synthesized and evaluated for their affinity for adenosine receptor subtypes from bovine, porcine, and human species. In the N(6)-cyclopentylamino series, the 5-substituted derivatives showed a reduced affinity at the bovine A(1)AR compared to the parent compounds; however, the selectivity for A(1) versus A(2A) receptor was retained or increased. The corresponding N(6)-3-(R)-tetrahydrofuranylamino analogues displayed a very low affinity toward the bovine A(1)AR. The 5-methylthionocarbamoyl derivative of 2-Me-CCPA showed the best affinity at porcine A(1)AR with a K(i) value of 13 nM. At human AR subtypes tecadenoson derivatives showed 2.3- to 5-fold lower affinity at A(1)AR and very ...
To the Editor: Recently, Jeremias et al1 reported their studies comparing the vasodilator action of intracoronary injected adenosine with ATP in 6 healthy mongrel dogs. On the basis of a dose-response curve ranging from 10 to 100 μg, the authors conclude that adenosine and ATP are approximately equipotent vasodilators. Neither substance could induce maximal vasodilation, as assessed with postischemic hyperemia. Similar results were obtained by Kato et al2 in the human coronary vasculature using a single dose of adenosine and ATP (20 μg), without comparison with postischemic hyperemia. Both groups conclude that adenosine and ATP are equipotent coronary vasodilators and suggest that the ATP-induced vasodilation is caused by its degradation to AMP and adenosine, with subsequent stimulation of adenosine A2 receptors. We disagree their conclusions for the following 2 reasons:. 1. Equimolar doses of ATP and adenosine should be compared. The molecular weight of ATP is roughly twice that of adenosine ...
The review summarizes data evaluating the role of adenosine receptor signaling in murine hematopoietic functions. The studies carried out utilized either non-selective activation of adenosine receptors induced by elevation of extracellular adenosine or by administration of synthetic adenosine analogs having various proportions of selectivity for a particular receptor. Numerous studies have described stimulatory effects of non-selective activation of adenosine receptors, manifested as enhancement of proliferation of cells at various levels of the hematopoietic hierarchy. Subsequent experimental approaches, considering the hematopoiesis-modulating action of adenosine receptor agonists with a high level of selectivity to individual adenosine receptor subtypes, have revealed differential effects of various adenosine analogs. Whereas selective activation of A(1) receptors has resulted in suppression of proliferation of hematopoietic progenitor and precursor cells, that of A(3) receptors has led to ...
Background & Aims: During fibrosis hepatic stellate cells (HSC) undergo activation, proliferation and senescence but the regulation of these important processes is poorly understood. The adenosine A2A receptor (A2A) is known to be present on HSC, and its activation results in liver fibrosis. In this study, we tested if A2A has a role in the regulation of HSC proliferation, apoptosis, senescence, and the relevant molecular mechanism.Methods: The ability of adenosine to regulate p53 and Rb protein levels, proliferation, apoptosis and senescence was tested in the human HSC cell line LX-2 and rat primary HSC.Results: Adenosine receptor activation down-regulates p53 and Rb protein levels, increases BrdU incorporation and increases cell survival in LX-2 cells and in primary rat HSC. These effects of NECA were reproduced by an adenosine A2A receptor specific agonist (CGS21680) and blocked by a specific antagonist (ZM241385). By day twenty-one of culture primary rat HSC entered senescence and expressed -gal
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P>Adenosine is a well-described anti-inflammatory modulator of immune responses within peripheral tissues. Extracellular adenosine accumulates in inflamed and damaged tissues and inhibits the effector functions of various immune cell populations, including CD8 T cells. However, it remains unclear whether extracellular adenosine also regulates the initial activation of naive CD8 T cells by professional and semi-professional antigen-presenting cells, which determines their differentiation into effector or tolerant CD8 T cells, respectively. We show that adenosine inhibited the initial activation of murine naive CD8 T cells after alpha CD3/CD28-mediated stimulation. Adenosine caused inhibition of activation, cytokine production, metabolic activity, proliferation and ultimately effector differentiation of naive CD8 T cells. Remarkably, adenosine interfered efficiently with CD8 T-cell priming by professional antigen-presenting cells (dendritic cells) and semi-professional antigen-presenting cells ...
