Receptor, Adenosine A2A
Receptor, Adenosine A1
Receptor, Adenosine A3
Receptor, Adenosine A2B
Receptors, Adenosine A2
Adenosine A2 Receptor Agonists
Adenosine A2 Receptor Antagonists
Receptors, Purinergic P1
Adenosine A1 Receptor Antagonists
Purinergic P1 Receptor Antagonists
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
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)
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)
Dose-Response Relationship, Drug
Nucleoside Transport Proteins
Receptors, Purinergic P2
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.
8-Bromo Cyclic Adenosine Monophosphate
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
A 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.
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
Adenosine Diphosphate Sugars
Purinergic P2 Receptor Antagonists
Rats, Inbred Strains
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Equilibrative-Nucleoside Transporter 2
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.
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.
Cyclic AMP-Dependent Protein Kinases
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
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.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
A 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.
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.
Analysis of a ubiquitous promoter element in a primitive eukaryote: early evolution of the initiator element. (1/6258)Typical metazoan core promoter elements, such as TATA boxes and Inr motifs, have yet to be identified in early-evolving eukaryotes, underscoring the extensive divergence of these organisms. Towards the identification of core promoters in protists, we have studied transcription of protein-encoding genes in one of the earliest-diverging lineages of Eukaryota, that represented by the parasitic protist Trichomonas vaginalis. A highly conserved element, comprised of a motif similar to a metazoan initiator (Inr) element, surrounds the start site of transcription in all examined T. vaginalis genes. In contrast, a metazoan-like TATA element appears to be absent in trichomonad promoters. We demonstrate that the conserved motif found in T. vaginalis protein-encoding genes is an Inr promoter element. This trichomonad Inr is essential for transcription, responsible for accurate start site selection, and interchangeable between genes, demonstrating its role as a core promoter element. The sequence requirements of the trichomonad Inr are similar to metazoan Inrs and can be replaced by a mammalian Inr. These studies show that the Inr is a ubiquitous, core promoter element for protein-encoding genes in an early-evolving eukaryote. Functional and structural similarities between this protist Inr and the metazoan Inr strongly indicate that the Inr promoter element evolved early in eukaryotic evolution. (+info)
Expression of both P1 and P2 purine receptor genes by human articular chondrocytes and profile of ligand-mediated prostaglandin E2 release. (2/6258)OBJECTIVE: To assess the expression and function of purine receptors in articular chondrocytes. METHODS: Reverse transcriptase-polymerase chain reaction (RT-PCR) was used to screen human chondrocyte RNA for expression of P1 and P2 purine receptor subtypes. Purine-stimulated prostaglandin E2 (PGE2) release from chondrocytes, untreated or treated with recombinant human interleukin-1alpha (rHuIL-1alpha), was assessed by radioimmunoassay. RESULTS: RT-PCR demonstrated that human articular chondrocytes transcribe messenger RNA for the P1 receptor subtypes A2a and A2b and the P2 receptor subtype P2Y2, but not for the P1 receptor subtypes A1 and A3. The P1 receptor agonists adenosine and 5'-N-ethylcarboxamidoadenosine did not change PGE2 release from chondrocytes. The P2Y2 agonists ATP and UTP stimulated a small release of PGE2 that was potentiated after pretreatment with rHuIL-1alpha. PGE2 release in response to ATP and UTP cotreatment was not additive, but release in response to coaddition of ATP and bradykinin (BK) or UTP and BK was additive, consistent with ATP and UTP competition for the same receptor site. The potentiation of PGE2 release in response to ATP and UTP after rHuIL-1alpha pretreatment was mimicked by phorbol myristate acetate. CONCLUSION: Human chondrocytes express both P1 and P2 purine receptor subtypes. The function of the P1 receptor subtype is not yet known, but stimulation of the P2Y2 receptor increases IL-1-mediated PGE2 release. (+info)
Presynaptic action of adenosine on a 4-aminopyridine-sensitive current in the rat carotid body. (3/6258)1. Plasma adenosine concentration increases during hypoxia to a level that excites carotid body chemoreceptors by an undetermined mechanism. We have examined this further by determining the electrophysiological responses to exogenous adenosine of sinus nerve chemoafferents in vitro and of whole-cell currents in isolated type I cells. 2. Steady-state, single-fibre chemoafferent discharge was increased approximately 5-fold above basal levels by 100 microM adenosine. This adenosine-stimulated discharge was reversibly and increasingly reduced by methoxyverapamil (D600, 100 microM), by application of nickel chloride (Ni2+, 2 mM) and by removal of extracellular Ca2+. These effects strongly suggest a presynaptic, excitatory action of adenosine on type I cells of the carotid body. 3. Adenosine decreased whole-cell outward currents at membrane potentials above -40 mV in isolated type I cells recorded during superfusion with bicarbonate-buffered saline solution at 34-36 C. This effect was reversible and concentration dependent with a maximal effect at 10 microM. 4. The degree of current inhibition induced by 10 microM adenosine was voltage independent (45.39 +/- 2. 55 % (mean +/- s.e.m.) between -40 and +30 mV) and largely ( approximately 75 %), but not entirely, Ca2+ independent. 4-Aminopyridine (4-AP, 5 mM) decreased the amplitude of the control outward current by 80.60 +/- 3.67 % and abolished the effect of adenosine. 5. Adenosine was without effect upon currents near the resting membrane potential of approximately -55 mV and did not induce depolarization in current-clamp experiments. 6. We conclude that adenosine acts to inhibit a 4-AP-sensitive current in isolated type I cells of the rat carotid body and suggest that this mechanism contributes to the chemoexcitatory effect of adenosine in the whole carotid body. (+info)
A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AV nodal conduction in guinea-pig. (4/6258)1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-510), and the prototypical calcium channel blocker diltiazem. 2. In the atrial-paced isolated heart, CVT-510 was approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50 = 41 nM) than to increase coronary conductance (EC50 = 200 nM). At concentrations of CVT-510 (40 nM) and diltiazem (1 microM) that caused equal prolongation of S-H interval (approximately 10 ms), diltiazem, but not CVT-510, significantly reduced left ventricular developed pressure (LVP) and markedly increased coronary conductance. CVT-510 shortened atrial (EC50 = 73 nM) but not the ventricular monophasic action potentials (MAP). 3. In atrial-paced anaesthetized guinea-pigs, intravenous infusions of CVT-510 and diltiazem caused nearly equal prolongations of P-R interval. However, diltiazem, but not CVT-510, significantly reduced mean arterial blood pressure. 4. Both CVT-510 and diltiazem prolonged S-H interval, i.e., slowed AV nodal conduction. However, the A1 receptor-selective agonist CVT-510 did so without causing the negative inotropic, vasodilator, and hypotensive effects associated with diltiazem. Because CVT-510 did not affect the ventricular action potential, it is unlikely that this agonist will have a proarrythmic action in ventricular myocardium. (+info)
A new synthesis of 5'-deoxy-8,5'-cyclo-adenosine and -inosine: conformationally-fixed purine nucleosides (nucleosides and nucleotides. XVI). (5/6258)A versatile method for the synthesis of 5'-deoxy-8,5'-cycloadenosine, a conformationally-fixed "anti" type of adenosine, was presented. Irradiation of 2', 3'-O-isopropylidene-5'-deoxy-5'-phenylthioadenosine with 60W Hg vapor lamp afforded 2',3'-O-isopropylidene-5'-deoxy-8,5'-cycloadenosine in high yield. The use of other 5'-alkylthio derivatives also gave the cycloadenosine, though the yields were rather poor. Deacetonation of the cyclocompound with 0.1N HCl gave 5'-deoxy-8,5'-cycloadenosine. The cycloinosine derivative was similarly prepared. The nmr, mass and CD spectra of 5'-deoxy-8,5'-cycloadenosine were given and discussed with the previously reported results. (+info)
End group of naturally terminated and UV lesion terminated T7 in vitro RNA. (6/6258)The 3' terminal nucleosides of RNA transcribed in vitro by E. coli RNA polymerase from T7 DNA and UV irradiated TN DNA were determined. The 3' terminal nucleoside of naturally terminated (t1 termination site) RNA cytidine. In the case of RNA terminated at UV lesions, it is cytidine in 0 per cent of the molecules and adenosine in the remaining 30 per cent. Cytidine trialcohols are labile in high concentrations of KOH and at high temperature and appear to convert to uridine. (+info)
Nucleoside-3'-phosphotriesters as key intermediates for the oligoribonucleotide synthesis. III. An improved preparation of nucleoside 3'-phosphotriesters, their 1H NMR characterization and new conditions for removal of 2-cyanoethyl group. (7/6258)An improved procedure for the transformation of 5'-O-monomethoxytrityl-2'-O-acetyl-3'-phosphates of uridine la, inosine ib and 6-N-benzoyladenosine lc into corresponding 3'/2,2,2-trichloroethyl, 2-cyanoethyl/-phosphates iiaic is reported. H NMR characterization of nucleoside 3'-phosphotriesters is presented. New conditions i.e. anhydrous triethylamine-pyridine treatment have been found for the selective removal of 2-cyanoethyl group from nucleoside 3'-phosphotriesters in the presence of neighbouring 2'-O-acetyl one. (+info)
Electrophysiologic effects of adenosine in patients with supraventricular tachycardia. (8/6258)BACKGROUND: We correlated the electrophysiologic (EP) effects of adenosine with tachycardia mechanisms in patients with supraventricular tachycardias (SVT). METHODS AND RESULTS: Adenosine was administered to 229 patients with SVTs during EP study: atrioventricular (AV) reentry (AVRT; n=59), typical atrioventricular node reentry (AVNRT; n=82), atypical AVNRT (n=13), permanent junctional reciprocating tachycardia (PJRT; n=12), atrial tachycardia (AT; n=53), and inappropriate sinus tachycardia (IST; n=10). There was no difference in incidence of tachycardia termination at the AV node in AVRT (85%) versus AVNRT (86%) after adenosine, but patients with AVRT showed increases in the ventriculoatrial (VA) intervals (13%) compared with typical AVNRT (0%), P<0.005. Changes in atrial, AV, or VA intervals after adenosine did not predict the mode of termination of long R-P tachycardias. For patients with AT, there was no correlation with location of the atrial focus and adenosine response. AV block after adenosine was only observed in AT patients (27%) or IST (30%). Patients with IST showed atrial cycle length increases after adenosine (P<0.05) with little change in activation sequence. The incidence of atrial fibrillation after adenosine was higher for those with AVRT (15%) compared with typical AVNRT (0%) P<0.001, or atypical AVNRT (0%) but similar to those with AT (11%) and PJRT (17%). CONCLUSIONS: The EP response to adenosine proved of limited value to identify the location of AT or SVT mechanisms. Features favoring AT were the presence of AV block or marked shortening of atrial cycle length before tachycardia suppression. Atrial fibrillation was more common after adenosine in patients with AVRT, PJRT, or AT. Patients with IST showed increases in cycle length with little change in atrial activation sequence after adenosine. (+info)
Role of Adenosine A1 Receptors in Modulating Extracellular Adenosine Levels | Journal of Pharmacology and Experimental...
This study demonstrates that three structurally distinct A1 receptor antagonists increase extracellular adenosine levels in two different types of cardiovascular cells, i.e., cardiac fibroblasts and vascular smooth muscle cells, and in two species, rats and humans. The extracellular adenosine responses to A1 receptor antagonists are concentration dependent, and are attenuated by pertussis toxin, a toxin that inactivates inhibitory G proteins, and by AMPCP, an inhibitor of ecto-5′-nucleotidase. This study also demonstrates that augmentation of extracellular adenosine levels attenuates the increase in extracellular adenosine induced by A1 receptor antagonists. Finally, this study shows that the effects of A1receptor antagonists on extracellular adenosine levels develop with a time lag of several hours.. Our working hypothesis is that high-affinity A1receptors detect elevated levels of adenosine in the biophase of the cell surface and engage a signal transduction process that ultimately decreases ...
Chronic exposure to adenosine receptor agonists and antagonists reciprocally regulates the A<sub>1</sub> adenosine receptor...
TY - JOUR. T1 - Chronic exposure to adenosine receptor agonists and antagonists reciprocally regulates the A1 adenosine receptor-adenylyl cyclase system in cerebellar granule cells. AU - Hettinger-Smith, Barbara D.. AU - Leid, Mark. AU - Murray, Thomas F.. PY - 1996/11. Y1 - 1996/11. N2 - Chronic treatment with the adenosine receptor antagonist caffeine evokes an up-regulation of A1 adenosine receptors and increased coupling of the receptor to G proteins in rat brain membranes. However, chronic agonist exposure has not been explored. Primary cultures of cerebellar granule cells were exposed chronically to A1 adenosine receptor agonists and antagonists. Exposure to the A1 adenosine receptor agonist N6-cyclopentyladenosine resulted in (1) a time- and concentration-dependent reduction in the density of receptors labeled by 1,3[3H]dipropyl-8-cyclopentylxanthine, (2) an enhanced ability of guanyl nucleotides to decrease the fraction of A1 adenosine receptor sites displaying high affinity for ...
Alterations in Adenosine Metabolism and Signaling in Patients with Chronic Obstructive Pulmonary Disease and Idiopathic...
Background Adenosine is generated in response to cellular stress and damage and is elevated in the lungs of patients with chronic lung disease. Adenosine signaling through its cell surface receptors serves as an amplifier of chronic lung disorders, suggesting adenosine-based therapeutics may be beneficial in the treatment of lung diseases such as chronic obstructive pulmonary disease (COPD) and idiopathic pulmonary fibrosis (IPF). Previous studies in mouse models of chronic lung disease demonstrate that the key components of adenosine metabolism and signaling are altered. Changes include an up-regulation of CD73, the major enzyme of adenosine production and down-regulation of adenosine deaminase (ADA), the major enzyme for adenosine metabolism. In addition, adenosine receptors are elevated. Methodology/Principal Findings The focus of this study was to utilize tissues from patients with COPD or IPF to examine whether changes in purinergic metabolism and signaling occur in human disease. Results
Adenosine - wikidoc
Intravenously administered adenosine is rapidly cleared from the circulation via cellular uptake, primarily by erythrocytes and vascular endothelial cells. This process involves a specific transmembrane nucleoside carrier system that is reversible, nonconcentrative, and bidirectionally symmetrical. Intracellular adenosine is rapidly metabolized either via phosphorylation to adenosine monophosphate by adenosine kinase, or via deamination to inosine by adenosine deaminase in the cytosol. Since adenosine kinase has a lower Km and Vmax than adenosine deaminase, deamination plays a significant role only when cytosolic adenosine saturates the phosphorylation pathway. Inosine formed by deamination of adenosine can leave the cell intact or can be degraded to hypoxanthine, xanthine, and ultimately uric acid. Adenosine monophosphate formed by phosphorylation of adenosine is incorporated into the high-energy phosphate pool. While extracellular adenosine is primarily cleared by cellular uptake with a ...
NAVER Academic | Physiological and pathophysiological roles of adenosine
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.
Livestock Metabolome Database: Showing metabocard for Adenosine (LMDB00019)
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 ...
Extracellular adenosine as a master regulator of immune cell migration into the central nervous system via induction of CX3CL1 ...
Having the ability to modulate lymphocyte entry into the central nervous system (CNS) would benefit patients with neuroinflammatory diseases. We have previously shown that extracellular adenosine regulates CNS entry of lymphocytes during experimental autoimmune encephalomyelitis (EAE), the animal model for the CNS inflammatory disease multiple sclerosis. For instance, while extracellular adenosine levels are vastly increased following inflammatory cellular damage (from the hydrolysis of released cytoplasimic ATP by CD39 and CD73), mice lacking CD73 or given adenosine receptor (AR) antagonists have significantly reduced CNS lymphocyte entry during EAE. We now show through detailed genetic studies that AR signaling regulates lymphocyte migration into the CNS though induction of CX3CL1, a specialized chemokine that acts as both an adhesion molecule and chemoattractant for lymphocytes, monocytes, and NK cells. We show that AR signaling is necessary and sufficient to induce CNS expression of CX3CL1 ...
Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A2A Adenosine Receptor Agonists ATL193 and...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, both adenosine and dipyridamole produce severe bronchoconstriction when given to asthmatics. Because of its ultrashort half-life, adenosine must be administered by a constant IV infusion.. Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A1, A2B, and A3.5 The discovery of highly selective and relatively short-acting adenosine receptor A2A agonists6-9 has opened the ...
Synthesis and Biological Evaluation of Adenosines with Heterobicyclic and Polycyclic N6-Substituents as Adenosine A1 Receptor...
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 ...
Adenosine receptor antagonists alter the stability of human epileptic GABAA receptors. | IRIS Uniroma1
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 ...
Abstract TP269: Reduction of Human Brain Adenosine Levels Following Remote Ischemic Preconditioning | Stroke
Introduction: Prior studies demonstrate that ischemic preconditioning (IP) alters adenosine metabolism. The significance of this effect is not fully understood, but evidence suggests that reduction in extracellular adenosine may represent use as an alternative fuel. Transformation into AMP/ADP may also replenish intracellular total adenine nucleotides (TAN), improving the potential high-energy phosphate bonds available in cells facing ischemia. In both cases, adenosine supports cell energy requirements and may be a key component of IPs protective mechanisms. There are no previous studies of brain adenosine in human patients undergoing remote IP.. Methods: In adults with aneurysmal subarachnoid hemorrhage (SAH), 3-4 remote IP sessions were conducted on non-consecutive days, 4-12 days after hemorrhage. Each session consisted of 4 5-min cycles of lower extremity blood pressure cuff inflation to 30mmHg above systolic blood pressure, followed by 5-min reperfusion. Patients had microdialysis (MD) ...
