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A concise synthesis of a series of N6-substituted adenosines with bicyclo[3.2.1]octan-6-yl and polycyclic N6-substituents has been developed. The adenosine A1 receptor (A1R) affinity and potency of these compounds was initially assessed using competitive binding assays and cyclic adenosine monophosphate (cAMP) accumulation assays in DDT1 MF-2 cells. The potency and receptor subtype selectivity of selected examples was further evaluated by measuring their effects on cAMP accumulation at all human adenosine receptor subtypes expressed in CHO cells. The results of these assays indicated that all of the synthesised N6-substituted adenosines are full agonists at A1R and activate this receptor selectively over the other adenosine receptor subtypes. The two standout compounds in terms of potency were N6-(3-thiabicyclo[3.2.1]octan-6-yl)adenosine and N6-(cubanylmethyl)adenosine with EC50 values at human A1R of 2.3 nM and 1.1 nM, respectively. The cubanylmethyl derivative in particular proved to be highly ...

TY - JOUR. T1 - The effect of development on the pattern of A1 and A2a-adenosine receptor gene and protein expression in rat peripheral arterial chemoreceptors.. AU - Gauda, Estelle B.. AU - Cooper, Reed Z.. AU - Donnelly, David F.. AU - Mason, Ariel. AU - McLemore, Gabrielle L.. PY - 2006. Y1 - 2006. UR - http://www.scopus.com/inward/record.url?scp=33745272264&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=33745272264&partnerID=8YFLogxK. M3 - Article. C2 - 16683708. VL - 580. JO - Advances in Experimental Medicine and Biology. JF - Advances in Experimental Medicine and Biology. SN - 0065-2598. ER - ...

Adenosine is an important mediator of the endogenous defense against ischemia-induced injury in the heart. Adenosine can achieve cardioprotection by mediating the effect of ischemic preconditioning and by protecting against myocyte injury when it is present during the infarct-producing ischemia. A novel adenosine A3 receptor can mediate this protective function. One approach to achieve cardioprotection is to enhance myocardial sensitivity to the endogenous adenosine by increasing the number of adenosine receptors instead of administering an adenosine receptor agonist. The objective of the present study was to investigate whether genetic manipulation of the cardiac myocyte, achieved by gene transfer and overexpression of the human A3 receptor cDNA, renders the myocytes resistant to the deleterious effect of ischemia. Prolonged hypoxia with glucose deprivation, causing myocyte injury and adenosine release, was used to simulate ischemia in cultured chick embryo ventricular myocytes. During simulated

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Adenosine mediates many physiological functions via activation of extracellular receptors. The modulation of cell growth by adenosine was found to be receptor-mediated. In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. When both A1 and A2 receptors were blocked, colony formation or growth was not inhibited at low concentrations of adenosine but was inhibited at high adenosine concentrations ...

Intra- and extracellular adenosine levels rise in response to physiological stimuli and with metabolic/energetic perturbations, inflammatory challenge and tissue injury. Extracellular adenosine engages members of the G-protein coupled adenosine receptor (AR) family to mediate generally beneficial acute and adaptive responses within all constituent cells of the heart. In this way the four AR sub-types - A1, A2A, A2B, and A 3Rs - regulate myocardial contraction, heart rate and conduction, adrenergic control, coronary vascular tone, cardiac and vascular growth, inflammatory-vascular cell interactions, and cellular stress-resistance, injury and death. The AR sub-types exert both distinct and overlapping effects, and may interact in mediating these cardiovascular responses. The roles of the ARs in beneficial modulation of cardiac and vascular function, growth and stress-resistance render them attractive therapeutic targets. However, interactions between ARs and with other receptors, and their ubiquitous