294964902 - EP 1019427 A1 2000-07-19 - N?6 -SUBSTITUTED-ADENOSINE-5 -URONAMIDES AS ADENOSINE RECEPTOR MODULATORS - [origin: WO9906053A1] A series of adenosine-5 -uronamide derivatives bearing N 6 -arylurea, alkarylurea, heteroarylurea, arylcarbonyl, alkarylcarbonyl or heteroarylcarbonyl groups which have affinity and, in some cases, selectivity for the adenosine A1 or A3 receptors are disclosed. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A1 or A3 receptors, or can be used in a diagnostic application to determine the relative binding of other compounds to the A1 or A3 receptors.[origin: WO9906053A1] A series of adenosine-5 -uronamide derivatives bearing N 6 -arylurea, alkarylurea, heteroarylurea, arylcarbonyl, alkarylcarbonyl or heteroarylcarbonyl groups which have affinity and, in some cases, selectivity for the adenosine A1 or A3 receptors are disclosed. These compounds can be used in a pharmaceutical composition to treat
The IUPHAR/BPS Guide to Pharmacology. cyclopentyladenosine ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Objectives:. The overall goal of this proposal is to develop methods to achieve heart and vascular protection from ischemia and thus improve soldiers performance in adverse environment. The major hypothesis is that new approach and method can be developed to enhance resistance to stress-induced circulatory insufficiency and myocardial ischemia. The goals here are to determine whether a decreased adenosine transporter function is associated with a reduced physiological responsiveness to the vasculo-protective drug persantine using two in vitro endpoints: the ability of persantine 1) to inhibit platelet aggregation and 2) to inhibit [3H] uridine uptake. Both are endpoints that indicate physiological responsiveness. Both relate directly to the cardiovascular protective effects of , that is, persantine the availability of extracellular adenosine level and the anti-platelet property. Specifically, the relationship between circulating adenosine increase to persantine in vivo and blockade of ...
Definition of adenosine in the Financial Dictionary - by Free online English dictionary and encyclopedia. What is adenosine? Meaning of adenosine as a finance term. What does adenosine mean in finance?
The adenosinergic system is essential in the mediation of intrinsic protection and myocardial resistance to insult; it may be considered a cardioprotective molecule and adenosine receptors (ARs) represent potential therapeutic targets in the setting of heart failure (HF). The aim of the study was to test whether differences exist between mRNA expression of ARs in the anterior left ventricle (LV) wall (pacing site: PS) compared to the infero septal wall (opposite region: OS) in an experimental model of dilated cardiomyopathy. Cardiac tissue was collected from LV PS and OS of adult male minipigs with pacing-induced HF (n = 10) and from a control group (C, n = 4). ARs and TNF-α mRNA expression was measured by Real Time-PCR and the results were normalized with the three most stably expressed genes (GAPDH, HPRT1, TBP). Immunohistochemistry analysis was also performed. After 3 weeks of pacing higher levels of expression for each analyzed AR were observed in PS except for A1R (A1R: C = 0.6±0.2, PS = ...
Since their discovery approximately 25 years ago, adenosine receptors have now emerged as important novel molecular targets in disease and drug discovery. These proteins play important roles in the entire spectrum of disease from inflammation to immune suppression. Because of their expression on a number of different cell types and in a number of different organ systems they play important roles in specific diseases, including asthma, rheumatoid arthritis, Parkinsons disease, multiple sclerosis, Alzheimers disease, heart disease, stroke, cancer, sepsis, and obesity. As a result of intense investigations into understanding the molecular structures and pharmacology of these proteins, new molecules have been synthesized that have high specificity for these proteins and are now entering clinical trials. These molecules will define the next new classes of drugs for a number of diseases with unmet medical needs.
The IUPHAR/BPS Guide to Pharmacology. A1 receptor - Adenosine receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
Sweeney-Nixon, M. I., White, T., & Sawynok, J. (1989). Adenosine release from the spinal cord may mediate antinodideption by intracerebroventricular morphine. Society For Neuroscience Abstracts, 15, 371 ...