Effects of Intravenous and Intracoronary Adenosine 5′-Triphosphate as Compared With Adenosine on Coronary Flow and Pressure...
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 ...
Cardiovascular adenosine receptors: Expression, actions and interactio by John Patrick Headrick, Kevin Ashton et al.
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
Desensitization of A<sub>1</sub> adenosine receptors in rat cerebral...
TY - JOUR. T1 - Desensitization of A1 adenosine receptors in rat cerebral cortex. AU - Park, K. S.. AU - Yang, W. S.. AU - Kim, K. H.. PY - 1996. Y1 - 1996. N2 - Following the subcutaneous administration of R(-)N6-(2-phenylisopropyl)adenosine (600 nmol/kg/hr) to rats for 1 week using Alzet® mini-osmotic pumps, A1 adenosine receptor functions were determined using [3H]DPCPX binding, GTP(γ)S binding, and adenylyl cyclase assays. A1 adenosine receptor binding and the inhibition of adenylyl cyclase activity by PIA was not altered in cerebrocortical membranes prepared from PIA-treated rats. However, there was a significant decrease in the A1 adenosine receptor-mediated stimulation of [35S]GTP(γ)S binding to cerebrocortical membranes prepared from PIA-treated rats (22.0% decrease in basal activity; 19.7% decrease in maximal activity). These results suggest that the desensitization of A1 adenosine receptors following chronic administration involves agonist-induced uncoupling of the receptors ...
Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor | Garvan Institute of Medical...
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
Myocardial adenosine A1-receptor sensitivity during juvenile and adult by Darrell R. Sawmiller, Richard A. Fenton et al.
In the heart, endogenous adenosine attenuates the beta-adrenergic-elicited increase in contractile performance via activation of adenosine A1 receptors. It has been recently reported that this function of adenosine becomes more pronounced with myocardial maturation. The purpose of the present study was to determine whether mature hearts possess a greater sensitivity than immature hearts to this antiadrenergic effect of adenosine. Isolated perfused hearts or atria from immature (ca. 23 days) and mature (ca. 80 days) rats were stimulated with isoproterenol (Iso), a beta-adrenergic agonist, at 10(-8) M and concomitantly exposed to increasing concentrations of 2-chloro-N6-cyclopentyladenosine (CCPA), a highly selective and potent adenosine A1-receptor agonist, from 10(-12) to 10(-6) M. CCPA at 10(-10)-10(-6) M dose dependently reduced the Iso-elicited contractile response more in immature than in mature hearts or atria. At 10(-6) M, CCPA reduced the Iso-elicited contractile response by 103% in immature
Unscramble adenosine | Words unscrambled from letters adenosine | Scrabble Word adenosine | Words Made with the Letters...
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Legere Pharmaceuticals: Oral administration of adenosine is effective for improving metabolic syndrome-related parameters [......
We have demonstrated previously that both acute and chronic oral administration of adenosine have novel functions such as anti-hypertensive effects and improved hyperlipidaemia in stroke-prone spontaneously hypertensive rats (SHRSP) fed a normal diet. The purpose of the present study was to investigate the effect of adenosine administration on metabolic syndrome-related parameters in SHRSP fed a high-fat diet. Six-week-old rats were divided into three groups, and were administered either water (control) or adenosine (10 or 100 mg/l) for 8 weeks. During this period, the rats had free access to a high-fat diet based on AIN-93M. The results showed that hypertension, plasma lipid, NO, insulin, glucose and urinary 8-hydroxy-2-deoxyguanosine levels improved significantly in both adenosine groups. The mRNA expression levels of genes involved in anti-oxidative activity and adenosine receptors were also altered in the adenosine groups. Administration of adenosine also increased plasma adiponectin ...
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 ...
Adenosine receptor - Wikipedia
Each type of adenosine receptor 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 action on all four adenosine receptors in heart tissue, as well as producing a sedative effect through action on A1 and A2A receptors in the brain. Xanthine derivatives ...
Dose-dependent effect of caffeine on adenosine-induced myocardial stress perfusion in Rubidium-82 PET/CT - Alle medarbejdere på...
TY - ABST. T1 - Dose-dependent effect of caffeine on adenosine-induced myocardial stress perfusion in Rubidium-82 PET/CT. T2 - no influence of one cup of coffee on myocardial flow reserve. AU - Byrne, C.. AU - Kjaer, A.. AU - Wissenberg, M.. AU - Hurry, P. K.. AU - Schmedes, A. V.. AU - Forman, J. L.. AU - Hasbak, P.. PY - 2018. Y1 - 2018. U2 - 10.1093/eurheartj/ehy563.3007. DO - 10.1093/eurheartj/ehy563.3007. M3 - Conference abstract in journal. VL - 39. SP - 628. EP - 629. JO - European Heart Journal. JF - European Heart Journal. SN - 0195-668X. IS - suppl. 1. ER - ...
Silk polymer-based adenosine release: Therapeutic potential for epilepsy<...
TY - JOUR. T1 - Silk polymer-based adenosine release. T2 - Therapeutic potential for epilepsy. AU - Wilz, Andrew. AU - Pritchard, Eleanor M.. AU - Li, Tianfu. AU - Lan, Jing Quan. AU - Kaplan, David L.. AU - Boison, Detlev. N1 - Funding Information: This project was supported by grant R01NS058780 from the National Institute of Neurological Disorders and Stroke and by the Epilepsy Research Foundation through the generous support of the Arlene and Arnold Goldstein Family Foundation.. PY - 2008/9. Y1 - 2008/9. N2 - Adenosine augmentation therapies (AAT) make rational use of the brains own adenosine-based seizure control system and hold promise for the therapy of refractory epilepsy. In an effort to develop an AAT compatible with future clinical application, we developed a novel silk protein-based release system for adenosine. Adenosine releasing brain implants with target release doses of 0, 40, 200, and 1000 ng adenosine per day were prepared by embedding adenosine containing microspheres into ...
Welcome to CDC stacks | Regadenoson and adenosine are equivalent vasodilators and are superior than dipyridamole- a study of...
Regadenoson produced higher stress MBF than dipyridamole and adenosine (3.58 ± 0.58 vs. 2.81 ± 0.67 vs. 2.78 ± 0.61 ml/min/g, p = 0.0009 and p = 0.0008 respectively). Regadenoson had a much higher heart rate response than adenosine and dipyridamole respectively (95 ± 11 vs. 76 ± 13 vs. 86 ± 12 beats/ minute) When stress MBF was adjusted for heart rate, there were no differences between regadenoson and adenosine (37.8 ± 6 vs. 36.6 ± 4 μl/sec/g, p = NS), but differences between regadenoson and dipyridamole persisted (37.8 ± 6 vs. 32.6 ± 5 μl/sec/g, p = 0.03). The unadjusted MPR was higher with regadenoson (3.11 ± 0.63) when compared with adenosine (2.7 ± 0.61, p = 0.02) and when compared with dipyridamole (2.61 ± 0.57, p = 0.04). Similar to stress MBF, these differences in MPR between regadenoson and adenosine were abolished when adjusted for heart rate (2.04 ± 0.34 vs. 2.12 ± 0.27, p = NS), but persisted between regadenoson and dipyridamole (2.04 ± 0.34 vs. 1.77 ± 0.33, p = ...
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Novel Role for Adenosine in Circadian Rhythms and Alcohol Use Disorders | Medical Research Archives
In the central nervous system, the nucleoside adenosine regulates neuronal activity by modulating the actions of other neurotransmitter systems, thereby influencing many different physiological processes and behaviors. Adenosinergic mechanisms are especially important in fine-tuning glutamatergic neurotransmission. Astrocytic release of adenosine triphosphate and its subsequent extracellular breakdown provides adenosine to drive homeostatic sleep. Acute ethanol (alcohol) exposure increases extracellular adenosine, which mediates the ataxic and hypnotic/sedative effects of alcohol, while chronic ethanol exposure leads to downregulated adenosine signaling that underlies insomnia, a major predictor of relapse. Adenosine gates glutamatergic input to the circadian clock located in the suprachiasmatic nucleus of the hypothalamus, modulating both photic (light-induced) and nonphotic (behaviorally-induced) synchronization of circadian activity rhythms. A recent study using mice lacking the equilibrative ...
Adenosine modulates cell growth in human epidermoid carcinoma (A431) cells | [email protected]
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 ...
Adenosine Infusion Improves Oxygenation in Term Infants With Respiratory Failure | American Academy of Pediatrics
Objective. Adenosine infusion causes selective pulmonary vasodilation in fetal and neonatal lambs with pulmonary hypertension. We investigated the effects of a continuous infusion of adenosine on oxygenation in term infants with persistent pulmonary hypertension of newborn (PPHN).. Design. A randomized, placebo-controlled, masked trial comparing the efficacy of intravenous infusion of adenosine to normal saline infusion over a 24-hour period.. Setting. Inborn and outborn level III neonatal intensive care units at a university medical center.. Participants. Eighteen term infants with PPHN and arterial postductal Po2 of 60 to 100 Torr on inspired O2 concentration of 100% and optimal hyperventilation (PaCo2 ,30 Torr) were enrolled into the study. Study infants were randomly assigned to receive a placebo infusion of normal saline, or adenosine infusion in doses of 25 to 50 µg/kg/min over a 24-hour period.. Results. Nine infants each received adenosine or placebo. The two groups did not differ in ...
The initial studies to test the hypothesis that adenosine release mediates the anti-inflammatory effects of methotrexate were performed in vitro. In these studies, methotrexate treatment increased adenosine release from cultured endothelial cells and fibroblasts and the adenosine released diminished stimulated neutrophil adhesion to the monolayers of cultured cells (Cronstein et al., 1991). Subsequent in vivo studies confirmed the hypothesis that adenosine mediates the anti-inflammatory effects of methotrexate; pharmacologically relevant doses of methotrexate induce intracellular AICAR accumulation in splenocytes, increase adenosine concentrations in inflammatory exudates, and diminish leukocyte accumulation at an inflamed site (Cronstein et al., 1993). Moreover, the increase in exudate adenosine concentration was responsible for the anti-inflammatory effects of the drug since adenosine receptor antagonists or adenosine deaminase, an enzyme which converts adenosine to the receptor-inactive ...
Differential Expression of Adenosine Receptors in Human Endothelial Cells | Circulation Research
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 ...
Design and synthesis of adenosine receptor antagonists | Department of Chemical and Pharmaceutical Sciences
Adenosine receptors (AR) belong to the G-protein coupled receptor family. There are four receptor subtypes: A1, A2A, A2B e A3. Adenosine receptor subtypes show a different distribution in the organism and are implicated in several physiopathological processes. In particular, antagonists towards A1AR are promising in the treatment of cognitive disorders. A2A antagonists seem to be involved in decrease the neurological impairment observed in Parkinsonâ€™s disease. A2B antagonists are potential therapeutic agents in asthma and diabetes. Finally, antagonists at the A3AR could be implicated in tumor growth inhibition and in glaucoma treatment. The crystallographic structure acquisition of the human A2A receptor allowed the design of new AR antagonists by the help of computational techniques. Our group is focused on the synthesis of new adenosine receptor antagonists (particularly towards A2A and A3) for their potential therapeutic use, but also as tools for pharmacological investigations on ...
Adenosine receptor interactions alter cardiac contractility in rat heart
Summary 1. The effect of the adenosine A2 receptor (AdoA2R) agonist N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)-ethyl]adenosine (DPMA) on adenosine A1 receptor (AdoA1R)-mediated negative inotropic responses was investigated in rat heart. 2. Hearts from male Wistar rats (250-350 g) were perfused with Krebs-Henseleit solution at constant flow in non-recirculating Langendorff mode. Hearts were paced at 5 Hz (5 ms duration, supramaximal voltage) via ventricular electrodes. After 30 min equilibration, (R)-N6-phenylisopropyl adenosine (R-PIA) concentration-response curves were constructed in the absence or presence of DPMA. 3. In paced hearts, R-PIA induced concentration-dependent decreases in triple product (heart rate נpeak systolic developed pressure נdP?/?dtmax), which were significantly attenuated by 1 nmol?/?L DPMA with a shift in pEC50 from 8.0 ᠰ.5 (n = 9) in control hearts to 6.63 ᠱ.03 (n = 5) in treated tissues (P , 0.05). The AdoA2AR antagonist 8-(3-chlorostyryl)caffeine (1 ...
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Modulating P1 Adenosine Receptors in Disease Progression of SOD1G93A Mutant Mice<...
TY - JOUR. T1 - Modulating P1 Adenosine Receptors in Disease Progression of SOD1G93A Mutant Mice. AU - Armida, Monica. AU - Matteucci, Alessandra. AU - Pèzzola, Antonella. AU - Baqi, Younis. AU - Müller, Christa E. AU - Popoli, Patrizia. AU - Potenza, Rosa Luisa. PY - 2019/5. Y1 - 2019/5. N2 - Amyotrophic lateral sclerosis (ALS) is a fatal progressing neurodegenerative disease; to date, despite the intense research effort, only two therapeutic options, with very limited effects, are available. The purinergic system has been indicated as a possible new therapeutic target for ALS, but the results are often contradictory and generally confused. The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. Body weight, motor performance ...
adenosine monophosphate injection
2 Biologic Description. Side effects requiring immediate medical attention. Adverse reactions to Adenosine of any severity reported in less than 1% of patients include: back discomfort, lower extremity discomfort, weakness, myocardial infarction, ventricular arrhythmia, third-degree AV block, bradycardia, palpitation, sinus exit block, sinus pause, T-wave changes, hypertension (systolic blood pressure > 200 mm Hg), drowsiness, emotional instability, tremors, blurred vision, dry mouth, ear discomfort, metallic taste, nasal congestion, scotomas, tongue discomfort. 1. Since Adenosine significantly increases blood flow in normal coronary arteries with little or no increase in stenotic arteries, Adenosine causes relatively less thallium-201 uptake in vascular territories supplied by stenotic coronary arteries i.e., a greater difference is seen after Adenosine between areas served by normal and areas served by stenotic vessels than is seen prior to Adenosine. Do not use in patients with ...
Adenosine Sleep: What Is Adenosine and What Does Adenosine Do?
Adenosine is one of the bodys more powerful molecules and is linked to the digestion process. During digestion, the glucose in the foods we eat breaks down into glycolysis. This breaks down further into Adenosine Tri-Phosphate (ATP). This is responsible for energy transference between cells. After ATP is used up, it decomposes yet again into adenosine. As adenosine builds up in the bloodstream, it interacts with specific cell receptors, inhibiting neural activity and causing drowsiness.. What does this actually mean? Well, when the body runs out of fuel in the form of easily digestible sugars from the food we eat, adenosine signals the body to become drowsy. This essentially tells us to sleep and rebuild our energy reserves. Its a critical chain reaction that initiates the early stages of non-REM sleep and is essential to the natural sleep cycle.. ...
Adenosine regulates CD8 T-cell priming by inhibition of membrane-proximal T-cell receptor signalling
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 ...
Biofyzikální ústav AV ČR
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 ...
Adenosine depresses excitatory but not fast inhibitory synaptic transmission in area CA1 of the rat hippocampus. · NEOMED...
The effects of adenosine on inhibitory synaptic transmission in area CA1 were examined using the rat hippocampal slice preparation and intracellular recording. Adenosine did not change fast inhibitory synaptic potentials (IPSPs) but depressed late IPSPs evoked by direct activation of interneurons in the presence of 6,7-dinitroquinoxaline-2,3-dione (DNQX) and D,L-2-amino-5-phosphonovalerate (APV). Directly activated IPSPs were unchanged by the selective adenosine A1 receptor antagonist 8-cyclopentyltheophylline (CPT), but CPT reversed hyperpolarization and depression of late IPSPs produced by adenosine. These results indicate that adenosine depresses disynaptic IPSPs in area CA1 by decreasing synaptic activation of inhibitory neurons ...
Recent evidence suggests that ethanol initially causes an increase in receptor-dependent cAMP levels, followed by heterologous desensitization of receptors coupled to GS after chronic exposure. Here we investigated the role of adenosine in mediating these responses. We found that ethanol caused accumulation of extracellular adenosine in NG108-15 and S49 lymphoma cells. This adenosine activated adenosine receptors to increase intracellular cAMP levels. The addition of adenosine deaminase, to degrade accumulated extracellular adenosine, or isobutyl-methylxanthine, an adenosine receptor antagonist, completely blocked ethanol-induced increases in cAMP levels in NG108-15 cells. Chronic exposure of NG108-15 and S49 wild type cells to ethanol resulted in heterologous desensitization of adenosine receptor- and prostaglandin E1 receptor-dependent cAMP signal transduction. Coincubation of NG108-15 and S49 wild type cells with adenosine deaminase and ethanol for 48 hr prevented heterologous ...
Treatment with an adenosine uptake inhibitor attenuates glomer...
Treatment with an adenosine uptake inhibitor attenuates glomerulonephritis in mice.: This study evaluated the effects of KF24345 (3-[1-(6,7-diethoxy-2-morpholin
BBA - Molecular Cell Research (v.1823, #4) | www.chemweb.com
Activation of protein kinase C (PKC) via adenosine receptors is known to be involved in the cardioprotection of ischemic preconditioning (IPC). Specifically, activation of PKCε is critical for cardioprotection. There is ample evidence that PKCε resides in cardiac mitochondria. However, the signals that promote translocation of PKCε are largely unknown. The present study was designed to determine whether and how adenosine receptor activation induces translocation of PKCε to mitochondria. Freshly isolated adult rat cardiac myocytes and rat heart-derived H9c2 were used in the study. Immunofluorescence imaging of isolated mitochondria showed that PKCε but not PKCδ was localized in mitochondria and this mitochondrial localization of PKCε was significantly increased by adenosine treatment. The adenosine-induced increase in PKCε-positive mitochondria was largely prevented not only by PKC inhibitor chelerythrine, but also by the HSP90 inhibitor geldanamycin and by siRNA targeting HSP90. ...