In this function, we ask if the simultaneous motion of agonist and antagonist among surface area receptors (i. in modulating G-protein activation and receptor desensitization. Quite simply, we determine the results from the simultaneous motion of agonist and antagonist among surface area receptors for G-protein activation and receptor desensitization. A Monte Carlo model construction can be used to monitor the diffusion and result of specific receptors, allowing the necessity for receptors and G-proteins or receptors and kinases to discover one another by diffusion (collision coupling) to become applied explicitly. Simulations are accustomed to scan a wide range of circumstances and to recognize regimes which may be of experimental curiosity. Strategies Estimating the function of diffusion The reactions making GPCR activation and phosphorylation are proven schematically in Fig. 1. To be able to accurately simulate these reactions, we initial determine which bimolecular reactions will tend to be ...

The report displayed here plans showcase players to make steady progress while adequately managing one of a kind difficulties in the worldwide Adenosine advertise. The examiners and analysts creating the report have thought about different elements anticipated to emphatically and contrarily sway the worldwide Adenosine advertise. The report incorporates SWOT and PESTLE investigations to give a more profound comprehension of the worldwide Adenosine advertise. The entirety of the main organizations remembered for the report are profiled dependent on net edge, piece of the overall industry, tentative arrangements, late advancements, target client socioeconomics, items and applications, and other basic variables. The report additionally offers local examination of the Adenosine advertise with high spotlight on showcase development, development rate, and development potential. Top Players Considered in Global Builders and Adenosine Market :- , Yamasa, Meihua Group, Tuoxin, Mingxin Pharmaceuticla, ...

Synonyms for adenosine 5'-diphosphate in Free Thesaurus. Antonyms for adenosine 5'-diphosphate. 1 synonym for adenosine diphosphate: ADP. What are synonyms for adenosine 5'-diphosphate?

Read A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics by with Rakuten Kobo. This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide ...

The protein encoded by this gene is an adenosine receptor that belongs to the G-protein coupled receptor 1 family. There are 3 types of adenosine receptors, each with a specific pattern of ligand binding and tissue distribution, and together they regulate…

A nucleoside that is composed of adenine and d-ribose. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.

Adenosine is a ubiquitous signaling molecule whose physiological functions are mediated by its interaction with four G-protein-coupled receptor subtypes, termed A(1), A(2A), A(2B) and A(3). As a result of increased metabolic rates, this nucleoside is released from a variety of cells throughout the b …

Breakdown of excessive amounts of adenosine triphosphate (ATP), the main energy source of a cell, leads to the formation of extracellular adenosine, an important signaling molecule involved in multiple pathways that regulate neuronal and immunological function. Adenosine is either actively produced by certain cells or is released from damaged tissue, particularly when cells are starved of oxygen. Adenosine levels are tightly regulated at all points throughout its production, release, uptake and degradation, and disruptions in control that result in excessively high levels are associated with a number of human pathologies, including severe combined immunodeficiency (SCID).. The diversity in the regulation and function of adenosine (both of which differ in a tissue- and cell-specific manner) means that it has been difficult to unravel its exact role at the molecular level. In addition, data obtained in vitro, or in tissue culture, might not be relevant to whole organisms, and mammalian model ...

Adenosine Sanolabor is a medicine available in a number of countries worldwide. A list of US medications equivalent to Adenosine Sanolabor is available on the Drugs.com website.

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Adora1 - Adora1 (untagged) - Mouse adenosine A1 receptor (cDNA clone MGC:90841 IMAGE:30536680), (10ug) available for purchase from OriGene - Your Gene Company.

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Mechanisms involved in increased sensitivity to adenosine A2A receptor activation and hypoxia-induced vasodilatation in porcine coronary ...

duralone ATP injection(Adenosine Tri-Phosphate) is utilized in the Krebs Cycle - which physiologically is one of the key providers of duralone ATP

Adenosine is so readily formed in the brain that for some time its quantity there was overestimated by a factor of 20 or more (Berne et al. 1974; Newman and McIlwain, 1977). Now, rapid fixation...