Adenosine is an endogenous immunosuppressant that binds to adenosine receptor checkpoints and protects tissue from immune-mediated rejection. Abnormally high adenosine levels (up to 100-fold greater than other tissues) contribute to a highly immunosuppressive tumor microenvironment (TME). We hypothesized that adenosine deaminase 2 (ADA2), a human enzyme that catalyzes the deamination of adenosine, could be administered at therapeutic levels to deplete high levels of TME adenosine and stimulate anti-tumor immune activity. Recombinant wild-type ADA2 (wtADA2) was cleared extremely rapidly from circulation (t1/2 = 69 min, 7.5 mg/kg iv, n = 9 mice), rendering it unsuitable for therapeutic testing. Therefore, a series of variants was designed to attenuate the heparin binding properties of ADA2 to improve bio-distribution and conjugated with 20K PEG to improve pharmacokinetics (PK). The variant PEG-ADA2-K374D displayed 94% less binding to heparin compared to wtADA2, enzymatic activity comparable to ...
ATP (ADENOSINE TRIPHOSPHATE) It is a chemical compound. ATP is an abbreviation of adenosine triphosphate. Its name indicates that it contains adenosine and
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Effects of increased myocardial adenosine concentrations in patients with acute myocardial-infarction receiving thrombolytic ...
Our work demonstrates that human endothelial cells of disparate origin are characterized by differential expression of adenosine receptor subtypes. HUVECs express mRNA for A2A and A2B receptors at a ratio of 10:1, and this preferential gene expression agrees well with the typical pharmacological phenotype of A2A receptor-mediated simulation of adenylate cyclase by adenosine analogs. Using complementary techniques, RT-PCR, and gene expression array, we found that A1 and A3 adenosine receptors are not expressed in HUVECs. Previous studies in HUVECs have suggested a potential role of A1 receptor in maintaining endothelial barrier function4 and of A1 and A3 receptors in modulation of tissue factors expression.6 The apparent contradiction between these results and ours can be explained by the use of nonselective concentrations of adenosine receptor ligands in previous studies.. HMEC-1 also express only A2A and A2B mRNA, but in contrast to HUVECs, they express predominantly A2B receptor mRNA, with a ...
We examined how the endogenous anticonvulsant adenosine might influence gamma-aminobutyric acid type A (GABA(A)) receptor stability and which adenosine receptors (ARs) were involved. Upon repetitive activation (GABA 500 microM), GABA(A) receptors, microtransplanted into Xenopus oocytes from neurosurgically resected epileptic human nervous tissues, exhibited an obvious GABA(A)-current (I(GABA)) run-down, which was consistently and significantly reduced by treatment with the nonselective adenosine receptor antagonist CGS15943 (100 nM) or with adenosine deaminase (ADA) (1 units/ml), that inactivates adenosine. It was also found that selective antagonists of A2B (MRS1706, 10 nM) or A3 (MRS1334, 30 nM) receptors reduced I(GABA) run-down, whereas treatment with the specific A1 receptor antagonist DPCPX (10 nM) was ineffective. The selective A2A receptor antagonist SCH58261 (10 nM) reduced or potentiated I(GABA) run-down in approximately 40% and approximately 20% of tested oocytes, respectively. The ...
Adenosine is a purine nucleoside that is commonly expressed in the body and involved in a wide range of physiological processes. The effects of adenosine are mediated through specific G-protein coupled cell surface receptors, named A1, A2A, A2B and A3 adenosine receptors (ARs). It is now well recognized that extracellular levels of adenosine markedly increase under metabolically stressful conditions and in the last two decades it has become clear that adenosine is a mediator involved in the pathogenesis of lung inflammatory disorders and in cancer. Indeed adenosine induces bronchoconstriction in animal models and in patients with airway diseases such as asthma and chronic obstructive pulmonary diseases (COPD). COPD is defined as an inflammatory respiratory disease, largely caused by exposure to tobacco smoke. The disease is characterized by a progressive and incompletely reversible airflow obstruction. The key elements of COPD are exposure to cigarette smoke, airway inflammation, and airflow ...
The possibility that adenosine modulates voltage-dependent conductances in locus coeruleus neurons was investigated in current-clamp and voltage-clamp experiments in a totally submerged rat brain slice preparation. Adenosine (100 microM) reduced the duration of control action potentials and action potentials prolonged by 1 mM barium. Adenosine (100 microM) also reduced the amplitude and slightly reduced the duration of TTX-resistant "calcium" action potentials. Action potential duration was also reduced by the adenosine receptor agonist 2- chloroadenosine in a concentration-dependent manner and the adenosine- induced reduction of action potential duration was blocked by the adenosine receptor antagonist 8-(p-sulfophenyl)theophylline, indicating that this action of adenosine is mediated by an adenosine receptor. The adenosine-induced reduction of action potential duration persisted in the presence of externally applied tetraethylammonium ion (6 mM) and cesium (3 mM). By contrast, adenosine did ...