Adenosine A3 receptor - Wikipedia
The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during cardiac ischemia, it is involved in the inhibition of neutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death. Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18). Multiple transcript variants encoding different isoforms have been found for this gene. An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of infarction the A3 ...
Spinal Adenosine Receptor Activation Reduces Hypersensitivity after Surgery by a Different Mechanism Than after Nerve Injury |...
In the current study, the combination of T62 and clonidine produced a synergistic interaction in rats with incisional pain. Synergy usually indicates that the two drugs have different final pathways to produce their effect, although other levels of interaction, such as altered drug disposition, can also be responsible. We did not measure tissue concentrations of drugs, so we cannot exclude a pharmacokinetic mechanism of synergy in the current study. Nonetheless, the observation of synergy is somewhat surprising if, as indicated by studies with spinal nerve ligation, the effect of T62 relies entirely on stimulating spinal norepinephrine release, which acts on α2adrenoceptors. One would in that case expect an additive interaction, and intrathecal adenosine and clonidine do interact additively in spinal-ligated rats. 14 In contrast, a synthetic adenosine agonist interacts synergistically with clonidine in acute thermal nociception tests in normal rats. 20 In addition, idazoxan only partially ...
CV Therapeutics and Astellas Announce FDA Approval for Lexiscan(TM) (regadenoson)... ( -First A2A Adenosine Receptor Agoni...)
... -First A2A Adenosine Receptor Agonist Approved for Use as Pharmacolo... Stress Agent in Myocardial Perfusion Imaging- ...PALO ALTO Calif. and DEERFIELD Ill. April 10 FirstCall/...Lexiscan is the first A2A adenosine receptor agonist shown to be safe...,CV,Therapeutics,and,Astellas,Announce,FDA,Approval,for,Lexiscan(TM),(regadenoson),Injection,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
Adenosine 5-diphosphate synonyms, adenosine 5-diphosphate antonyms - FreeThesaurus.com
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?
Adenosine triphosphatase test synonyms, adenosine triphosphatase test antonyms - FreeThesaurus.com
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?
Adenosine Global Industry By End Use, By Region, And Segment Forecasts, 2019 - 2025 - Yamasa , Meihua Group , Tuoxin , ...
The report displayed here plans showcase players to make steady progress while adequately managing one of a kind difficulties in the worldwide Adenosine advertise. The examiners and analysts creating the report have thought about different elements anticipated to emphatically and contrarily sway the worldwide Adenosine advertise. The report incorporates SWOT and PESTLE investigations to give a more profound comprehension of the worldwide Adenosine advertise. The entirety of the main organizations remembered for the report are profiled dependent on net edge, piece of the overall industry, tentative arrangements, late advancements, target client socioeconomics, items and applications, and other basic variables. The report additionally offers local examination of the Adenosine advertise with high spotlight on showcase development, development rate, and development potential. Top Players Considered in Global Builders and Adenosine Market :- , Yamasa, Meihua Group, Tuoxin, Mingxin Pharmaceuticla, ...
Adenosine financial definition of adenosine
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?
ANTAGONIST OF A2B ADENOSINE RECEPTORS FOR ASTHMA | SBIR.gov
DESCRIPTION: (Adapted from the Investigators Abstract): Adenosine administered as an aerosol to asthmatics causes bronchoconstriction, while in non-asthmatics adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells triggers degranulation, releasing histamine, leukotrienes, and other allergic mediators. A2B adenosine receptors are blocked by theophylline, a xanthine that is effective in treating asthma. However, theophylline is a non-selective antagonist of all four adenosine receptor subtypes and produces side effects due primarily to A1 receptor blockade, including insomnia and diuresis. The incidence of asthma is increasing and current treatment options are limited. New drugs that are potent and selective antagonists of A2B adenosine receptors have great potential for the treatment of asthma and other allergic diseases. Adenosine Therapeutics, LLC owns the first potent and selective A2B antagonists. The purpose of this phase I ...
Circulating Adenosine Levels Before and After Intravenous (IV) Persantine - Full Text View - ClinicalTrials.gov
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 ...
Attenuation of chronic pulmonary inflammation in A<sub>2B</sub> adenosine receptor...
TY - JOUR. T1 - Attenuation of chronic pulmonary inflammation in A2B adenosine receptor knockout mice. AU - Zaynagetdinov, Rinat. AU - Ryzhov, Sergey. AU - Goldstein, Anna E.. AU - Yin, Huiyong. AU - Novitskiy, Sergey V.. AU - Goleniewska, Kasia. AU - Polosukhin, Vasiliy V.. AU - Newcomb, Dawn C.. AU - Mitchell, Daphne. AU - Morschl, Eva. AU - Zhou, Yang. AU - Blackburn, Michael R.. AU - Peebles, R. Stokes. AU - Biaggioni, Italo. AU - Feoktistov, Igor. PY - 2010/5/1. Y1 - 2010/5/1. N2 - Pharmacologic evidence suggests that activation of A2B adenosine receptors results in proinflammatory effects relevant to the progression of asthma, a chronic lung disease associated with elevated interstitial adenosine concentrations in the lung. This concept has been challenged by the finding that genetic removal of A2B receptors leads to exaggerated responses in models of acute inflammation. Therefore, the goal of our study was to determine the effects of A2B receptor gene ablation in the context of ...
Gs-Coupled Adenosine Receptors Differentially Limit Antigen-Induced Mast Cell Activation | Journal of Pharmacology and...
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 ...
Effects of chronic adenosine uptake blockade on adrenergic responsiveness and left ventricular chamber function in pressure...
BACKGROUND: Increased sympathetic activity contributes to the progression of heart failure. Adenosine counteracts sympathetic activity by inhibition of presynaptic norepinephrine release and attenuation of the metabolic and contractile responses to beta-adrenergic stimulation. In this study, we tested the hypothesis that the adenosinergic effects (uptake blockade) of dipyridamole may retard the progression of pressure overload hypertrophy in the rat. METHODS AND RESULTS: To verify that the administration of dipyridamole increases myocardial adenosine levels in the rat, epicardial adenosine concentrations were measured from 12 isolated, perfused rat hearts exposed to 10(-7) and 10(-6) mol/l dipyridamole. Adenosine concentrations were increased with both doses of dipyridamole. Also, 9 weeks of dipyridamole treatment resulted in decreased sensitivity to the adenosine A1-receptor agonist, 2-chloro-N6-cyclopentyl adenosine, suggesting that dipyridamole increases adenosine levels in the intact rat. In ...
Repositório Institucional UNIFESP: Acute adenosine increases cardiac vagal and reduces sympathetic efferent nerve activities in...
Adenosine is the first drug of choice in the treatment of supraventricular arrhythmias. While the effects of adenosine on sympathetic nerve activity (SNA) have been investigated, no information is available on the effects on cardiac vagal nerve activity (VNA). We assessed in rats the responses of cardiac VNA, SNA and cardiovascular variables to intravenous bolus administration of adenosine. in 34 urethane-anaesthetized rats, cardiac VNA or cervical preganglionic sympathetic fibres were recorded together with ECG, arterial pressure and ventilation, before and after administration of three doses of adenosine (100, 500 and 1000 mu g kg-1). the effects of adenosine were also assessed in isolated perfused hearts (n= 5). Adenosine induced marked bradycardia and hypotension, associated with a significant dose-dependent increase in VNA (+204 +/- 56%, P , 0.01; +275 +/- 120%, P , 0.01; and +372 +/- 78%, P , 0.01, for the three doses, respectively; n= 7). Muscarinic blockade by atropine (5 mg kg-1, i.v.) ...
Determination of adenosine effects and adenosine receptors in murine corpus cavernosum<...
TY - JOUR. T1 - Determination of adenosine effects and adenosine receptors in murine corpus cavernosum. AU - Tostes, Rita C.. AU - Giachini, Fernanda R.C.. AU - Carneiro, Fernando S.. AU - Leite, Romulo. AU - Inscho, Edward W.. AU - Webb, R. Clinton. PY - 2007/8. Y1 - 2007/8. N2 - This study tested the hypothesis that adenosine, in murine corpora cavernosa, produces direct relaxation of smooth muscle cells and inhibition of contractile responses mediated by sympathetic nerve stimulation. Penes were excised from anesthetized male C57BL/6 mice, dissected, and cavernosal strips were mounted to record isometric force. Adenosine, 2-chloroadenosine (stable analog of adenosine), and 2-phenylaminoadenosine (CV1808) (A2 A/A2B agonist) produced concentration-dependent relaxations of phenylephrine-contracted tissues. Relaxation to 2-chloroadenosine was inhibited, in a concentration-dependent manner, by 2-(2-furanyl)-7-(2- phenylethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine (SCH58261; A2A ...
Medicinal chemistry and pharmacology of A2B adenosine receptors | Pubblicazioni Scientifiche Unicam
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar across species, ranging from 85% identity between human and mouse and 95% identity between rat and mouse. The A2B receptors show a ubiquitous distribution, the highest levels are present in cecum, colon and bladder, followed by blood vessels, lung, eye and mast cells. Through A2B receptors adenosine seems to cause mast cells degranulation, vasodilation, cardiac fibroblast proliferation, inhibition of Tumor Necrosis Factor (TNF-α), increased synthesis of interleukin-6 (IL-6), stimulation of Cl- secretion in intestinal epithelia and hepatic glucose prodn. Hence, A2B adenosine receptor agonists could be useful ...
A Role for Extracellular Adenosine in Time-Dependent Reversal of Long-Term Potentiation by Low-Frequency Stimulation at...
In the present study, we have made some progress in understanding the extracellular adenosine involved in the LFS-induced depotentiation at Schaffer collateral-CA1 synapses. There are four principal observations emerged from this work. First, the time-dependent reversal of LTP by LFS was mimicked by extracellular application of adenosine and was blocked by A1 adenosine receptor antagonist DPCPX but not by A2 receptor antagonist DMPX. Although transient extracellular application of 5-HT1A receptor agonist buspirone after LTP induction could also effectively reverse previously established LTP, 5-HT1A receptor antagonist NAN-190 did not affect the LFS-induced depotentiation. Second, the source of extracellular adenosine during LFS to exert depotentiation appeared to be attributable to the efflux of cAMP that is subsequently converted into adenosine by ecto-5′-nucleotidase. However, the extracellular conversion of ATP is not the major source of adenosine underlying the LFS-induced depotentiation. ...
Uncoupling between ATP overflow and extracellular adenosine formation shifts purinergic signaling | Current Status of Src...
Uncoupling between ATP overflow and extracellular adenosine formation shifts purinergic signaling in post-inflammatory ileitis. small amounts of adenosine discovered in TNBS-treated arrangements, since blockade of Cav3 (T-type) stations existing in ICCs with mibefradil (3 M) or inhibition from the equilibrative nucleoside transporter 1 with dipyridamole (0.5 M), both reduced extracellular adenosine. Data suggest that post-inflammatory ileitis operates a change on purinergic neuromodulation reflecting the upregulation of ATP-releasing enteric glial cells as well as the depletion of ICCs accounting for buy UNC 0224 reduced adenosine overflow via equilibrative nucleoside transporters. = 6) and 0.80 0.09 (= 6) in charge and TNBS-treated samples, respectively (see Number ?Figure5A5A). Negative and positive ideals represent facilitation and inhibition of evoked [3H]ACh launch, respectively. None from the medicines considerably ( 0.05) changed the basal tritium outflow. Open up in another window Number ...
Renal arteriolar angiotensin responses during varied adenosine receptor activation. | Hypertension
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 ...
Dual effect of (-)-N6-phenylisopropyl adenosine on guinea-pig trachea. - Semantic Scholar
The effect of (-)-N6-phenylisopropyl adenosine (PIA), a metabolically stable P1-receptor agonist, was investigated on guinea-pig isolated trachea. PIA showed two opposite effects: contraction, evident at low concentrations (10(-7) to 2-5 X 10(-6) M), and relaxation at higher doses. Relaxation by PIA was antagonized in an apparently competitive manner by two antagonists of extracellular (P1) adenosine receptors: theophylline (Theo) and 8-phenyltheophylline (PT). Contraction by PIA was not inhibited by methylxanthines and was not mediated by stimulation of cholinergic or histaminergic systems. Inhibitors of arachidonic acid cascade acting at different levels, i.e. indomethacin, nordihydroguaiaretic acid (NDGA) and BW755C, all inhibited the contraction by PIA, while they potentiated the relaxation in a concentration-dependent manner. Mepacrine, an inhibitor of phospholipase A2, inhibited the contraction by PIA, but did not affect the relaxation. These results indicate that the contractile effect induced by
Elevated Adenosine Induces Placental DNA Hypomethylation Independent of A2B Receptor Signaling in Preeclampsia | Hypertension
Preeclampsia is a prevalent pregnancy hypertensive disease with both maternal and fetal morbidity and mortality. Emerging evidence indicates that global placental DNA hypomethylation is observed in patients with preeclampsia and is linked to altered gene expression and disease development. However, the molecular basis underlying placental epigenetic changes in preeclampsia remains unclear. Using 2 independent experimental models of preeclampsia, adenosine deaminase-deficient mice and a pathogenic autoantibody-induced mouse model of preeclampsia, we demonstrate that elevated placental adenosine not only induces hallmark features of preeclampsia but also causes placental DNA hypomethylation. The use of genetic approaches to express an adenosine deaminase minigene specifically in placentas, or adenosine deaminase enzyme replacement therapy, restored placental adenosine to normal levels, attenuated preeclampsia features, and abolished placental DNA hypomethylation in adenosine deaminase-deficient ...
Comparison of adenosine and exercise thallium-201 single-photon emission computed tomography (SPECT) myocardial perfusion...
Pharmacologic stress with dipyridamole has provided useful diagnostic, as well as prognostic, information in patients undergoing thallium-201 myocardial perfusion imaging. With its ultrashort half-life and a potent and consistent vasodilator effect, adenosine may be the coronary vasodilator of choice with myocardial perfusion imaging.. Fifty-one healthy subjects and 93 patients with suspected coronary artery disease constituted the study group. In this multicenter study the comparative safety and diagnostic efficacy of single-photon emission computed tomography (SPECT) thallium imaging during adenosine-induced coronary hyperemia was compared with exercise treadmill stress. There was a mean increase in heart rate of 37% and a mean decrease in diastolic blood pressure of 5% during the adenosine infusion of 140 μg/kg per min for 6 min. Adenosine infusion was well tolerated in 95% of the subjects. Side effects requiring intervention occurred in seven subjects (5%). None of the subjects experienced ...
Uneven distribution of nucleoside transporters and intracellular enzymatic degradation prevent transport of intact [ 14 C]...
Efflux transport of adenosine across the choroid plexus (CP) epithelium might contribute to the homeostasis of this neuromodulator in the extracellular fluids of the brain. The aim of this study was to explore adenosine transport across sheep CP epithelial cell monolayers in primary culture. To explore transport of adenosine across the CP epithelium, we have developed a method for primary culture of the sheep choroid plexus epithelial cells (CPEC) on plastic permeable supports and analysed [14C] adenosine transport across this cellular layer, [14C] adenosine metabolism inside the cells, and cellular uptake of [14C] adenosine from either of the chambers. The primary cell culture consisted of an enriched epithelial cell fraction from the sheep fourth ventricle CP and was grown on laminin-precoated filter inserts. CPEC grew as monolayers forming typical polygonal islands, reaching optical confluence on the third day after the seeding. Transepithelial electrical resistance increased over the time after
Release of adenosine and its metabolites from activated human leucocytes | Clinical Science | Portland Press
1. Human leucocytes whose adenine nucleotide pool was prelabelled with [3H]adenine were investigated for their capacity to release adenosine and its metabolites and histamine when activated with the calcium ionophore A23187, antiimmunoglobulin E and the chemotactic peptide N-formyl-methionyl-leucyl-phenylalanine (f-MLP).. 2. Sixty-nine per cent of the 3H-label assimilated by the cells was incorporated into their adenine nucleotide pool in the ratio adenosine 5′-phosphate (AMP):adenosine 5′-pyrophosphate (ADP):adenosine 5′-triphosphate (ATP), 3:1:1. Spontaneous release of label from leucocytes plateaued at 5 min at 22.1 ± 4.2% of the total radiolabel incorporated and mainly consisted of hypoxanthine, inosine and adenosine.. 3. Activation of cells with the calcium ionophore A23187 (1.0 μmol/l) caused a net increase in [3H]purine release above baseline of 27.9 ± 4.6% accompanied by a net basophil histamine release of 46.6 ± 9.4%. A23187 (1.0-3.0 μmol/l) caused a parallel ...
Vasoactivity of adenosine in the trout (Oncorhynchus mykiss) coronary system: involvement of nitric oxide and interaction with...
A vasoconstrictory response to adenosine has been reported in coronary rings from fish. Since the reactivity of the large coronary arteries and the microcirculation may differ, the present study was undertaken to determine the role of adenosine in the intact coronary system of trout under constant pressure or flow using an isolated and non-working heart preparation. The involvement of nitric oxide (NO) and the interaction with noradrenaline were also studied. At 10(-9) to 10(-8 )mol l-1, adenosine caused a vasoconstrictory response, whereas between 10(-7) and 10(-5 )mol l-1 the response was predominantly vasodilative. Theophylline abolished both these responses to adenosine. The vasodilation induced by adenosine (at 10(-5 )mol l-1) was significantly reduced when the preparation was perfused under constant-flow than rather under constant-pressure conditions. The nitric oxide synthase inhibitor N-nitro-l-arginine (l-NA, 10(-4 )mol l-1) partially reduced the vasodilation induced by adenosine (at ...