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Note:Only the main profile, including all conditions, is shown. Additional statistics and tissue specific profiles are available here.. ...

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This study demonstrates that three structurally distinct A1 receptor antagonists increase extracellular adenosine levels in two different types of cardiovascular cells, i.e., cardiac fibroblasts and vascular smooth muscle cells, and in two species, rats and humans. The extracellular adenosine responses to A1 receptor antagonists are concentration dependent, and are attenuated by pertussis toxin, a toxin that inactivates inhibitory G proteins, and by AMPCP, an inhibitor of ecto-5′-nucleotidase. This study also demonstrates that augmentation of extracellular adenosine levels attenuates the increase in extracellular adenosine induced by A1 receptor antagonists. Finally, this study shows that the effects of A1receptor antagonists on extracellular adenosine levels develop with a time lag of several hours.. Our working hypothesis is that high-affinity A1receptors detect elevated levels of adenosine in the biophase of the cell surface and engage a signal transduction process that ultimately decreases ...

Our work demonstrates that human endothelial cells of disparate origin are characterized by differential expression of adenosine receptor subtypes. HUVECs express mRNA for A2A and A2B receptors at a ratio of 10:1, and this preferential gene expression agrees well with the typical pharmacological phenotype of A2A receptor-mediated simulation of adenylate cyclase by adenosine analogs. Using complementary techniques, RT-PCR, and gene expression array, we found that A1 and A3 adenosine receptors are not expressed in HUVECs. Previous studies in HUVECs have suggested a potential role of A1 receptor in maintaining endothelial barrier function4 and of A1 and A3 receptors in modulation of tissue factors expression.6 The apparent contradiction between these results and ours can be explained by the use of nonselective concentrations of adenosine receptor ligands in previous studies.. HMEC-1 also express only A2A and A2B mRNA, but in contrast to HUVECs, they express predominantly A2B receptor mRNA, with a ...

TY - JOUR. T1 - Microwave-assisted and conventional synthesis of benzothieno [3,2-e] [1,3,4] triazolo[4,3-c]pyrimidines. T2 - A comparative study. AU - Gaonkar, Santhosh L.. AU - Ahn, Chuljin. AU - Princia, AU - Shetty, Nitinkumar S.. PY - 2014/8/20. Y1 - 2014/8/20. N2 - Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4] triazolo[4,3-c] pyrimidines (5a-c) were synthesized from the precursor 2-amino-7-oxo-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile 1 by employing the conventional method as well as the microwave irradiation technique. The precursor 2-amino-3-cyanothiophene analogue 1 was synthesized by employing the well-known Gewald reaction. In the present work it has been found that the microwave supported syntheses are more efficient than the conventional classical heating methods. The structures of all the compounds were ascertained by spectral and analytical data.. AB - Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4] triazolo[4,3-c] pyrimidines ...

The review summarizes data evaluating the role of adenosine receptor signaling in murine hematopoietic functions. The studies carried out utilized either non-selective activation of adenosine receptors induced by elevation of extracellular adenosine or by administration of synthetic adenosine analogs having various proportions of selectivity for a particular receptor. Numerous studies have described stimulatory effects of non-selective activation of adenosine receptors, manifested as enhancement of proliferation of cells at various levels of the hematopoietic hierarchy. Subsequent experimental approaches, considering the hematopoiesis-modulating action of adenosine receptor agonists with a high level of selectivity to individual adenosine receptor subtypes, have revealed differential effects of various adenosine analogs. Whereas selective activation of A(1) receptors has resulted in suppression of proliferation of hematopoietic progenitor and precursor cells, that of A(3) receptors has led to ...