ANTAGONIST OF A2B ADENOSINE RECEPTORS FOR ASTHMA | SBIR.govANTAGONIST OF A2B ADENOSINE RECEPTORS FOR ASTHMA | SBIR.gov

... receptor subtypes and produces side effects due primarily to A1 receptor blockade, including insomnia and diuresis. The ... adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells ... A2B adenosine receptors are blocked by theophylline, a xanthine that is effective in treating asthma. However, theophylline is ... New drugs that are potent and selective antagonists of A2B adenosine receptors have great potential for the treatment of asthma ...
more infohttps://www.sbir.gov/sbirsearch/detail/71816

Anti-Adenosine A1 Receptor/adora1 antibody (ab223377)Anti-Adenosine A1 Receptor/adora1 antibody (ab223377)

Rabbit polyclonal Adenosine A1 Receptor antibody validated for Western Blot, ICC/IF & tested in Human. Immunogen corresponding ... Anti-Adenosine A1 Receptor antibody. See all Adenosine A1 Receptor primary antibodies. ... All lanes : Anti-Adenosine A1 Receptor antibody (ab223377) at 1/1000 dilution. Lane 1 : HeLa (human epithelial cell line from ... 4% formaldehyde-fixed SK-N-BE cells stained for Adenosine A1 Receptor (green) using ab223377 at 1/100 dilution in ICC/IF. ...
more infohttps://www.abcam.com/adenosine-a1-receptor-antibody-ab223377.html

Adenosine A1 Receptor ELISA Kits | Biocompare.comAdenosine A1 Receptor ELISA Kits | Biocompare.com

Compare Adenosine A1 Receptor ELISA Kits from leading suppliers on Biocompare. View specifications, prices, citations, reviews ... Adenosine A1 Receptor ELISA Kits. The ELISA (enzyme-linked immunosorbent assay) is a well-established antibody-based tool for ... Your search returned 112 Adenosine A1 Receptor ELISA ELISA Kit across 14 suppliers. ... Our laboratory focuses on effects of aryl hydrocarbon receptor (AhR) activation in dendritic cells. ... read more ...
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Anti-Adenosine A1 Receptor antibody [EPR6179] (ab124780) ProtocolsAnti-Adenosine A1 Receptor antibody [EPR6179] (ab124780) Protocols

Abcam provides specific protocols for Anti-Adenosine A1 Receptor antibody [EPR6179] (ab124780) : Flow cytometry protocols, ...
more infohttp://www.abcam.com/adenosine-a1-receptor-antibody-epr6179-ab124780-protocols.html

MilliporeSigma Calbiochem Adenosine A1 Receptor Agonist I, CPA 25mg:LifeMilliporeSigma Calbiochem Adenosine A1 Receptor Agonist I, CPA 25mg:Life

MilliporeSigma Calbiochem Adenosine A1 Receptor Agonist I, CPA 25mg Life Sciences:Protein Biology:Protein Extraction and ... MilliporeSigma Calbiochem Adenosine A1 Receptor Agonist I, CPA A potent and selective agonist of adenosine A1 receptor (A1R) (K ... A potent and selective agonist of adenosine A1 receptor (A1R) (Ki = 2.3 nM, 790 nM, 18.6µM, 43nM for human A1, A2A, A2B, and A3 ...
more infohttps://www.fishersci.com/shop/products/calbiochem-adenosine-a1-receptor-agonist-i-cpa/11913525MG