Comparison of the inhibition of insulin release by activation of adenosine and α2-adrenergic receptors in rat β-cells |...
Rat islets were used to compare the mechanisms whereby adenosine and adrenaline inhibit insulin release. Adenosine (1 microM-2.5 mM) and its analogue N6(-)-phenylisopropyladenosine (L-PIA) (1 nM-10 microM) caused a concentration-dependent but incomplete (45-60%) inhibition of glucose-stimulated release. L-PIA was more potent than D-PIA [the N6(+) analogue], but much less than adrenaline, which caused nearly complete inhibition (85% at 0.1 microM). 8-Phenyltheophylline prevented the inhibitory effect of L-PIA and 50 microM-adenosine, but not that of 500 microM-adenosine or of adrenaline. In contrast, yohimbine selectively prevented the inhibition by adrenaline. Adenosine and L-PIA thus appear to exert their effects by activating membrane A1 receptors, whereas adrenaline acts on alpha 2-adrenergic receptors. Adenosine, L-PIA and adrenaline slightly inhibited 45Ca2+ efflux, 86Rb+ efflux and 45Ca2+ influx in glucose-stimulated islets. The inhibition of insulin release by adenosine or L-PIA was ...
A new procedure for haptenizing adenosine leading to a more specific radioimmunoassay method | Biochemical Journal
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 ...
The Adenosine Receptor and Serum Deprivation-Induced Neuronal Differentiation
Adenosine is a multi-functional physiological molecule found abundantly in the body. It is one of the important components of ATP cellular energy metabolism. Adenosine has diverse actions as a ligand on many different types of cells and tissues acting via specific receptors. Currently, four subtypes of adenosine receptors are described, namely, the A1, A2A, A2B and A3 receptors. Neuroblastoma, mostly found in young children, is a malignant tumor derived from peripheral neurons in the body. Several different types of neuroblastoma cell lines of human origin have been established and contributed to the studies of neuroblastoma itself, neuronal differentiation, neurotransmitters, alcoholism, Alzheimers disease and other neuronal diseases and disorders. In 1987, it was shown by Abbracchio et al. that a human neuroblastoma cell line, IMR32, could be induced to differentiate into cells that have a more neuronal morphology, with long neurites, by an adenosine receptor agonist ...
Heart failure: A1 Adenosine Antagonists for Heart Failure - wikidoc
August 20, 2007 By Grendel Burrell, M.D.  Preliminary results of the Phase 2, 50-patient, of BG9928 (ADENTRI®), an A1 adenosine receptor antagonist in stable patients with heart failure were reported in 2003 at the American Heart Associations annual scientific session. Dr. Barry Greenberg, professor of medicine and director of the Advanced Heart Failure Program at University of California, San Diego Medical Center, and colleagues reported the results in the August 14, 2007, issue of the Journal of the American College of Cardiology, in an article titled Effects of Multiple Oral Doses of an A1 Adenosine Antagonist, BG9928, in Patients With Heart Failure: Results of a Placebo-Controlled, Dose-Escalation Study (J Am Coll Cardiol, 2007; 50:600-606, doi:10.1016/j.jacc.2007.03.059 (Published online 29 July 2007)). BG9928 is a selective inhibitor of the A1 adenosine receptor. The objective of the study was to assess the pharmacokinetics and pharmacologic effects of BG9928 (ADENTRI®) in heart ...
Evidence for increased dorsal hippocampal adenosine release and metabolism during pharmacologically induced seizures in rats<...
TY - JOUR. T1 - Evidence for increased dorsal hippocampal adenosine release and metabolism during pharmacologically induced seizures in rats. AU - Berman, Robert F. AU - Fredholm, Bertil B.. AU - Aden, Ulrika. AU - OConnor, William T.. PY - 2000/7/28. Y1 - 2000/7/28. N2 - There is growing pharmacological evidence from several animal models of seizure disorder that adenosine possesses endogenous anticonvulsant activity. In order to further evaluate the role of adenosine in seizure activity, we monitored adenosine and its major biochemical metabolites inosine, xanthine, and hypoxanthine in the dorsal hippocampus by in vivo microdialysis before and during the induction of generalized seizures. Seizures were induced pharmacologically in groups of urethane-anesthetized rats by the administration of bicuculline (0.5 mg/kg, i.v.), kainic acid (12.0 mg/kg, i.v.) or pentylenetetrazol (100-250 mg/kg, i.p). Seizure activity was monitored electrophysiologically from the dorsal hippocampus. Dialysate ...
A.sub.2B adenosine receptor antagonists - Patent # 7125993 - PatentGenius
Disclosed are processes for the synthesis of novel compounds that are A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound of the formula (3): ##STR00002##
Adenosine hydrolase | definition of adenosine hydrolase by Medical dictionary
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Adenosine 5-diphosphate | definition of adenosine 5-diphosphate by Medical dictionary
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OPUS Würzburg | Search
The actions of adenosine on histamine release of human lung fragments were investigated. Histamine release was stimulated either with the calcium ionophore A 23187 orwith concanavalin A. Adenosine and its analogue 5-N-ethylcarboxamidoadenosine alone had no significant effect on basal release or on the release elicited by A 23187 or concanavalin A. However, in the presence of the adenosine receptor antagonist 8-[4-[[[[(2-aminoethyl)amino]-carbonyl] methyloxy]-phenyl]-1,3-dipropylaxanthine (XAC), which itself did not affect the release, adenosine increased the stimulated histamine release. On the other hand, in the presence of the nucleoside transport inhibitor S-(p-nitrobenzyl)-6-thioninosine (NBTI), adenosine caused a reduction in stimulated histamine release. NBTI itself caused a stimulation of release. Thus, a stimulatory effect of adenosine was seen in the presence ofXAC, whereas an inhibitory effect was unmasked by NBTI. From these data it is concluded that adenosine exerts two opposing ...
OPUS Würzburg | Search
The actions of adenosine on histamine release of human lung fragments were investigated. Histamine release was stimulated either with the calcium ionophore A 23187 orwith concanavalin A. Adenosine and its analogue 5-N-ethylcarboxamidoadenosine alone had no significant effect on basal release or on the release elicited by A 23187 or concanavalin A. However, in the presence of the adenosine receptor antagonist 8-[4-[[[[(2-aminoethyl)amino]-carbonyl] methyloxy]-phenyl]-1,3-dipropylaxanthine (XAC), which itself did not affect the release, adenosine increased the stimulated histamine release. On the other hand, in the presence of the nucleoside transport inhibitor S-(p-nitrobenzyl)-6-thioninosine (NBTI), adenosine caused a reduction in stimulated histamine release. NBTI itself caused a stimulation of release. Thus, a stimulatory effect of adenosine was seen in the presence ofXAC, whereas an inhibitory effect was unmasked by NBTI. From these data it is concluded that adenosine exerts two opposing ...
A1 adenosine receptors potently regulate heart rate in mammalian embryos<...
TY - JOUR. T1 - A1 adenosine receptors potently regulate heart rate in mammalian embryos. AU - Hofman, Paul L.. AU - Hiatt, Kelly. AU - Yoder, Mervin. AU - Rivkees, Scott A.. PY - 1997. Y1 - 1997. N2 - A1 adenosine receptors (A1ARs) have been recently shown to be expressed in rodent embryonic hearts at very early stages of development. To determine the functional significance of fetal cardiac A1AR expression during embryogenesis, murine fetal heart preparations were studied between postconceptual days 9 and 12. Dose-response curves generated using a variety of adenosine agonists revealed that A1AR activation potently regulated fetal heart rates. The A1AR agonist, N6-cyclopentyladenosine, inhibited heart rates in a dose-dependent manner (half-maximal effective concentration = 3.6 x 10-8M) and stopped fetal cardiac contractions in 63% of preparations. In contrast, A2a and A2b receptor activation did not alter heart rates, and activation of A3 receptors produced modest declines in heart rates. ...
Adenosine Receptors as Novel Targets for the Treatment of Various Cancers | Bentham Science
Title:Adenosine Receptors as Novel Targets for the Treatment of Various Cancers. VOLUME: 25 ISSUE: 26. Author(s):Bapi Gorain, Hira Choudhury*, Gan Sook Yee and Subrat Kumar Bhattamisra*. Affiliation:School of Pharmacy, Faculty of Health and Medical Science, Taylors University, Subang Jaya, Selangor, Department of Pharmaceutical Technology, School of Pharmacy, International Medical University, Bukit Jalil 57000, Kuala Lumpur, Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil 57000, Kuala Lumpur, Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil 57000, Kuala Lumpur. Keywords:Adenosine, adenosine receptors, receptor modulators, cancer, signalling pathways, tumour cell.. Abstract:Adenosine is a ubiquitous signaling nucleoside molecule, released from different cells within the body to act on vasculature and immunoescape. The physiological action on the proliferation of tumour cell has been reported by the ...
Ontogenetic profile of the adenosine uptake sites in rat forebrain. - Semantic Scholar
The ontogenesis of rat forebrain adenosine uptake sites labelled by [3H]nitrobenzylthioinosine ([3H]NBI) was determined and compared to that of rat forebrain adenosine receptors labelled by N6-cyclohexyl[3H]adenosine ([3H]-CHA). [3H]NBI binding is highly invariant with similar levels of [3H]NBI binding sites from embryonic day 19 to day 30 postpartum. Scatchard and Hill analyses reveal the binding of [3H]NBI in 6-day-old tissue to be indistinguishable from such binding in 30-day-old tissue. In contrast, [3H]-CHA binding is highly variant. [3H]CHA binding develops slowly but steadily from about embryonic day 19, with adult binding levels being achieved at around 25 days postpartum. The ontogenetic profile of [3H]CHA appears to coincide with synaptogenesis whereas that of [3H]NBI does not.
High dose adenosine stress perfusion cardiovascular magnetic resonance (CMR) imaging for detection of coronary artery disease |...
We prospectively recruited from 1230 consecutive patients undergoing CMRP. First pass CMRP was performed on a Philips Achieva CV 1.5 T MR scanner (Philips, The Netherlands), with standardised acquisition protocol with standard dose adenosine (SDA) at 140 µg/kg/min for 3 minutes. 3 short axis slices of 10 mm thickness were acquired per cardiac cycle using a single shot prospectively gated balanced TFE sequence (TR 2.5 ms, TE 1.3 ms, Flip angle 50° and voxel size 2.8 × 2.8 mm2) after the administration of a 0.1 mmol/Kg bolus of intravenous Gadolinium. Heart rate (HR) and blood pressure (BP) were recorded at baseline and during stress. Non responders were defined as those patients with a normal CMRP scan and blunted haemodynamic response (maximum HR increase ,10 beats per minute and fall in systolic BP (SBP) ,10 mmHg). CMRP in this group was then repeated with high dose adenosine (HDA) at 175 µg/kg/min for 3 minutes. CMRP images were interpreted by 2 independent experienced observers. Coronary ...
tRNA threonylcarbamoyladenosine biosynthesis protein elisa and antibody
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Contribution of Adenosine A<sub>2A</sub> and A<sub>2B</sub> Receptors to Ischemic Coronary Dilation: Role of K<sub>V</sub...
TY - JOUR. T1 - Contribution of Adenosine A2A and A2B Receptors to Ischemic Coronary Dilation. T2 - Role of KV and KATP Channels. AU - Berwick, Zachary C.. AU - Payne, Gregory A.. AU - Lynch, Brandon. AU - Dick, Gregory M.. AU - Sturek, Michael. AU - Tune, Johnathan D.. PY - 2010/11/1. Y1 - 2010/11/1. N2 - This study was designed to elucidate the contribution of adenosine A2A and A2B receptors to coronary reactive hyperemia and downstream K+ channels involved. Coronary blood flow was measured in open-chest anesthetized dogs. Adenosine dose-dependently increased coronary flow from 0.72 ± 0.1 to 2.6 ± 0.5 mL/minute/g under control conditions. Inhibition of A2A receptors with SCH58261 (1 μm) attenuated adenosine-induced dilation by ~50%, while combined administration with the A2B receptor antagonist alloxazine (3 μm) produced no additional effect. SCH58261 significantly reduced reactive hyperemia in response to a transient 15 second occlusion; debt/repayment ratio decreased from 343 ± 63 to ...
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Adenosine and A2A Receptors in Human Brown Adipose Tissue - Full Text View - ClinicalTrials.gov
Adenosine is a purine nucleoside released locally in BAT when noradrenaline and ATP are released from sympathetic nerves. Recently it was found that adenosine activates murine and human brown adipocytes, and recruits beiging of white fat via adenosine A2A receptors (A2AR). Furthermore, studies with mice have shown improvements in glucose homeostasis after administration of A2AR agonists.. In this study the investigators use the PET radiotracer [15O]-H2O to quantify perfusion of BAT, white adipose tissue (WAT) and muscle in three conditions: room temperature, cold exposure and intravenous infusion of adenosine. Another PET radiotracer [11C]TMSX is used to quantify adenosine A2A receptor density of BAT, WAT and muscle in room temperature and during cold exposure. ...
Selective adenosine A2Areceptor agonists and antagonists protect against spinal cord injury through peripheral and central...
Permanent functional deficits following spinal cord injury (SCI) arise both from mechanical injury and from secondary tissue reactions involving inflammation. Enhanced release of adenosine and glutamate soon after SCI represents a component in the sequelae that may be responsible for resulting functional deficits. The role of adenosine A2A receptor in central ischemia/trauma is still to be elucidated. In our previous studies we have demonstrated that the adenosine A2A receptor-selective agonist CGS21680, systemically administered after SCI, protects from tissue damage, locomotor dysfunction and different inflammatory readouts. In this work we studied the effect of the adenosine A2A receptor antagonist SCH58261, systemically administered after SCI, on the same parameters. We investigated the hypothesis that the main action mechanism of agonists and antagonists is at peripheral or central sites. Spinal trauma was induced by extradural compression of SC exposed via a four-level T5-T8 laminectomy in mouse.
Adenosine 5′-triphosphate (ATP) Assay Kit Market 2020 Regional Landscape, Production, Sales & Consumption Status and Prospects...
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3-Deazaneplanocin A (DZNep) hydrochloride|SAHH and ENZ2 inhibitor|CAS# 120964-45-6
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Effect of Intravenous Dipyridamole on Cerebral Blood Flow in Humans | Stroke
Although dipyridamole produces coronary vasodilation, most reports on dipyridamole effects in animals have failed to show a change in CBF after intravenous infusion of dipyridamole.16 17 18 19 To our knowledge, this is the first study to quantitatively estimate the change in CBF in response to intravenous dipyridamole in humans. We found CBF values for the dipyridamole stress to be lower than those at rest (Table 2⇑ and Figure 2⇑). Dipyridamole stress also caused a significant reduction in Paco2 (Table 1⇑), and the vascular response to Paco2 change caused by the dipyridamole infusion closely followed the response due to hypocapnia (Table 2⇑ and Figure 1⇑). Thus, the decrease in CBF during dipyridamole stress can be explained by the decrease in Paco2 rather than the direct action of dipyridamole on CBF. The decrease in Paco2 during dipyridamole stress is most likely due to the hyperventilation side effect of adenosine.29 It has been reported that large doses of intravenous adenosine and ...
CAS 38594-96-6 (-)-N6-(2-PHENYLISOPROPYL)-ADENOSINE - BOC Sciences
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The role of ATP and adenosine in the control of hepatic blood flow in the rabbit liver in vivo | Comparative Hepatology | Full...
The role of adenosine and ATP in the regulation of hepatic arterial blood flow in the buffer response was studied in vitro and in a new in vivo model in the rabbit. The model achieves portal-systemic diversion by insertion of a silicone rubber prosthesis between the portal vein and inferior vena cava and avoids alterations in systemic haemodynamics. Hepatic arterial (HA) blood flow increased in response to reduced portal venous (PV) blood flow, the buffer response, from 19.4 (3.3) ml min-1 100 g-1 to 25.6 (4.3) ml min-1 100 g-1 (mean (SE), p | 0.05, Students paired t-test). This represented a buffering capacity of 18.7 (5.2) %. Intra-portal injections of ATP or adenosine (1 micrograms kg-1-0.5 mg kg-1) elicited immediate increases in HA blood flow to give -log ED50 values of 2.0 and 1.7 mg kg-1 for ATP and adenosine respectively. Injection of ATP and adenosine had no measurable effect on PV flow. In vitro, using an isolated dual-perfused rabbit liver preparation, the addition of 8
Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ... Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ... adenosine; hypoxia and Akt-induced stem cell factor; ROS generated via pharmacologic activation of the mitochondrial potassium- ...
Adenosine triphosphate is a major "energy currency" of the cell. The high energy bonds between the phosphate groups can be ... ISBN 978-3-642-33430-6. Agteresch, Hendrik J.; Dagnelie, Pieter C.; van den Berg, J Willem; Wilson, J H. (1999). "Adenosine ...
Nave CR (2005). "Adenosine Triphosphate". Hyper Physics [serial on the Internet]. Georgia State University. Douglass JG, Patel ... Regrelor was synthesized from adenosine diphosphate (ADP), an endogenous chemical involved in metabolism. The authors noted ...
"ATP: Adenosine Triphosphate , Boundless Biology". courses.lumenlearning.com-US. Retrieved 2017-11-12. Carvalho AT, Szeler K, ... For example, dATP stands for deoxyribose adenosine triphosphate. NTPs are the building blocks of RNA, and dNTPs are the ...
Kielley WW (1961). "Myosin adenosine triphosphatase". In Boyer PD, Lardy H, Myrbäck K (eds.). The Enzymes. Vol. 5 (2nd ed.). ... Wikimedia Commons has media related to Adenosine triphosphatases. "ATP synthase - a splendid molecular machine" ATPase at the ... Martin SS, Senior AE (November 1980). "Membrane adenosine triphosphatase activities in rat pancreas". Biochimica et Biophysica ... "The membrane-bound copper transporting adenosine triphosphatase (Cu-ATPase), which selectively binds copper ions, transports ...
... acts by blocking binding of adenosine to the adenosine A1 receptor, which enhances release of the neurotransmitter ... When caffeine is consumed, it antagonizes adenosine receptors; in other words, caffeine prevents adenosine from activating the ... an agent that reduces the effects of adenosine). The caffeine molecule is structurally similar to adenosine, and is capable of ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ...
"Adenosine-5'-phosphosulfate". pubchem.ncbi.nlm.nih.gov. Retrieved 2022-07-14. (CS1 German-language sources (de), CS1: long ... In biochemistry, metabolism of sulfate may use such a group, for example with adenosine-5'-phosphosulfate. Frost, Ray L.; ...
Equilibrative nucleoside transporter family
hENT4 is uniquely selective for adenosine, and also transports a variety of organic cations. The generalized transport reaction ... Noji T, Karasawa A, Kusaka H (Jul 2004). "Adenosine uptake inhibitors". European Journal of Pharmacology. 495 (1): 1-16. doi: ... They are blocked by adenosine reuptake inhibitors like dipyridamole and dilazep, drugs used clinically for their vasodilatory ... By regulating the concentration of adenosine available to cell surface receptors, mammalian ENTs additionally influence ...
Adenosine receptors are thought to be a large driver of drowsiness and sleep, and their action increases with extended ... Caffeine is an adenosine receptor antagonist, and only indirectly increases catecholamine transmission in the brain. Pitolisant ... Caffeine has been found to increase striatal dopamine in animal models, as well as inhibit the inhibitory effect of adenosine ... Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). "Oligomerization of adenosine A2A and dopamine D2 receptors in living ...
The product is adenosine diphosphate (ADP) and an inorganic phosphate (Pi). ADP can be further hydrolyzed to give energy, ... "ATP: Adenosine Triphosphate". cnx.org. Retrieved 2018-05-16. Wackerhage, H.; Hoffmann, U.; Essfeld, D.; Leyk, D.; Mueller, K.; ... adenosine monophosphate (AMP), and another inorganic phosphate (Pi). ATP hydrolysis is the final link between the energy ... catabolic reaction process by which chemical energy that has been stored in the high-energy phosphoanhydride bonds in adenosine ...
... 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 ... These two ... "Adenosine-cannabinoid receptor interactions. Implications for striatal function". Br. J. Pharmacol. 160 (3): 443-453. doi: ... can be differentiated by their output connectivity and their expression of dopamine and adenosine receptors and neuropeptides. ...
Other names in common use include ADP ribose phosphorylase, and adenosine diphosphoribose phosphorylase. Evans WR, San Pietro A ... Stern AI, Avron M (1966). "An adenosine 5'-diphosphate ribose:orthophosphate adenylyltransferase from Euglena gracilis". ... 1966). "Phosphorolysis of adenosine diphosphoribose". Arch. Biochem. Biophys. 113 (1): 236-44. doi:10.1016/0003-9861(66)90178-0 ...
Adenosine is very relevant in bone metabolism, as it plays a role in formation and activation of both osteoclasts and ... Adenosine acts by binding to purinergic receptors and influencing adenylyl cyclase activity and the formation of cAMP and PKA ... Then, it converts adenosine triphosphate into cyclic AMP, which activates Protein kinase A. PKA leads to protein tyrosine ... There are two main types of purinergic receptors, P1 binding to adenosine, and P2 binding to ATP or ADP, presenting different ...
... and express the peptide enkephalin and a high density of dopamine D2 and adenosine A2A receptors (they also express adenosine ... In contrast, the D2-type medium spiny neurons in the NAcc shell which express adenosine A2A receptors have no role in ... Ferré S, Lluís C, Justinova Z, Quiroz C, Orru M, Navarro G, Canela EI, Franco R, Goldberg SR (June 2010). "Adenosine- ... The indirect pathway (i.e., D2-type) neurons in the NAcc core which co-express adenosine A2A receptors activation-dependently ...
This pathway consists of MSNs that express dopamine receptor D2, muscarinic acetylcholine receptor M1, and adenosine receptor ... and adenosine receptor A1. The direct pathway has been proposed to facilitate motor actions, timing of motor actions, gating of ... "Adenosine-cannabinoid receptor interactions. Implications for striatal function". British Journal of Pharmacology. 160 (3): 443 ...
Kline LK, Fittler F, Hall RH (1969). "N6-(Δ2-isopentenyl)adenosine. Biosynthesis in transfer ribonucleic acid in vitro". ...
PPi is pyrophosphate APS is adenosine 5-phosphosulfate; ATP is adenosine triphosphate; O2 is oxygen molecule; AMP is adenosine ... This incorporation releases pyrophosphate (PPi). ATP sulfurylase converts PPi to ATP in the presence of adenosine 5´ ... and with the substrates adenosine 5´ phosphosulfate (APS) and luciferin. The addition of one of the four deoxynucleotide ...
... increased adenosine receptor function; increased cortisol. In the central nervous system (CNS), the major mediators of the ...
Nucleic acid metabolism
The nucleoside, adenosine, is then deaminated and hydrolyzed to form hypoxanthine via adenosine deaminase and nucleosidase ... "Adenosine deaminase (ADA) deficiency". Learn.Genetics. Archived from the original on 3 November 2014. Retrieved 31 October 2014 ... IMP is then converted to AMP (adenosine monophosphate) using GTP and aspartate, which is converted into fumarate. While IMP can ... Adenylate kinase is a specific nucleoside-monophosphate kinase that functions only on adenosine-monophosphate. Carbohydrate ...
Ghosh HP, Preiss J (1966). "Adenosine diphosphate glucose pyrophosphorylase. A regulatory enzyme in the biosynthesis of starch ... I. Purification and properties of the adenosine diphosphoglucose pyrophosphorylase of Arthrobacter species NRRL B1973". J. Biol ... Other names in common use include ADP glucose pyrophosphorylase, glucose 1-phosphate adenylyltransferase, adenosine diphosphate ... glucose pyrophosphorylase, adenosine diphosphoglucose pyrophosphorylase, ADP-glucose pyrophosphorylase, ADP-glucose synthase, ...
Medium spiny neuron
... and express the peptide enkephalin and a high density of dopamine D2 and adenosine A2A receptors (they also express adenosine ... adenosine A1 receptors, dynorphin peptides, and substance P peptides. Indirect pathway MSNs inhibit their output structure and ... and express the peptides dynorphin and substance P and dopamine D1 and adenosine A1 but not A2A receptors (Ferréet al., 1997; ... "Adenosine-cannabinoid receptor interactions. Implications for striatal function". Br. J. Pharmacol. 160 (3): 443-453. doi: ...
Histidine biosynthesis is carefully regulated by feedback inhibition/ R5P can be converted to adenosine diphosphate ribose, ... Evans WR, San Pietro A (January 1966). "Phosphorolysis of adenosine diphosphoribose". Archives of Biochemistry and Biophysics. ... Adenosine triphosphate). Formation of each molecule is controlled by the flow of glucose 6-phosphate (G6P) in two different ...
Adenosine activates adenosine receptors. The word purine (pure urine) was coined by the German chemist Emil Fischer in 1884. He ... and adenosine monophosphate (AMP). In order to perform these essential cellular processes, both purines and pyrimidines are ... adenosine) with ribose moiety. These nucleosides with phosphoric acid form corresponding nucleotides (deoxyguanylate, ...
List of OMIM disorder codes
APC Adenosine deaminase deficiency, partial; 102700; ADA Adenosine triphosphate, elevated, of erythrocytes; 102900; PKLR ...
Nagata N, Urade Y (2012). "[Sleep-wake regulation by prostaglandin D2 and adenosine]". Brain Nerve. 64 (6): 621-8. PMID ... PGD2 with Adenosine promotes sleep. In silico simulations have predicted the following as potential inhibitors of PGD2 synthase ...
Wouter Van Belle
"Belgian Asociality - Adenosine Trifosfaat Preparaat". Ultratop. Retrieved 10 November 2021. "BiezeBaaze - Wachten op misschien ... Adenosine Trifosfaat Preparaat (1995), #44 in Flanders BiezeBaaze, Wachten op misschien (2003), #31 in Flanders Flip Kowlier ...
July 2008). "Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: ... SCH-442,416 is a highly selective adenosine A2a subtype receptor antagonist. It is widely used in its 11C radiolabelled form to ... April 2005). "In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416". European Journal of ... El Yacoubi M, Costentin J, Vaugeois JM (December 2003). "Adenosine A2A receptors and depression". Neurology. 61 (11 Suppl 6): ...
However, unlike adenosine, it is relatively resistant to breakdown by the enzyme adenosine deaminase, which causes it to ... Chemically, it mimics nucleoside adenosine; however, unlike adenosine, cladribine has a chlorine molecule at position 2, which ... Carson had studied adenosine deaminase deficiency and recognised that because the lack of adenosine deaminase led to the ... renders it partially resistant to breakdown by adenosine deaminase. This causes it to accumulate in cells and interfere with ...
... adenosine triphosphate, the energy molecule; and oxygen. It occurs in modified excretory organs known as Malpighian tubules in ...
Dowler MJ, Nakada HI (1968). "Yeast phosphoramidate-adenosine diphosphate phosphotransferase". J. Biol. Chem. 243 (7): 1434-40 ... Other names in common use include phosphoramidate-adenosine diphosphate phosphotransferase, and phosphoramidate-ADP- ...
Adenosine deaminase 2 deficiency: MedlinePlus Genetics
Adenosine deaminase 2 (ADA2) deficiency is a disorder characterized by abnormal inflammation of various tissues. Explore ... Garg N, Kasapcopur O, Foster J 2nd, Barut K, Tekin A, Kizilkilic O, Tekin M. Novel adenosine deaminase 2 mutations in a child ... Deficiency of Adenosine Deaminase Type 2: A Description of Phenotype and Genotype in Fifteen Cases. Arthritis Rheumatol. 2016 ... Adenosine deaminase 2 (ADA2) deficiency is a disorder characterized by abnormal inflammation of various tissues. Signs and ...
Adenosine-Guided Ablation Reduces Arrhythmia Recurrence
Using adenosine to help unmask dormant pulmonary vein conduction following ablation, researchers reduced atrial tachyarrhythmia ... The Adenosine Following Pulmonary Vein Isolation to Target Dormant Conduction Elimination (ADVICE) trial was presented here at ... Adenosine may be used during the AF ablation procedure to detect pulmonary veins at risk of later reconnection, the so-called ... "If a routine strategy of adenosine testing is used with elimination of dormant conduction when present, which it is in about ...
Pharmacologic Stress Testing Technique: Approach Considerations, Adenosine Technique, Dipyridamole (Persantine) Technique
Adenosine Technique. Dosing and practical considerations. The use of adenosine requires an infusion pump that delivers the dose ... Adenosine-walk protocol. For patients who are able, combined low-level treadmill exercise during adenosine infusion has been ... Adenosine is infused at a rate of 140 mcg/kg/min for 6 minutes. At the 3-minute mark, the stress radiopharmaceutical is ... Spare adenosine A2a receptors are associated with positive exercise stress test in coronary artery disease. Mol Med. 2016 Jul ...
Adenosine - Wikipedia
When adenosine enters the circulation, it is broken down by adenosine deaminase, which is present in red blood cells and the ... Adenosine is believed to be an anti-inflammatory agent at the A2A receptor. Topical treatment of adenosine to foot wounds in ... Adenosine used as a second messenger can be the result of de novo purine biosynthesis via adenosine monophosphate (AMP), though ... Adenosine has been shown to promote thickening of hair on people with thinning hair. A 2013 study compared topical adenosine ...
Caffeine and adenosine
... as does adenosine, exerts effects on neurons and glial cells of all brain areas. In consequence, caffeine, when acting as an AR ... Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): A1, A2A, A3, and A2B ... Caffeine and adenosine J Alzheimers Dis. 2010;20 Suppl 1:S3-15. doi: 10.3233/JAD-2010-1379. ... Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): A1, A2A, A3, and A2B ...
Adenosine Triphosphate News, Research - Page 2
Adenocard, Adenoscan (adenosine) dosing, indications, interactions, adverse effects, and more
... adenosine), frequency-based adverse effects, comprehensive interactions, contraindications, pregnancy & lactation schedules, ... Push adenosine as fast as possible (1-3 sec). While keeping pressure on adenosine syringe plunger, push NS flush as fast as ... encoded search term (adenosine (Adenocard%2C Adenoscan)) and adenosine (Adenocard, Adenoscan) What to Read Next on Medscape ... FDA Issues Warning on Regadenoson, Adenosine * Selective adenosine-receptor agonist for resting perfusion scans now on the ...
Physiology, Adenosine Triphosphate - StatPearls - NCBI Bookshelf
Adenosine triphosphate (ATP) is the source of energy for use and storage at the cellular level. The structure of ATP is a ... The intravenous adenosine infusion acts on the A1 adenosine receptor, initiating a signaling cascade that ultimately aids the ... Adenosine also decreased postoperative opioid usage, suggesting a potential long-lasting A1 adenosine receptor activation. ... Physiology, Adenosine Triphosphate. Jacob Dunn; Michael H. Grider.. Author Information. Authors. Jacob Dunn1; Michael H. Grider ...
Adenosine 5′-diphosphate =90 16178-48-6 C10H13N5Na2O10P2
Adenosine 5′-diphosphate disodium salt ≥90%; CAS Number: 16178-48-6; EC Number: 240-314-7; Synonyms: 5′-ADP-Na2; find Sigma- ... Upon its conversion to adenosine by ecto-ADPases, platelet activation is inhibited via adenosine receptors. ... Adenosine 5′-diphosphate disodium salt has been used as a purinergic G protein-coupled receptor P2Y12 agonistin platelet ... Adenosine 5′-diphosphate (ADP) is an adenine nucleotide involved in energy storage and nucleic acid metabolism via its ...
DailyMed - RED GINSENG VITALIZING HYDROG EL MASK- niacinamide, adenosine patch
Adenosine (UNII: K72T3FS567) (ADENOSINE - UNII:K72T3FS567) Adenosine. 0.016 g in 40 g. ... RED GINSENG VITALIZING HYDROG EL MASK- niacinamide, adenosine patch. Out of scope - Out of scope for RxNorm and will not ... RED GINSENG VITALIZING HYDROG EL MASK- niacinamide, adenosine patch. To receive this label RSS feed. Copy the URL below and ... RED GINSENG VITALIZING HYDROG EL MASK- niacinamide, adenosine patch. If this SPL contains inactivated NDCs listed by the FDA ...
JCI - Adenosine kinase inhibition promotes survival of fetal adenosine deaminase-deficient thymocytes by blocking dATP...
An adenosine receptor agonist does not mimic and an adenosine receptor antagonist does not prevent the effects of ADA ... Adenosine receptor expression. Adenosine receptor expression was analyzed by RT-PCR with RNA prepared from day-15 fetal ... Elevated adenosine can force reversal of the hydrolytic reaction to form SAH from adenosine and homocysteine (22). ... Adenosine receptor expression in murine fetal thymocytes. Adenosine receptor expression was analyzed by RT-PCR with RNA from ...
Adenosine A2A Receptors | Adenosine Receptors | Tocris Bioscience
View and buy high purity products active at Adenosine A2A Receptors from Tocris Bioscience. ... Adenosine A2A Receptors. Adenosine A2A receptors are members of the adenosine receptor group of G-protein-coupled receptors ... CD39 and CD73 are ectonucleotidases that convert ATP to adenosine, elevating concentrations of adenosine locally. Adenosine is ... Adenosine A2A receptors are members of the adenosine receptor group of G-protein-coupled receptors that also includes A1, A2B ...
Free Brochure Report of Adenosine Market is available for Download
The Efficacy and Safety of Succinylated Atelocollagen and Adenosine for the Treatment of Periorbital Wrinkles
However, we did not observe any effects of adenosine on periorbital wrinkles. Succinylated atelocollagen may be an effective ... right or left periorbital area was treated with either a solution containing succinylated atelocollagen and adenosine or a ... application of succinylated atelocollagen on periorbital wrinkles and to compare the results of treatment with adenosine, a ... D. Ryu, J. Jung, K. Chung, H. Suh, S. Oh and J. Lee, "The Efficacy and Safety of Succinylated Atelocollagen and Adenosine for ...
Direct Association of Adenosine Deaminase with a T Cell Activation Antigen, CD26 - NASA/ADS
Amino acid sequence analysis and immunoprecipitation studies demonstrated that this 43-kilodalton protein was adenosine ... Direct Association of Adenosine Deaminase with a T Cell Activation Antigen, CD26 *Kameoka, Junichi ... Amino acid sequence analysis and immunoprecipitation studies demonstrated that this 43-kilodalton protein was adenosine ...
Search of: adenosine AND Deaminase AND stem cell AND Vector AND Vector AND Hematopoietic - Results on Map - ClinicalTrials.gov
Adenosine and its Role in ATP and Athletic Energy
Adenosine Triphosphate is present in every living cell of the body. It is also available as a dietary supplement. Each year, ... Adenosine forms from the breakdown of adenosine triphosphate (ATP), the primary energy source in cells. Chemically, ATP is an ... Adenosine and the ATP Equation. Adenosine is a naturally occurring extracellular signaling molecule that facilitates essential ... Interval training seems to offer the greatest opportunity for elevated adenosine to occur. Adenosine production is dependent ...