Adora1 MGI Mouse Gene Detail - MGI:99401 - adenosine A1 receptorAdora1 MGI Mouse Gene Detail - MGI:99401 - adenosine A1 receptor

J:243585 Riff R, et al., Systemic inflammatory response syndrome-related lymphopenia is associated with adenosine A1 receptor ...
more infohttp://www.informatics.jax.org/marker/MGI:99401

anti-Adenosine A1 Receptor antibody [N3C2], Internal  | GeneTexanti-Adenosine A1 Receptor antibody [N3C2], Internal | GeneTex

... adenosine A1 receptor) for WB. Anti-Adenosine A1 Receptor pAb (GTX100025) is tested in Human, Mouse samples. 100% Ab-Assurance. ... Adenosine A1 Receptor antibody [N3C2], Internal See all Adenosine A1 Receptor products ... RDC7 antibody, ADORA1 antibody, adenosine receptor A1 antibody, adenosine A1 receptor antibody. ... adenosine A1 receptor. Background. The protein encoded by this gene is an adenosine receptor that belongs to the G-protein ...
more infohttp://www.genetex.com/Adenosine-A1-Receptor-antibody-N3C2-Internal-GTX100025.html

Caffeine acts via A1 adenosine receptors to disrupt embryonic cardiac function.Caffeine acts via A1 adenosine receptors to disrupt embryonic cardiac function.

Evidence suggests that adenosine acts via cardiac A1 adenosine receptors (A1ARs) to protect embryos against hypoxia. During ... BACKGROUND: Evidence suggests that adenosine acts via cardiac A1 adenosine receptors (A1ARs) to protect embryos against hypoxia ... Treatment with adenosine receptor-selective antagonists revealed that SCH-58261 (A2aAR-specific antagonist) had no affects on ... METHODOLOGY/PRINCIPAL FINDINGS: Effects of caffeine and adenosine receptor-selective antagonists on heart rate were studied in ...
more infohttp://www.biomedsearch.com/nih/Caffeine-Acts-via-A1-Adenosine/22164264.html

Adenosine A1 receptor - WikipediaAdenosine A1 receptor - Wikipedia

The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. Activation of the adenosine A1 receptor ... "Adenosine Receptors: A1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Adenosine A1 Receptor at the US National Library of Medicine Medical Subject Headings (MeSH) Human ADORA1 genome location and ...
more infohttps://en.wikipedia.org/wiki/Adenosine_A1_receptor

Adenosine A1 Receptor Antibody 55026-1-AP  | ProteintechAdenosine A1 Receptor Antibody 55026-1-AP | Proteintech

Adenosine A1 Receptor Antibody 55026-1-AP has been identified with IHC, WB, ELISA. 55026-1-AP detected 37 kDa band in SH-SY5Y ... Adenosine A1 Receptor Antibody 1 Publications. Rabbit Polyclonal, Catalog number: 55026-1-AP ... SH-SY5Y cells were subjected to SDS PAGE followed by western blot with 55026-1-AP(Adenosine A1 Receptor antibody) at dilution ... SH-SY5Y cells were subjected to SDS PAGE followed by western blot with 55026-1-AP(Adenosine A1 Receptor antibody) at dilution ...
more infohttps://www.ptglab.com/Products/ADORA1-Antibody-55026-1-AP.htm

Ageing-related decline in adenosine A1 receptor binding in the rat brain: An autoradiographic study - Meerlo - 2005 - Journal...Ageing-related decline in adenosine A1 receptor binding in the rat brain: An autoradiographic study - Meerlo - 2005 - Journal...

Ageing-related decline in adenosine A1 receptor binding in the rat brain: An autoradiographic study. Authors. *. Peter Meerlo, ... also in response to an adenosine A1 agonist, old rats had less sleep compared with young animals." Our sincere apologies are ...
more infohttp://onlinelibrary.wiley.com/doi/10.1002/jnr.20427/full

A1 Adenosine Receptor Upregulation and Activation Attenuates Neuroinflammation and Demyelination in a Model of Multiple...A1 Adenosine Receptor Upregulation and Activation Attenuates Neuroinflammation and Demyelination in a Model of Multiple...