RCSB PDB - 1QYR: 2.1 Angstrom Crystal structure of KsgA: A Universally Conserved Adenosine Dimethyltransferase
... to two adjacent adenosine bases in 16S rRNA. This enzyme and the resulting modified adenosine bases appear to be conserved in ... to two adjacent adenosine bases in 16S rRNA. This enzyme and the resulting modified adenosine bases appear to be conserved in ... 2.1 Angstrom Crystal structure of KsgA: A Universally Conserved Adenosine Dimethyltransferase. *PDB DOI: 10.2210/pdb1QYR/pdb ... which methylate a single adenosine base in 23S rRNA and confer resistance to the MLS-B group of antibiotics. Despite their ...
Portage targets adenosine pathway with Tarus acquisition - BioProcess InsiderBioProcess International
Portage Biotech will gain four assets targeting various aspects of the adenosine pathway through the acquisition of Tarus ... TT-53 (now PORT-8):a dual inhibitor of adenosine receptors 2A and 2B (A2A/A2B), which aims to treat solid tumors. Portage plans ... TT-10 (now PORT-6):an adenosine receptor type 2A (A2A) inhibitor to treat solid tumors. It has been granted IND clearance and ... TT-4 (now PORT-7): an adenosine receptor type 2B (A2B) inhibitor to treat solid tumors, clinical development is expected to ...
Adenosine 5'-Triphosphate (ATP Supplement) - Proteinfactory
... is a clinically validated and patented form of Adenosine 5-Triphosphate (ATP supplement). Get the best ATP supplement right ... Adenosine 5-Triphosphate (ATP Supplement). Adenosine 5′-Triphosphate (ATP supplement) can be used for lean muscle building and ... "PEAK ATP® is a clinically validated and patented form of Adenosine 5-Triphosphate (ATP supplement) Disodium shown to improve ... Study shows effects of oral adenosine-5-triphosphate supplementation on athletic performance, skeletal muscle hypertrophy and ...
LOINC LG42243-2 - Adenosine monophosphate.cyclic|Pt|Ser/Plas
Cefazolin sodium and Adenosine interactions starting with G - eHealthMe
Adenosine analogs and sleep in rats. | Journal of Pharmacology and Experimental Therapeutics
The effects of N6-L-(phenylisopropyl)adenosine, cyclohexyladenosine and adenosine-5-N-ethylcarboxamide on sleep were examined ... for 0.1 mumol/kg of cyclohexyl-adenosine and 0.3 mumol/kg of N6-L-(phenylisopropyl)adenosine, respectively. Slow-wave sleep1 ... that activation of A1 rather than A2 receptors contributed to the sleep effects of the drugs because adenosine and adenosine ... Adenosine analogs and sleep in rats.. M Radulovacki, R M Virus, M Djuricic-Nedelson and R D Green ...
Adenosine A2 Receptor Agonists | Profiles RNS
Adenosine A1 and A2A receptor regulation of protein phosphatase 2A in the murine heart. J Cell Physiol. 2008 Jul; 216(1):83-90. ... Yang D, Chen H, Koupenova M, Carroll SH, Eliades A, Freedman JE, Toselli P, Ravid K. A new role for the A2b adenosine receptor ... Adenosine A2A and beta-adrenergic calcium transient and contractile responses in rat ventricular myocytes. Am J Physiol Heart ... "Adenosine A2 Receptor Agonists" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ( ...
Adenosine triphosphate (ATP) Complete
Search of: adenosine AND Deaminase AND stem cell AND Vector AND Vector AND Deaminase - Results by Topic - ClinicalTrials.gov
Presynaptic inhibition of excitatory synaptic transmission by adenosine in rat hippocampus: analysis of unitary EPSP variance...
Presynaptic inhibition of excitatory synaptic transmission by adenosine in rat hippocampus: analysis of unitary EPSP variance ... Presynaptic inhibition of excitatory synaptic transmission by adenosine in rat hippocampus: analysis of unitary EPSP variance ... Presynaptic inhibition of excitatory synaptic transmission by adenosine in rat hippocampus: analysis of unitary EPSP variance ... Presynaptic inhibition of excitatory synaptic transmission by adenosine in rat hippocampus: analysis of unitary EPSP variance ...
Atrial Flutter Converted to Sinus Rhythm by Adenosine Infusion | Kansas Journal of Medicine
Modulation of adenosine signalling in sheep adipose tissue by growth hormone | Biochemical Society Transactions | Portland Press
TriphosphateReceptorsNucleosideMonophosphateKinaseMetabolismRole of adenosinePathwayIntravenousSubtypesMoleculeAgonistEffect of adenosineResponse to adenosineInjectionCyclic AdenosineExtracellular adenosineAntagonists on operant behaviorExertsCardiacDeficiencyCaffeineAntiarrhythmicInhibitionEnzyme called adenosineIncrease adenosine levelsProteinPotentPathwaysLevels of adenosineRelease of adenosineFunction of adenosineSuggest that adenosineTheophyllineEffectsInosineTriphosphataseDipyridamoleUptakeTherapeuticRiboseIntracellular adenosineDerivativesInfusionEnzymesNECAIMSEAR at SEAROSupraventricular tachycardiaMyocardialConcentrationsDrugsDoseCellular
- Its derivatives include the energy carriers adenosine mono-, di-, and triphosphate, also known as AMP/ADP/ATP. (wikipedia.org)
- Scientists have developed a prototype sensor that could help doctors rapidly measure adenosine triphosphate (ATP) and lactate levels in blood samples from patients, aiding in the rapid assessment of the severity of some diseases. (news-medical.net)
- Adenosine triphosphate (ATP) is the source of energy for use and storage at the cellular level. (nih.gov)
- Adenosine Triphosphate is present in every living cell of the body. (nfpt.com)
- Adenosine forms from the breakdown of adenosine triphosphate (ATP), the primary energy source in cells. (nfpt.com)
- These powerhouses, located within cells, convert carbohydrates (glucose, in their most elemental form) to adenosine triphosphate (ATP). (nfpt.com)
- Adenosine 5′-Triphosphate (ATP supplement) can be used for lean muscle building and energy, It is distributed and manufactured by the TSI group. (proteinfactory.com)
- PEAK ATP® is a clinically validated and patented form of Adenosine 5'-Triphosphate (ATP supplement) Disodium shown to improve body composition and athletic performance by increasing muscular excitability, blood flow and recovery. (proteinfactory.com)
- Prior research has focused largely on the two major ectonucleotidases, ectonucleoside triphosphate diphosphohydrolase 1/cluster of differentiation (CD)39 and ecto-5'-nucleotidase/CD73, which catalyze the breakdown of extracellular ATP into adenosine, and on the subsequent activation of different subtypes of adenosine receptors with mixed findings of antitumor and protumor effects. (utu.fi)
- As its name suggests, adenosine triphosphate is comprised of adenosine bound to three phosphate groups ( [link] ). (edu.vn)
- Although adenosine triphosphate-magnesium chloride (ATP-MgCl 2 ) has demonstrated cytoprotective effects in a variety of adverse pathophysiologic conditions, its ability to alter radiation injury is unknown. (utmb.edu)
- Disodium adenosine triphosphate is used to maintain the skin in good condition. (loreal.com)
- In atp adenosine triphosphate, the energy released when ATP is hydrolyzed to ADP and AMP is used to fuel metabolic reactions and other cellular processes, such as the movement of proteins within cells, by active transport across plasma membranes and muscle contraction. (ibiologia.com)
- What are the components of Adenosine triphosphate ATP? (ibiologia.com)
- ATP stands for Adenosine triphosphate, and it is usually administered in liposomal form via a spray during a hair transplant procedure. (hairlosscure2020.com)
- Effects of adenosine triphosphate and other substances on hydroxyproline-induced inhibition of Avena coleoptile elongation (Unpublished thesis). (txstate.edu)
- Extracellular adenosine triphosphate increases cation permeability of chronic lymphocytic leukemic lymphocytes. (austin.org.au)
- Extracellular adenosine triphosphate (ATP) is known to reversibly increase the cation permeability of a variety of freshly isolated and cultured cell types. (austin.org.au)
- SAMe, also known as S-Adenosyl Methionine, is a supplement made from Adenosine Triphosphate and Methionine and is used as a treatment for mild depression, boosting mood and nergy levels. (trackmystack.com)
- Adenosine triphosphate (ATP), is an energy-carrying molecule found in the cells of all living things. (kitabdukan.com)
- Adenosine triphosphate is an organic compound and hydrotropic that provides energy to drive many processes in living cells, such as muscle contraction, nerve impulse propagation, condensate dissolution, and chemical synthesis. (kitabdukan.com)
- ABCB6 is an associate from the adenosine triphosphate (ATP)-binding cassette category of transporter protein that's increasingly named another physiological and therapeutic focus on. (conferencedequebec.org)
- Now, a new study in mice has found that remote inflammation spreads by neuron crosstalk, and that the molecule adenosine triphosphate (ATP) plays a key role in this by acting as a neurotransmitter and inflammation enhancer. (cosmosmagazine.com)
- Adenosine Triphosphate Sampling Pen market is segmented by Type and by Application . (znewsafrica.com)
- Players, stakeholders, and other participants in the global Adenosine Triphosphate Sampling Pen market will be able to gain the upper hand as they use the report as a powerful resource. (znewsafrica.com)
- The interaction between Fe content titanium dioxide (TiO2) NPs and adenosine triphosphate (ATP) biomolecules has been envisioned. (edu.in)
- The structure of Adenosine 5'-triphosphate disodium salt's molecules can be abbreviated as AP ~ P ~P, where A representative of adenosine, P behalf of phosphate groups, ~ represents a particular chemical bond, called the high-energy phosphate bond, high-energy phosphate bond cleavage, the large amount of energy is released out. (prius-biotech.com)
- Adenosine 5'-triphosphate disodium salt is a kind of coenzyme. (prius-biotech.com)
- Adenosine triphosphate is used as Pharmaceutical Raw Material. (prius-biotech.com)
- Both propofol and thiamylal inhibit adenosine triphosphate-sensitive potassium (KATP) channels. (asahq.org)
- ADENOSINE triphosphate (ATP)-sensitive potassium (K ATP ) channels are composed of two different types of protein subunits, i.e. , a sulfonylurea receptor (SUR) and an inwardly rectifying K + channel (Kir6). (asahq.org)
- ATP - adenosine triphosphate, the vital energy source that keeps our body's cells alive, runs amok at the site of a spinal cord injury, pouring into the area around the wound and killing the cells that normally allow us to move, scientists report in the cover story of the August issue of Nature Medicine. (news-medical.net)
- Stimulate the release of adenosine triphosphate (ATP). (nutrimedical.com)
- Adenosine 5-triphosphate is a well-known extracellular signaling molecule and neurotransmitter recognized to activate purinergic P2X receptors. (careersfromscience.org)
- Methylxanthines (e.g. caffeine found in coffee, theophylline found in tea, or theobromine found in chocolate) have a purine structure and bind to some of the same receptors as adenosine. (wikipedia.org)
- Caffeine has a three-dimensional structure similar to that of adenosine," which allows it to bind and block its receptors. (wikipedia.org)
- Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): A1, A2A, A3, and A2B and, as does adenosine, exerts effects on neurons and glial cells of all brain areas. (nih.gov)
- In consequence, caffeine, when acting as an AR antagonist, is doing the opposite of activation of adenosine receptors due to removal of endogenous adenosinergic tonus. (nih.gov)
- Adenosine A 2A receptors are members of the adenosine receptor group of G-protein-coupled receptors that also includes A 1 , A 2B and A 3 . (tocris.com)
- Adenosine is a crucial mediator of altered immune function in cancer as it binds A 2A and A 2B receptors on lymphocytes silencing the antitumor immune response. (tocris.com)
- Tocris offers the following scientific literature for Adenosine A 2A Receptors to showcase our products. (tocris.com)
- a dual inhibitor of adenosine receptors 2A and 2B (A2A/A2B), which aims to treat solid tumors. (bioprocessintl.com)
- Studies suggest that targeting the A2A and A2B receptors in cancers where adenosine is highly expressed could reduce immunosuppression and improve immune response to tumors, potentially reducing cancer progression and improving outcomes for patients. (bioprocessintl.com)
- Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (umassmed.edu)
- It appears, therefore, that activation of A1 rather than A2 receptors contributed to the sleep effects of the drugs because adenosine and adenosine analogs activate A1 receptors in nanomolar quantities whereas activation of A2 receptors requires micromolar concentration of these compounds. (aspetjournals.org)
- Use of selective adenosine receptor antagonists revealed that adenosine A2(B) receptors (A2(B)R) mediate the early HAS1 induction, whereas late HAS1 induction was mediated via A2(A)R and A3R. (nih.gov)
- 5. We conclude that, using the agents tested, the A2B adenosine receptor cloned from human brain expressed in Chinese hamster ovary cells exhibits an identical pharmacological profile to native A2B receptors in guinea-pig brain. (garvan.org.au)
- A valued reader of this site, Rachelle Holmes at Chicago Plastic Surgery Center , wrote to suggest the importance of understanding the adenosine A1 receptors in the mechanism of action of acupuncture for pain management. (thecamreport.com)
- Glucocorticoid receptor activation leads to up-regulation of adenosine A1 receptors and down-regulation of adenosine A2 responses in DDT1 MF-2 smooth muscle cells. (aspetjournals.org)
- The effect of glucocorticoid treatment of DDT1 MF-2 smooth muscle cells on the signaling via two adenosine receptors with opposing actions on cAMP generation was examined. (aspetjournals.org)
- Treatment with dexamethasone caused a dose- and time-dependent increase in the number of adenosine A1 receptors but did not affect the KD or the proportions of receptors in high and low affinity states. (aspetjournals.org)
- In addition, the adenosine A2 receptors were down-regulated, as indicated by the fact that the ability of the A2 receptor agonist 5'-N-ethylcarboxamidoadenosine to increase cAMP formation was decreased by 20-30% in dexamethasone-treated cells. (aspetjournals.org)
- The function of adenosine is controlled through four G-protein coupled receptors: A 1 , A 2A , A 2B and A 3 . (medscape.com)
- Adenosine receptors are ubiquitous and are activated by different ranges of endogenous adenosine concentrations. (medscape.com)
- A 2 subtypes are cyclic adenosine-3′,5′-monophosphate (cAMP)-elevating, Gs protein-coupled receptors positively coupled to adenylyl cyclase. (medscape.com)
- A multifunctional, ubiquitous molecule, adenosine acts at cell-surface G protein-coupled receptors, as well as numerous enzymes, including protein kinases and adenylyl cyclase. (guidetopharmacology.org)
- Adenosine acts as an activator (agonist) on (purinergic) adenosine receptors throughout the body. (selfhacked.com)
- Four adenosine receptors have been identified (A1, A2a, A2B, and A3), but as a drug, it mainly activates receptors in the so-called cardiac atrioventricular (AV) nodal tissue and those within the blood vessels to achieve its therapeutic effects [ 8 ]. (selfhacked.com)
- H did Powered by the Warsaw Tank book Adenosine receptors in health and disease 2009 of the great 501(c)(3 Corps in Italy during 1944. (stoneriverinc.com)
- book Adenosine receptors communications of drinks! (stoneriverinc.com)
- The book Adenosine receptors in will modify written to organized book email. (stoneriverinc.com)
- Through its receptors, adenosine is able to inhibit the acute inflammatory process, increase the protection capacity of the epithelial barrier, and reduce the damage due to an overactivation of the immune system, such as that occurring in cytokine storms. (uniroma5.it)
- In the NAc, subtypes of dopamine (DA) and adenosine (ADO) receptors are co-localized in distinct subpopulations of neurons where they play antagonistic roles on cellular functioning. (grantome.com)
- Our potent Pan Adenosine receptors fluorescent antagonist shows affinity for hA1, hA2A, hA2B and hA3 Adenosine receptors (Ki =20.9 nM, 171 nM, 44,7nM and 95.2 nM respectively in radioligand binding assays). (celtarys.com)
- Our potent and partially selective hA1 Adenosine receptor fluorescent antagonist shows higher affinity for hA1 (Ki =8.60 nM) compared to hA2A, hA2B and hA3 Adenosine receptors (Ki= 98.38 nM, 72.24 and 231.01 nM respectively in radioligand binding assays). (celtarys.com)
- We hypothesize that both striatal gene induction and catalepsy elicited by haloperidol arise from the combined effect of excitatory adenosinergic and glutamatergic inputs acting at adenosine A(2A) and N-methyl-D-aspartate (NMDA) receptors, respectively. (elsevier.com)
- These results indicate that the haloperidol-induced increases in c-fos and NT gene expression in the dorsolateral striatum and catalepsy are driven largely by adenosine and glutamatergic inputs acting at A(2A) and NMDA receptors. (elsevier.com)
- Chartoff, EH, Ward, RP & Dorsa, DM 1999, ' Role of adenosine and N-methyl-D-aspartate receptors in mediating haloperidol-induced gene expression and catalepsy ', Journal of Pharmacology and Experimental Therapeutics , vol. 291, no. 2, pp. 531-537. (elsevier.com)
- ATP is broken down into adenosine, which binds with receptors on nerve cells. (ibiologia.com)
- However, there are exceptions: One is the discovery that certain drugs that bind to a class of adenosine receptors on neurons (ADORA1) can restore memory in transgenic mice that already have become demented. (curealz.org)
- Researchers use A3 adenosine receptors to activate 'off signals' for chronic pain. (health-innovations.org)
- Objectives Caffeine is extensively consumed as a psychostimulant drug, acting on A1 and A2A adenosine receptors blockade. (edu.br)
- Our goal was to evaluate the effect of chronic caffeine exposure during gestation and breast-feeding in the functionality of adenosine A1 receptors in infant rats at P14. (edu.br)
- Human and animal studies have converged to suggest that caffeine consumption prevents memory deficits in aging and Alzheimer's disease through the antagonism of adenosine A2A receptors (A2ARs). (universiteitleiden.nl)
- We describe here the synthesis and biological activity of new 8-azaadenines bearing both a phenyl group on C(2) and a 9-benzyl group substituted in the ortho position with a Cl or a F atom or a CF3 group, to verify the synergistic effect of a combination of these substitution patterns on binding with the A1 adenosine receptors. (unipi.it)
- Agonists and antagonists of the other types of adenosine receptors had no significant effect. (lih.lu)
- To assess the effects of adenosine A2A receptors on BBB permeability in vitro and in vivo. (tischms.org)
- The involvement of adenosine A 2A receptors in regulating aspects of instrumental response output and behavioral activation may have implications for the treatment of effort-related psychiatric dysfunctions, such as psychomotor slowing and anergia in depression. (elsevier.com)
- Adenosine exerts its effects by interacting with G-protein coupled receptors (GPCR) namely A1, A2A, A2B and A3, respectively. (indexindex.com)
- Our results showed that adenosine, the endogenous agonist of adenosine receptors, and CPA, a selective agonist of A(1) receptor, decreased the atrial chronotropism of NWR and SHR in a concentration- and time-dependent manner, culminating in cardiac arrest (0 bpm). (unifesp.br)
- Pre-incubation of tissues from both strains with DPCPX, a selective A(1) receptor antagonist, inhibited the negative chronotropic effect of CPA, while simultaneous inhibition of A(2) and A(3) receptors, with ZM241385 and MRS1523, did not change the adenosine chronotropic effects. (unifesp.br)
- These data indicate that the negative chronotropic effect of adenosine in right atrium depends exclusively on the activation of A(1) receptors. (unifesp.br)
- Adenosine is one of the four nucleoside building blocks of RNA (and its derivative deoxyadenosine is a building block of DNA), which are essential for all life. (wikipedia.org)
- This is being contended and it is now considered a relative contraindication (however, selective adenosine antagonists are being investigated for use in treatment of asthma) Adenosine is an endogenous purine nucleoside that modulates many physiological processes. (wikipedia.org)
- Adenosine is an endogenous nucleoside with a short half-life that regulates many physiological functions involving the heart and cardiovascular system. (medscape.com)
- The endogenous, ubiquitous purine-nucleoside adenosine exerts multiple biochemical effects that serve important roles in cardiac and vascular biology. (medscape.com)
- It is inactivated either by extracellular metabolism via adenosine deaminase (also producing ammonia) or, following uptake by nucleoside transporters, via adenosine deaminase or adenosine kinase (requiring ATP as co-substrate). (guidetopharmacology.org)
- Adenosine is a nucleoside consisting of the nitrogenous base adenine and a five-carbon sugar, ribose. (edu.vn)
- Adenosine is an endogenous nucleoside occurring in all cells of the body. (medlibrary.org)
- Adenosine Injection is antagonized competitively by methylxanthines such as caffeine and theophylline, and potentiated by blockers of nucleoside transport such as dipyridamole. (medlibrary.org)
- It is an ester of phosphoric acid with the nucleoside adenosine. (lmdb.ca)
- While these results place adenosine nucleosidase in the non-specific inosine-uridine nucleoside hydrolases (IU-NH), significant differences in its substrate specificity compared to the lead enzyme of the class, (IU-NH) from Crithidia fasciculata were found. (mtsu.edu)
- Adenosine is nucleoside that is composed of adenine and d-ribose. (ecmdb.ca)
- Adenosine, a naturally produced nucleoside, has been shown to have cardioprotective effects and to inhibit secretion of various cytokines. (lih.lu)
- CBD inhibited adenosine uptake via equilibrative nucleoside transporter 1 and synergistically enhanced adenosine's TNF-α suppression upon LPS treatment. (thecannabisadvisory.com)
- Cyclic adenosine monophosphate (cAMP) is pervasive in signal transduction. (wikipedia.org)
- In some instances, the second phosphate group can also be further broken down to form adenosine monophosphate (AMP) . (nfpt.com)
- The effect of benzo( a )pyrene on the accumulation of cyclic adenosine 3′,5′-monophosphate (cyclic AMP) in mouse skin in response to isoproterenol has been measured. (aacrjournals.org)
- ADENOSINE MONOPHOSPHATE INJECTION is a potent vasodilator to increase the flow of blood to cardiac and skeletal muscles. (horsemedsupplies.com)
- Actions: ADENOSINE MONOPHOSPHATE INJECTION is used as a potent natural vasodilator which produces a marked increase in blood circulation to both skeletal and cardiac muscles. (horsemedsupplies.com)
- DO NOT administer ADENOSINE MONOPHOSPHATE INJECTION by the intravenous (IV) route under any circumstances. (horsemedsupplies.com)
- Intracellular adenosine is rapidly metabolized either via phosphorylation to adenosine monophosphate by adenosine kinase, or via deamination to inosine by adenosine deaminase in the cytosol. (medlibrary.org)
- Adenosine monophosphate formed by phosphorylation of adenosine is incorporated into the high-energy phosphate pool. (medlibrary.org)
- Adenosine monophosphate, also known as 5'-adenylic acid and abbreviated AMP, is a nucleotide that is found in RNA. (lmdb.ca)
- The importance of adenyl cyclase and adenosine 3′,5′- monophosphate in the induction of tyrosine aminotransferase by adrenocorticosteroids has been tested in HTC cells derived from a rat hepatoma and grown in tissue culture. (wustl.edu)
- Under various experimental conditions, with or without glucocorticoids, neither adenyl cyclase nor cyclic adenosine monophosphate could be detected in HTC cells. (wustl.edu)
- In addition, neither the cyclic nucleotide nor N 6 ,O 2 ′-dibutyryl cyclic adenosine monophosphate caused increased activity of the transaminase in HTC cells. (wustl.edu)
- We conclude that induction of tyrosine aminotransferase by glucocorticoids is not mediated by the adenyl cyclase-cyclic adenosine monophosphate system. (wustl.edu)
- The addition or removal of phosphate results in adenosine diphosphate (ADP) and adenosine monophosphate (AMP). (ibiologia.com)
- Regulation of renal gluconeogenesis by calcium ions, hormones and adenosine 3': 5'-cyclic monophosphate. (elsevier.com)
- Solanki, V & Murray, A 1982, ' The Effect of Ischemia on Cyclic Adenosine 3',5'-Monophosphate Accumulation in Mouse Skin ', Journal of Investigative Dermatology , vol. 78, pp. 48-51. (edu.au)
- We have induced and controlled normal aggregation of Dictyostelium discoideum amoebas by electrophoretic release of pulses of cyclic adenosine monophosphate from a microelectrode. (princeton.edu)
- Norepinephrine activated adenylate cyclase through β -adrenoceptors, thereby significantly increased the level of cyclic adenosine monophosphate (cAMP), which enhanced the analgesic activity of MA [ 25 , 26 ]. (hindawi.com)
- Cells were harvested and then analyzed by real-time quantitative polymerase chain reaction in order to measure the quantity of adenosine monophosphate-activated protein kinase-α ( AMPK-α ), CCAAT enhancer binding protein-β ( C/EBPβ ), G protein-coupled receptor 41 ( GPR41 ), GPR43 , peroxisome proliferator-activated receptor-γ ( PPARγ ), and stearoyl CoA desaturase ( SCD ) mRNA relative to ribosomal protein subunit 9 ( RPS9 ). (animbiosci.org)
- The impact of Cr source on adenosine monophosphate-activated protein kinase (AMPK) activity has also been reported in vitro and in vivo [ 12 ]. (animbiosci.org)
- Schramm, VL & Fullin, FA 1978, ' Kinetics of adenosine monophosphate nucleosidase inactivation by phosphate and protection by substrate and allosteric activator ', Journal of Biological Chemistry , vol. 253, no. 7, pp. 2161-2167. (elsevier.com)
- Activating Adenosine Monophosphate-Activated Protein Kinase Mediates Fibroblast Growth Factor 1 Protection From Nonalcoholic Fatty Liver Disease in Mice. (amedeo.com)
- New findings, needed for more effective therapeutic approaches, require consideration of redundant pathways controlling intratumoral adenosine levels, including the alternative NAD-inactivating pathway through the CD38-ectonucleotide pyrophosphatase phosphodiesterase (ENPP)1-CD73 axis, the counteracting ATP-regenerating ectoenzymatic pathway, and cellular adenosine uptake and its phosphorylation by adenosine kinase. (utu.fi)
- A study led by Texas A&M AgriLife Research provides compelling evidence of the important role of hepatocyte adenosine kinase in the progression of nonalcoholic fatty liver disease, NAFLD. (gleetune.com)
- Since adenosine kinase has a lower K m and V max than adenosine deaminase, deamination plays a significant role only when cytosolic adenosine saturates the phosphorylation pathway. (medlibrary.org)
- The study, "Hepatocyte Adenosine Kinase Promotes Excessive Fat Deposition and Liver Inflammation," appeared in September in the journal Gastroenterology . (loire-net.tv)
- An important player in the proper function of hepatocytes is an enzyme called adenosine kinase, ADK. (loire-net.tv)
- The research demonstrated that hepatocyte adenosine kinase promotes excessive fat deposition and liver inflammation and is a key factor in the pathogenesis of nonalcoholic fatty liver disease," he said. (loire-net.tv)
- If further research validates the effects of dietary components on inhibiting adenosine kinase in hepatocytes, scientists could develop new approaches for managing this disease. (loire-net.tv)
- Wu said the new study strongly indicates that an unhealthy diet, such as a diet with enriched saturated fatty acids, has a stimulatory effect on increasing the adenosine kinase protein amount in the liver. (loire-net.tv)
- The inhibition of MMP-9 secretion by adenosine, as well as the calcium effect, was prevented by the protein kinase A inhibitor H-89. (lih.lu)
- Structure of human adenosine kinase at 1.5 A resolution. (expasy.org)
- dipyridamole increases levels of adenosine by decreasing metabolism. (medscape.com)
- This review provides a holistic view of extracellular and intracellular adenosine metabolism as an integrated complex network and summarizes recent data on the underlying mechanisms through which adenosine and its precursors ATP and ADP control cancer immunosurveillance, tumor angiogenesis, lymphangiogenesis, cancer-associated thrombosis, blood flow, and tumor perfusion. (utu.fi)
- SIGNIFICANCE STATEMENT: The discovery of the role of adenosine as immune checkpoint regulator in cancer has led to the development of novel therapeutic strategies targeting extracellular adenosine metabolism and signaling in multiple clinical trials and preclinical models. (utu.fi)
- The authors concluded, "These observations indicate that adenosine mediates the effects of acupuncture and that interfering with adenosine metabolism may prolong the clinical benefit of acupuncture. (thecamreport.com)
- Extracellular adenosine is thought to be produced either by export or by metabolism, predominantly through ecto-5'-nucleotidase activity (also producing inorganic phosphate). (guidetopharmacology.org)
- Adenosine diphosphate ( ADP ), also known as adenosine pyrophosphate (APP), is an important organic compound in metabolism and is essential to the flow of energy in living cells. (luxist.com)
- Here, we investigated the hypothesis that the activation of the low-affinity adenosine receptor, the A2B receptor (A(2B)R), promotes glucose uptake in neurons and astrocytes, thereby linking brain activity with energy metabolism. (bordeaux-neurocampus.fr)
- Adenosine is the final product of ATP metabolism, mainly derived from the action of 5'- nucleotidase cleavage of AMP. (unina.it)
Role of adenosine1
- The goal of this study is to determine the role of adenosine signaling in retinal inflammation and its potential modulation by CBD. (thecannabisadvisory.com)
- Portage Biotech will gain four assets targeting various aspects of the adenosine pathway through the acquisition of Tarus Therapeutics. (bioprocessintl.com)
- According to Portage, the ability to evaluate all four investigational drugs alone or together will establish the best patient populations and oncology/non-oncology settings to make use of the adenosine pathway. (bioprocessintl.com)
- Our four newly acquired assets from Tarus Therapeutics will enable a comprehensive exploration of how targeting different aspects of the adenosine pathway could improve response in multiple cancer and non-cancer indications," said Walters. (bioprocessintl.com)
- Therefore, the adenosine pathway becomes an important therapeutic target to improve the effectiveness of immune therapies. (utu.fi)
- KSHV relies on manipulating the host cell N6-methyl adenosine (m6A) RNA modification pathway to enhance virus replication. (cam.ac.uk)
- Of these, 534 received intravenous adenosine 20 minutes after PVI to determine whether dormant PV conduction remained. (medscape.com)
- If one intravenous line is used, take care to inject the radiopharmaceutical slowly because a bolus or any forceful injection will cause an abrupt increase in the infusion rate of the adenosine running through the same line. (medscape.com)
- Adenosine is used as an intravenous medication for some cardiac arrhythmias. (wikipedia.org)
- Adenosine Injection is a sterile, nonpyrogenic solution for rapid bolus intravenous injection. (medlibrary.org)
- The intravenous bolus dose of 6 or 12 mg adenosine injection usually has no systemic hemodynamic effects. (medlibrary.org)
- A cumulative 60% of patients with paroxysmal supraventricular tachycardia had converted to normal sinus rhythm within one minute after an intravenous bolus dose of 6 mg adenosine injection (some converted on 3 mg and failures were given 6 mg), and a cumulative 92% converted after a bolus dose of 12 mg. (medlibrary.org)
- Intravenous adenosine injection is indicated for the following. (medlibrary.org)
- After 12 weeks, cardiac electron beam computed tomography (EBCT) was performed before and during intravenous infusion of adenosine, and myocardial perfusion (ml/min per g) and coronary microvascular permeability index (arbitrary units) were calculated. (elsevier.com)
- Adenosine InjectionUSP is AP-rated to AdenocardIV Injection (King PharmaceuticalsResearch and Development Inc). Theproduct should be given as a rapidbolus by the peripheral intravenous(IV) route. (pharmacytimes.com)
- Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). (wikipedia.org)
- Our potent and selective hA3 Adenosine receptor fluorescent antagonist shows a high affinity and selectivity for hA3 receptor over the other receptor subtypes (Ki =6.13 nM for A3 receptor in radioligand binding assay). (celtarys.com)
- There is high interest in the development of potent and selective ligands for these adenosine receptor (AR) subtypes, primarily for their therapeutic potential but also as pharmacological tools in receptor studies. (indexindex.com)
- The adenosine receptor (AR) subtypes expressed in rat retinal microglial cells was assessed by quantitative real-time RT-PCR. (thecannabisadvisory.com)
- Adenosine is a naturally occurring extracellular signaling molecule that facilitates essential functions in human biology and physiology. (nfpt.com)
- When a cell needs energy, it breaks this bond to form adenosine diphosphate (ADP) and a free phosphate molecule. (nfpt.com)
- The reason that these bonds are considered "high-energy" is because the products of such bond breaking-adenosine diphosphate (ADP) and one inorganic phosphate group (P i )-have considerably lower free energy than the reactants: ATP and a water molecule. (edu.vn)
- CP hands over its extra phosphate molecule to adenosine diphosphate (ADP), thus regenerating ATP. (ibiologia.com)
- ATP (Adenosine tri-phosphate) is an important molecule found in all living things. (kitabdukan.com)
- Adenosine acts as a regulatory signaling molecule in other areas of the nervous system, so the team hypothesized that A3AR might also play a role in regulating pain signals during pain processing. (health-innovations.org)
- a phosphate group is transferred to another molecule in a process called phosphorylation, and ATP is converted to adenosine diphosphate (ADP). (cosmosmagazine.com)
- Adenosine is a multi-tasking, high-energy molecule that exists naturally in our bodies. (aceology.com)
- Ex Vivo Perfusion With Adenosine A2A Receptor Agonist Enhances Rehabilitation of Murine Donor Lungs After Circulatory Death. (umassmed.edu)
- Ex vivo lung perfusion with adenosine A2A receptor agonist allows prolonged cold preservation of lungs donated after cardiac death. (umassmed.edu)
- The adenosine receptor agonist NECA (10 μM) caused a strong induction of HA synthase (HAS)1 at 6 h and a weaker induction again after 24 h. (nih.gov)
- Direct injection of an adenosine A1 receptor agonist mimicked the pain relieving effect of acupuncture. (thecamreport.com)
- 1 The effects of seven agonist and three antagonist adenosine receptor ligands were compared on the guinea-pig sinoatrial (SA) node (isolated right atrium) and atrioventricular (AV) node (perfused whole heart). (uu.nl)
- 4 The agonist potency and antagonist affinity data obtained are consistent with previous findings showing that the AV and SA node data are pharmacologically indistinguishable and belong to the adenosine A1-receptor class. (uu.nl)
- Capadenoson (BAY 68-4986) is a new adenosine A1 receptor agonist. (mosdj.com)
- The effect of adenosine was mimicked by the adenosine A2a receptor agonist CGS21680 and was inhibited by both the A2a antagonist SCH5826 and A2a RNA silencing. (lih.lu)
- The effect of GR190178, a selective low-efficacy adenosine A1 receptor agonist, on the treatment of neuropathic hyperalgesia in the rat. (ox.ac.uk)
- Adenosine A2A Receptor Agonist, 2-p-(2-Carboxyethyl)phenethylamino-5′-N-ethylcarboxamidoadenosine hydrochloride hydrate (CGS21680), Inhibits Inflammation and Increases Fibroblast Growth Factor 2 (FGF-2) Tissue Expression in Carrageenan Induced Rat Paw Edema. (unina.it)
- The purpose of the present work was to investigate on the antinflammatory effect of systemic administration of the adenosine A2A agonist, 2-p-(2- Carboxyethyl)phenethylamino-5′-N-ethylcarboxamidoadenosine hydrochloride hydrate (CGS21680), in the rat model of carrageenan-induced paw edema. (unina.it)
- NIDDK announces the availability of a highly selective A1 adenosine receptor (AR) agonist. (nih.gov)
Effect of adenosine2
Response to adenosine2
- The aim of this study was to examine the regulation and function of HA matrix in response to adenosine in human coronary artery SMC (HCASMC). (nih.gov)