Adenosine analogs with covalently attached lipids have enhanced potency at A1-adenosine receptors. FEBS Lett 225: 97-102. ... Johnston JB, Silva C, Gonzalez G, Holden J, Warren KG, Metz LM, Power C (2001a) Diminished adenosine A1 receptor expression on ... Mayne M, Shepel PN, Jiang Y, Geiger JD, Power C (1999) Dysregulation of adenosine A1 receptor-mediated cytokine expression in ... Ren H, Stiles GL (1995) Separate promoters in the human A1 adenosine receptor gene direct the synthesis of distinct messenger ...
more infohttp://www.jneurosci.org/content/24/6/1521

Synthesis and Biological Evaluation of Adenosines with Heterobicyclic and Polycyclic N6-Substituents as Adenosine A1 Receptor...Synthesis and Biological Evaluation of Adenosines with Heterobicyclic and Polycyclic N6-Substituents as Adenosine A1 Receptor...

Synthesis and Biological Evaluation of Adenosines with Heterobicyclic and Polycyclic N6-Substituents as Adenosine A1 Receptor ... N6-substituted adenosines are full agonists at A1R and activate this receptor selectively over the other adenosine receptor ... Novel Irreversible Agonists Acting at the A1 Adenosine Receptor, Journal of Medicinal Chemistry, 2016, 59, 24, 11182. CrossRef ... The adenosine A1 receptor (A1R) affinity and potency of these compounds was initially assessed using competitive binding assays ...
more infohttp://onlinelibrary.wiley.com/doi/10.1002/cmdc.201200208/full

ADORA1 / Adenosine A1 Receptor Antibody (Cytoplasmic Domain) for IHC IHC-plADORA1 / Adenosine A1 Receptor Antibody (Cytoplasmic Domain) for IHC IHC-pl

Adenosine A1 Receptor antibody LS-A10 is an unconjugated rabbit polyclonal antibody to Adenosine A1 Receptor (ADORA1) from ... ADORA1, A1 adenosine receptor, A1ar, Adenosine A1 receptor, Adenosine receptor A1, ADO-A1 receptor, RDC7 ... Adenosine A1 Receptor. ADORA1 / Adenosine A1 Receptor is an adenosine receptor that belongs to the G-protein coupled receptor 1 ... Adenosine A1 Receptor antibody LS-A10 is an unconjugated rabbit polyclonal antibody to Adenosine A1 Receptor (ADORA1) from ...
more infohttps://www.lsbio.com/antibodies/anti-adora1-antibody-adenosine-a1-receptor-antibody-cytoplasmic-domain-ihc-ihc-plus-ls-a10/1

Optimization of thermolytic response to A1 adenosine receptor agonists in rats | Journal of Pharmacology and Experimental...Optimization of thermolytic response to A1 adenosine receptor agonists in rats | Journal of Pharmacology and Experimental...

Optimization of thermolytic response to A1 adenosine receptor agonists in rats Message Subject (Your Name) has forwarded a page ... Optimization of thermolytic response to A1 adenosine receptor agonists in rats. Isaac R Bailey, Bernard Laughlin, Lucille Moore ... Optimization of thermolytic response to A1 adenosine receptor agonists in rats. Isaac R Bailey, Bernard Laughlin, Lucille Moore ... Optimization of thermolytic response to A1 adenosine receptor agonists in rats. Isaac R Bailey, Bernard Laughlin, Lucille Moore ...
more infohttp://jpet.aspetjournals.org/content/early/2017/06/26/jpet.117.241315/tab-article-info

Diminished Adenosine A1 Receptor Expression in Pancreatic α-Cells May Contribute to the Pathology of Type 1 Diabetes | DiabetesDiminished Adenosine A1 Receptor Expression in Pancreatic α-Cells May Contribute to the Pathology of Type 1 Diabetes | Diabetes

The adenosine A1 receptor (Adora1) is a G-protein coupled receptor (GPCR) that is involved in maintaining glucose homeostasis ... substituted adenosine analogs and their N6-cycloalkyl derivatives at A1- and A2-adenosine receptors coupled to adenylate ... Absence of adenosine A1 receptors unmasks pulses of insulin release and prolongs those of glucagon and somatostatin. Life Sci ... Activation of adenosine A1 receptors by drugs to lower plasma glucose in streptozotocin-induced diabetic rats. Auton Neurosci ...
more infohttp://diabetes.diabetesjournals.org/content/62/12/4208

Adenosine A1 ReceptorsAdenosine A1 Receptors

immune Adenosine A1 Receptors PIK-294, Rabbit polyclonal to MICALL2 Come cells play an important part in cells restoration and ... immune Adenosine A1 Receptors also known as UNC5CL (protein unc-5 homolog C-like), and play an important role in apoptotic and ... immune Adenosine A1 Receptors Indigo, Rabbit polyclonal to ACYP1. In order to link neural activity with cognitive function ... immune Adenosine A1 Receptors Rabbit Polyclonal to PPP1R7, TAK-960 Due to the highly complicated character of the extracellular ...
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Molecules | Free Full-Text | 5-Chloro-5-deoxy-(±)-ENBA, a Potent and Selective Adenosine A1 Receptor Agonist, Alleviates...Molecules | Free Full-Text | 5'-Chloro-5'-deoxy-(±)-ENBA, a Potent and Selective Adenosine A1 Receptor Agonist, Alleviates...

Our results demonstrated an involvement of adenosine A1 receptor in the amplified nociceptive thresholds and in spinal glial ... Our data suggest a possible use of adenosine A1 receptor agonist in neuropathic pain symptoms. ... a selective A1 adenosine receptor antagonist, without exerting any significant change on the motor coordination or arterial ... a potent and highly selective agonist of human adenosine A1 receptor, on thermal hyperalgesia and mechanical allodynia in a ...
more infohttp://mdpi.com/1420-3049/17/12/13712/xml

Frontiers | Anxiolytic Effect of Exogenous Ketone Supplementation Is Abolished by Adenosine A1 Receptor Inhibition in Wistar...Frontiers | Anxiolytic Effect of Exogenous Ketone Supplementation Is Abolished by Adenosine A1 Receptor Inhibition in Wistar...

... role of the adenosinergic system in the pathomechanism of anxiety we tested whether the inhibition of adenosine A1 receptors ( ... the potential role of the adenosinergic system in the pathomechanism of anxiety we tested whether the inhibition of adenosine ... A1 receptors (A1Rs) influence the anxiolytic effect of the exogenous ketone supplement. As A1Rs may mediate such an effect, in ... A1R, adenosine A1 receptor; A2AR, adenosine A2A receptor; AcAc, acetoacetate; ATP, adenosine triphosphate; βHB, beta- ...
more infohttps://www.frontiersin.org/articles/10.3389/fnbeh.2018.00029/full?utm_source=Email_to_authors_&utm_medium=Email&utm_content=T1_11.5e1_author&utm_campaign=Email_publication&field&journalName=Frontiers_in_Behavioral_Neuroscience&id=338125

New pyrazolo[3,4-b]pyridones as selective A1 adenosine receptor antagonists: synthesis, biological evaluation and molecular...New pyrazolo[3,4-b]pyridones as selective A1 adenosine receptor antagonists: synthesis, biological evaluation and molecular...

Binding affinities of the new compounds were determined for adenosine A, A and A receptors. Compounds and showed good affinity ... has been synthesized as potential A adenosine receptor (A AR) ligands. ... Binding affinities of the new compounds were determined for adenosine A1, A2A and A3 receptors. Compounds 5b and 5g showed good ... New pyrazolo[3,4-b]pyridones as selective A1 adenosine receptor antagonists: synthesis, biological evaluation and molecular ...
more infohttps://pubs.rsc.org/en/Content/ArticleLanding/OB/2005/B502831K

A Comparison of the Antagonist Affinities for the Gi- and Gs-Coupled States of the Human Adenosine A1-Receptor | Journal of...A Comparison of the Antagonist Affinities for the Gi- and Gs-Coupled States of the Human Adenosine A1-Receptor | Journal of...