- The response to adenosine in JET is a temporary loss of conduction to the atria leading to continuation of the tachycardia but with atrioventricular dissociation. (wikipedia.org)
- Tips for Trainers: Use ADENOSINE INJECTION in combination with Racehorse Meds B12 with Phosphorous Injection 24 hours and again 4-6 hours pre-event, to improve blood and nutrient supply to hard working muscles. (horsemedsupplies.com)
- Each mL contains 3 mg adenosine and 9 mg sodium chloride in Water for Injection. (medlibrary.org)
- Adenosine Injection slows conduction time through the A-V node, can interrupt the reentry pathways through the A-V node, and can restore normal sinus rhythm in patients with paroxysmal supraventricular tachycardia (PSVT), including PSVT associated with Wolff-Parkinson-White Syndrome. (medlibrary.org)
- Adenosine Injection is not blocked by atropine. (medlibrary.org)
- As adenosine injection requires no hepatic or renal function for its activation or inactivation, hepatic and renal failure would not be expected to alter its effectiveness or tolerability. (medlibrary.org)
- Valsalva maneuver), should be attempted prior to adenosine injection administration. (medlibrary.org)
- It is important to be sure the adenosine injection solution actually reaches the systemic circulation (see DOSAGE AND ADMINISTRATION).Adenosine Injection does not convert atrial flutter, atrial fibrillation, or ventricular tachycardia to normal sinus rhythm. (medlibrary.org)
- Adenosine Injection exerts its effect by decreasing conduction through the A-V node and may produce a short lasting first-, second- or third-degree heart block. (medlibrary.org)
- The recommended adenosine injection dose is 0.14 mg/kg/min infused over six minutes (total dose of 0.84 mg/kg) ( Table 1 ). (pfizermedicalinformation.com)
- Visually inspect adenosine injection for particulate matter and discoloration prior to administration. (pfizermedicalinformation.com)
- Do not administer adenosine injection if it contains particulate matter or is discolored. (pfizermedicalinformation.com)
- There are no data on the safety or efficacy of alternative adenosine injection infusion protocols. (pfizermedicalinformation.com)
- The safety and efficacy of adenosine injection administered by the intracoronary route have not been established. (pfizermedicalinformation.com)
- Adenosine Injection is indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately. (pfizermedicalinformation.com)
- Adenosine Injection USPis available in a 2-mL, 3-mg/mL prefilledsyringe and in 3-mg/mL, 2-mL, and4-mL injectable single-dose vials. (pharmacytimes.com)
- L'agrégation plaquettaire induite par le collagène dans des échantillons de plasma riche en plaquettes de 14 lapins sains a été mesurée par turbidimétrie en utilisant un agrégomètre, avant et une heure après une injection intra- veineuse d'alun. (who.int)
- An approach to a carbocyclic analogue of cyclic adenosine 5'-diphosphate ribose. (ox.ac.uk)
- While extracellular adenosine is primarily cleared by cellular uptake with a half-life of less than 10 seconds in whole blood, excessive amounts may be deaminated by an ecto-form of adenosine deaminase. (medlibrary.org)
- ATP consumption during intense neuronal activity leads to peaks of both extracellular adenosine levels and increased glucose uptake in the brain. (bordeaux-neurocampus.fr)
Antagonists on operant behavior1
- However, little is known about the effects of selective adenosine antagonists on operant behavior when these drugs are administered alone. (elsevier.com)
- [ 1-3 ] Adenosine is known to regulate myocardial and coronary circulatory functions and exerts potent vasodilatory effects in most vascular beds of mammalian species. (medscape.com)
- Because of its potent vasodilation effect on cardiac muscles, adenosine is effective in the treatment and prevention of heart strain and exercise induced changes in horses. (horsemedsupplies.com)
- Therefore, herein, we evaluated whether modifications of adenosine receptor signaling may contribute to the cardiac dysfunction observed in hypertension. (unifesp.br)
- Isolated right atria from spontaneously hypertensive (SHR) or normotensive Wistar rats (NWR) were used to investigate the influence of adenosine receptor signaling cascade in the cardiac chronotropism. (unifesp.br)
- Adenosine deaminase 2 (ADA2) deficiency is a disorder characterized by abnormal inflammation of various tissues. (medlineplus.gov)
- Meyts I, Aksentijevich I. Deficiency of Adenosine Deaminase 2 (DADA2): Updates on the Phenotype, Genetics, Pathogenesis, and Treatment. (medlineplus.gov)
- Adenosine Deaminase (ADA)-Deficient Severe Combined Immune Deficiency (SCID) in the US Immunodeficiency Network (USIDNet) Registry. (duke.edu)
- 1. Treatment with autologous CD34+ hematopoietic stem and progenitor cells transduced with human ADA via a lentiviral vector showed sustained ADA expression in patients with severe combined immunodeficiency from adenosine deaminase deficiency. (2minutemedicine.com)
- Reports and Data has recently published a new research report on Global Adenosine Deaminase Deficiency Market that covers current development scenario and emerging trends of the market. (icrowdnewswire.com)
- The report applies advanced statistical tools such as Porter's Five Forces analysis and SWOT analysis to shed light on the competitive landscape of the global Adenosine Deaminase Deficiency market. (icrowdnewswire.com)
- The report covers all the critical and essential information relating to the global Adenosine Deaminase Deficiency market which helps the readers and clients gain a thorough understanding of the market. (icrowdnewswire.com)
- Caffeine acts by blocking binding of adenosine to the adenosine A1 receptor, which enhances release of the neurotransmitter acetylcholine. (wikipedia.org)
- Methods: Six drugs were tested: two nonselective adenosine antagonists (caffeine and theophylline), two adenosine A 1 antagonists (DPCPX and CPT), and two adenosine A 2A antagonists (istradefylline (KW6002) and MSX-3). (elsevier.com)
- Because of the effects of adenosine on AV node-dependent SVTs, adenosine is considered a class V antiarrhythmic agent. (wikipedia.org)
- Adenosine is not chemically related to other antiarrhythmic drugs. (medlibrary.org)
- Adenosine is classified as a miscellaneous antiarrhythmic drug. (selfhacked.com)
- Unlike adenosine, other drugs for treating arrhythmias are categorized under classes I to IV of antiarrhythmic agents (Vaughan-Williams classification scheme) [ 8 ]. (selfhacked.com)
- Our aim was to investigate the combined therapeutic effect of two common antiarrhythmic compounds, adenosine and lidocaine (AL), on mortality, arrhythmia frequency and duration, and infarct size in the rat model of regional ischemia. (edu.au)
- Inhibition of enzymes involved in adenosine degradation increased the acupuncture-elicited increase in adenosine, as well as its anti-pain effect. (thecamreport.com)
- These results suggest that the activated A 2A AR in the retinal microglial cells plays a major role in anti-inflammation in the retina, and that CBD anti-inflammatory effects are linked to adenosine uptake inhibition. (thecannabisadvisory.com)
Enzyme called adenosine1
- This gene provides instructions for making an enzyme called adenosine deaminase 2. (medlineplus.gov)
Increase adenosine levels2
- Various popular training methods, such as cycling and interval training, may increase adenosine levels and thereby might enhance the response of adenosine-influenced adaptive mechanisms. (nfpt.com)
- The vasodilatory effect of GLP-1 is not abolished by theophylline and GLP-1 does not increase adenosine levels, indicating an adenosine-independent mechanism of GLP-1 coronary vasodilatation. (biomedcentral.com)
- Adenosine A1 and A2A receptor regulation of protein phosphatase 2A in the murine heart. (umassmed.edu)
- Adenosine A2A receptor stimulation increases angiogenesis by down-regulating production of the antiangiogenic matrix protein thrombospondin 1. (umassmed.edu)
- To test if A2AR activation in the hippocampus is actually sufficient to impair memory function and to begin elucidating the intracellular pathways operated by A2AR, we have developed a chimeric rhodopsin-A2AR protein (optoA2AR), which retains the extracellular and transmembrane domains of rhodopsin (conferring light responsiveness and eliminating adenosine-binding pockets) fused to the intracellular loop of A2AR to confer specific A2AR signaling. (universiteitleiden.nl)
- Moreover, 1 mu g/ml pertussis toxin, which inactivates the G alpha i protein subunit, reduced by 80% the negative chronotropic effects of adenosine in the NWR atrium, with minor effects in SHR tissue. (unifesp.br)
- Our potent and selective hA2A Adenosine receptor fluorescent ligand shows high affinity and selectivity for hA2A receptor (Ki =8.35 nM for hA2A receptor in radioligand binding assay). (celtarys.com)
- Of the 534 patients who received adenosine during the 20-minute period, 284 patients were identified as having dormant PV-conduction pathways. (medscape.com)
- There was no difference in the complication rates among those undergoing adenosine-guided ablation of identified pathways. (medscape.com)
- The total follow-up included 401 patients, including the 117 patients without any adenosine-identified dormant conduction pathways. (medscape.com)
- Through modulation of forward and reverse cholesterol transport pathways, adenosine can improve cholesterol balance and thereby protect macrophages from lipid overload and foam cell transformation. (medscape.com)
Levels of adenosine1
- sevelamer decreases levels of adenosine by increasing elimination. (medscape.com)
Release of adenosine1
- A 2A receptor agonists are the focus of efforts by the pharmaceutical industry to develop new cardiovascular therapies, and pharmacological actions of the atheroprotective and anti-inflammatory drug methotrexate are mediated via release of adenosine and activation of the A 2A receptor. (medscape.com)
Function of adenosine1
- Thus, in regard to stress or injury, the function of adenosine is primarily that of cytoprotection preventing tissue damage during instances of hypoxia, ischemia, and seizure activity. (wikipedia.org)
Suggest that adenosine2
- For a stress/rest protocol, adenosine does not require reversal, whereas dipyridamole requires theophylline administration to assure prompt reversal of its stress effects. (medscape.com)
- The recommended dose may be increased in patients on theophylline since methylxanthines prevent binding of adenosine at receptor sites. (wikipedia.org)
- theophylline decreases effects of adenosine by pharmacodynamic antagonism. (medscape.com)
- For patients who are able, combined low-level treadmill exercise during adenosine infusion has been demonstrated in several reports to be associated with a significant decrease in the frequency of adverse effects (eg, flushing, nausea, headache). (medscape.com)
- The dose is often decreased in patients on dipyridamole (Persantine) and diazepam (Valium) because adenosine potentiates the effects of these drugs. (wikipedia.org)
- Methylxanthines act as competitive antagonists of adenosine and can blunt its pharmacological effects. (wikipedia.org)
- green tea decreases effects of adenosine by unspecified interaction mechanism. (medscape.com)
- hawthorn increases effects of adenosine by pharmacodynamic synergism. (medscape.com)
- nicotine inhaled increases effects of adenosine by unknown mechanism. (medscape.com)
- From providing the backbone for basic energy transfer to its role in cell signaling, adenosine has such far-reaching effects as inducing vasodilation, regulating activity in the sympathetic nervous system, and reducing blood pressure and heart rate. (nfpt.com)
- The effects of N6-L-(phenylisopropyl)adenosine, cyclohexyladenosine and adenosine-5'-N-ethylcarboxamide on sleep were examined in rats. (aspetjournals.org)
- These effects consist of 1) increased slow-wave sleep2 from 6.6 to 45.7%, in all doses used for cyclohexyladenosine and adenosine-5'-N-ethylcarboxamide and for 0.1 and 0.3 mumol/kg of N6-L-(phenylisopropyl)adenosine and 2) increased values for rapid-eye-movement-sleep, amounting to 56.2 and 51.6% for 0.1 mumol/kg of cyclohexyl-adenosine and 0.3 mumol/kg of N6-L-(phenylisopropyl)adenosine, respectively. (aspetjournals.org)
- Of these four, it is the A 2A receptor that is in a large part responsible for the anti-inflammatory effects of adenosine as well as defense against excess cholesterol accumulation. (medscape.com)
- Also relevant are anti-platelet agents that decrease platelet activation and adhesion and reduce thrombotic occlusion of atherosclerotic arteries by antagonizing adenosine diphosphate-mediated effects on the P2Y12 receptor. (medscape.com)
- The purpose of this review is to discuss the effects of adenosine on cell types found in the arterial wall that are involved in atherosclerosis, to describe use of adenosine and its receptor ligands to limit excess cholesterol accumulation and to explore clinically applied anti-platelet effects. (medscape.com)
- Rationale: Adenosine A 2A antagonists can reverse many of the behavioral effects of dopamine antagonists, including actions on instrumental behavior. (elsevier.com)
- Objective: The present studies were undertaken to investigate the potential for rate-dependent stimulant effects of both selective and nonselective adenosine antagonists. (elsevier.com)
- Enzyme kinetic measurements of the effects of actin on the heavy meromyosin adenosine triphosphatase (ATPase) are used for a study of the binding of heavy meromyosin to actin. (nebraska.edu)
- The A2A receptor (A2AR) plays a central role in many antiinflammatory effects of adenosine. (elsevier.com)
- Inosine formed by deamination of adenosine can leave the cell intact or can be degraded to hypoxanthine, xanthine, and ultimately uric acid. (medlibrary.org)
- Reduced adenosine-to-inosine miR-455-5p editing promotes melanoma growth and metastasis. (phalanxbiotech.com)
- Regioselective bisphosphorylation of the primary 5'-hydroxyl groups leads to a carbocyclic, inosine analogue of seco adenosine 5'-diphosphate ribose(3). (ox.ac.uk)
- Is the Subject Area "Adenosine triphosphatase" applicable to this article? (plos.org)
- Dipyridamole potentiates the action of adenosine, requiring the use of lower doses. (wikipedia.org)
- Intravenously administered adenosine is rapidly cleared from the circulation via cellular uptake, primarily by erythrocytes and vascular endothelial cells. (medlibrary.org)
- Adenosine A2B receptor activation stimulates glucose uptake in the mouse forebrain. (bordeaux-neurocampus.fr)
- Finally, incubation of hippocampal, frontocortical, or striatal slices of C57Bl/6j mice at 37 °C, with either MRS1754 (200 nM) or adenosine deaminase (3 U/mL) significantly reduced glucose uptake. (bordeaux-neurocampus.fr)
- Adenosine uptake and tumor necrosis factor-α (TNF-α) release in cells or in retinas were determined. (thecannabisadvisory.com)
- Such properties are some of the reasons why adenosine and its derivatives are implemented in many therapeutic areas. (nfpt.com)
- Here we identify major gaps in knowledge that need to be filled to improve the therapeutic gain from agents targeting key components of the adenosine metabolic network and, on this basis, provide a holistic view of the cancer purinome as a complex and integrated network. (utu.fi)
- Intracellular adenosine may be produced by cytosolic 5'-nucleotidases or through S-adenosylhomocysteine hydrolase (also producing L-homocysteine ). (guidetopharmacology.org)
- The KsgA enzymes are homologous to another family of RNA methyltransferases, the Erm enzymes, which methylate a single adenosine base in 23S rRNA and confer resistance to the MLS-B group of antibiotics. (rcsb.org)
- Special attention is given to differences and commonalities in the purinome of different cancers, heterogeneity of the tumor microenvironment, subcellular compartmentalization of the adenosine system, and novel roles of purine-converting enzymes as targets for cancer therapy. (utu.fi)
- 3. Of these agents, NECA was observed to exhibit the greatest intrinsic activity in CHO.A2B4 cells (ca. 10 fold stimulation of cyclic AMP), while, in comparison, maximal responses to adenosine (32% NECA response), 2-chloroadenosine (61%), and APNEA (73%) were reduced. (garvan.org.au)
- Adenosine and/or NECA curves were obtained in the absence and presence of the antagonists 8-cyclopentyl-l,3-dipropylxanthine (DPCPX), 9-chloro-2-(2-furany1)-5,6- dihydro-l ,2,4-triazolo[1,5-c]quinazolin-5-imine (CGS 15943) and N6-(endonorbornan-2-yl)-9-methyladenine (N-0861). (uu.nl)
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- Adenosine is used as an adjunct to thallium (TI 201) or technetium (Tc99m) myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
- Conclusions: Resting and hyperaemic myocardial perfusion using a normalised upslope analysis during adenosine CMR is a highly reproducible technique in patients with NIDCM. (datadryad.org)
- Therefore, adenosine may represent a new approach to prevent matrix degradation and remodeling after myocardial injury. (lih.lu)
- CD39 and CD73 are ectonucleotidases that convert ATP to adenosine, elevating concentrations of adenosine locally. (tocris.com)
- The results indicate that the effect on sleep of all three adenosine analogs was obtained with nanomolar doses of the drugs and that it diminished or disappeared when the drug dose reached micromolar range (0.9 mumol/kg). (aspetjournals.org)
- Only 0.9-mumol/kg dose of cyclohexyladenosine and N6-L-(phenylisopropyl)adenosine increased wakefulness and decreased total sleep, whereas the same dose of adenosine-5'-N-ethylcarboxamide increased total sleep during the 0- to 3-hr time interval. (aspetjournals.org)
- Take adenosine as recommended and do not change its dose and frequency or stop taking it without your doctor's approval. (selfhacked.com)
- The effect was dose-dependent and was not specific to fMLP because adenosine also inhibited MMP-9 secretion by LPS- or H2O2-stimulated neutrophils. (lih.lu)
- Cellular production of adenosine is greatly enhanced in inflamed tissues, ischemic tissues and under hypoxia, where ATP is released from damaged cells. (unina.it)