... conformations of the adenosine A1-receptor in Chinese hamster ovary cells stably expressing the human adenosine A1-receptor and ... Hill KJ, Webber AC, and Hill SJ (2003) A role of protein kinase Cμ in signalling from the human adenosine A1-adenosine receptor ... Indeed, unlike the β2-adrenoceptor, the adenosine A1-receptor is resistant to agonist-induced receptor phosphorylation in CHO- ... we have examined a Gi-coupled receptor (the human adenosine A1-receptor; Libert et al., 1992; Olah and Stiles, 1995; Cordeaux ...
more infohttp://jpet.aspetjournals.org/content/320/1/218

AID 1061869 - Potentiation of CCPA-induced displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cell...AID 1061869 - Potentiation of CCPA-induced displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cell...

DPCPX from human adenosine A1 receptor expressed in CHO cell membranes at 10 uM after 90 mins relative to CCPA-treated control. ...
more infohttps://pubchem.ncbi.nlm.nih.gov/bioassay/1061869

Disinhibition of hippocampal CA3 neurons induced by suppression of an adenosine A1 receptor-mediated inhibitory tonus: Pre- and...Disinhibition of hippocampal CA3 neurons induced by suppression of an adenosine A1 receptor-mediated inhibitory tonus: Pre- and...

Bath application of the highly selective adenosine A1 receptor antagonist 1,3-dipropyl-8-cyclopentylxanthine at concentrations ... Disinhibition of hippocampal CA3 neurons induced by suppression of an adenosine A1 receptor-mediated inhibitory tonus: Pre- and ... Both 1,3-dipropyl-8-cyclopentylxanthine and the adenosine-degrading enzyme adenosine deaminase produced an apparently ... but not with theN-methyl-d-aspartate receptor antagonistd-2-amino-5-phosphonovaleric acid (50/μM), prevented the induction of ...
more infohttps://epub.ub.uni-muenchen.de/6113/

The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and...The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and...

The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and ... The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and ... The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and ... The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and ...
more infohttp://molpharm.aspetjournals.org/content/early/2016/09/28/mol.116.105015
  • Our results demonstrated an involvement of adenosine A 1 receptor in the amplified nociceptive thresholds and in spinal glial and microglial changes occurred in neuropathic pain, without affecting motor coordination or blood pressure. (mdpi.com)
  • Both 1,3-dipropyl-8-cyclopentylxanthine and the adenosine-degrading enzyme adenosine deaminase produced an apparently irreversible depolarization of the membrane potential by about 20 mV. (uni-muenchen.de)
  • The results suggest that adenosine receptors coupled to Gi alpha-3 may provide a site at which modulation of aqueous humor production in the ciliary epithelium occurs via the G protein-adenylyl cyclase pathway. (arvojournals.org)
  • METHODS: Solubilized preparations of adenosine receptors from PE and NPE cell lines were immunoprecipitated with G protein specific antisera 8730 (anti-Gi alpha), 3646 (anti-Gi alpha 1), 1521 (anti-Gi alpha 2), and 1518 (anti-Gi alpha 3), and of adenosine receptor-G protein complexes were detected by the binding of radioactive [3H]DPCPX. (arvojournals.org)
  • A series of ethyl 4-amino-1-(2-chloro-2-phenylethyl)-6-oxo-6,7-dihydro-1 H -pyrazolo[3,4- b ]pyridine-5-carboxylates ( 5a-j ) has been synthesized as potential A 1 adenosine receptor (A 1 AR) ligands. (rsc.org)
  • Background Small studies have indicated that adenosine A 1 receptor antagonists enhance diuresis and may improve renal function in patients with chronic heart failure or AHF. (onlinejacc.org)
  • In addition, an increase in the norepinephrine level was observed, suggesting a role for adenosine as a peripheral nervous system neuromodulator. (mysciencework.com)
  • A concise synthesis of a series of N 6 -substituted adenosines with bicyclo[3.2.ctan-6-yl and polycyclic N 6 -substituents has been developed. (wiley.com)
  • This was true even when the receptor was shown, in the same assay, to exist in two different conformational states coupled to two different G proteins. (aspetjournals.org)
  • The observations with the β-adrenoceptors suggest that the underlying principle on which original receptor classification was based is in need of re-examination. (aspetjournals.org)