In this report we show that it is possible to detect the expression of a G protein-coupled receptor, the A2AR, in human lymphocytes both on the basis of a functional assay (cAMP accumulation) and by flow cytometry using an antireceptor mAb. We were able to describe for the first time the distribution of A2AR among minor T cell subpopulations through the use of a combination of anti-A2AR mAb and mAbs that recognize T cell surface markers or cytokines. The principle findings of this study are that much higher levels of A2AR expression is found in T cells than in B cells (Fig. 3) and higher levels of cytokines are detected in activated T cells that express A2AR than in activated T cells that do not express these receptors (Figs. 6 and 7).. The detection of higher levels of cytokines among A2AR+ cells is surprising because A2AR-mediated signaling antagonizes the effects of T cell activation (Koshiba et al., 1997; Huang et al., 1997). Therefore, we expected that cytokine secretion would be the lowest ...

The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of ...

In the heart, endogenous adenosine attenuates the beta-adrenergic-elicited increase in contractile performance via activation of adenosine A1 receptors. It has been recently reported that this function of adenosine becomes more pronounced with myocardial maturation. The purpose of the present study was to determine whether mature hearts possess a greater sensitivity than immature hearts to this antiadrenergic effect of adenosine. Isolated perfused hearts or atria from immature (ca. 23 days) and mature (ca. 80 days) rats were stimulated with isoproterenol (Iso), a beta-adrenergic agonist, at 10(-8) M and concomitantly exposed to increasing concentrations of 2-chloro-N6-cyclopentyladenosine (CCPA), a highly selective and potent adenosine A1-receptor agonist, from 10(-12) to 10(-6) M. CCPA at 10(-10)-10(-6) M dose dependently reduced the Iso-elicited contractile response more in immature than in mature hearts or atria. At 10(-6) M, CCPA reduced the Iso-elicited contractile response by 103% in immature

In this study and previously (24), we have demonstrated that blockade of the A2AAR with an A2A-specific AR antagonist protected mice from EAE by hindering lymphocyte entry into the brain and spinal cord of wild-type mice. This finding was unexpected, as this function of adenosine, that is, mediating lymphocyte migration into the CNS, was previously unknown. Furthermore, the facts that adenosine suppresses the immune response and resolves inflammation (2) are at odds with the finding that blockade of the A2AAR, which mediates the preponderance of adenosines suppressive and anti-inflammatory functions (2), protects mice from EAE (24). The purpose of this study was to delineate adenosines role in the immune response from its function in mediating immune cell migration into the CNS via the A2A receptor.. We show that A2AAR−/− mice developed more severe EAE than did their wild-type counterparts. This severe disease was characterized in the CNS by increased numbers of lymphocytes and activated ...

1-1H-Indol-7-yl-3-[5-(2-{thieno[3,2-d]pyrimidin-4-ylamino}ethyl)-1,3-thiazol-2-yl]urea | C20H17N7OS2 | CID 25138117 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.

Synonyms for adenosine triphosphatase test in Free Thesaurus. Antonyms for adenosine triphosphatase test. 2 words related to adenosine: biochemistry, nucleoside. What are synonyms for adenosine triphosphatase test?

Two main findings arise from this study: (1) the adenosine A2A receptor antagonist SCH 58261 shows neuroprotective effects in an excitotoxic rat model of HD; and (2) the inhibition of QA-evoked increase in extracellular glutamate seems to be the main mechanism of the effects elicited by SCH 58261.. The finding that SCH 58261 significantly prevented most of the effects induced by the intrastriatal injection of an excitotoxin is in line with some findings suggesting that activation of A2A receptors could participate in the generation of excitotoxicity. Adenosine A2A receptor agonists have been reported indeed to stimulate glutamate release in the rat striatum (Popoli et al., 1995; Corsi et al., 1999). Moreover, in previous experiments, we observed that the intrastriatal injection of the adenosine A2A receptor agonist CGS 21680, together with QA, potentiated QA-induced mortality in a dose-dependent way (50, 75, and 83% of mortality after 3, 6, and 12 nmol QA plus CGS 21680, respectively; P. Popoli, ...

Cyclic AMP; 35-cyclic AMP; 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide; Acrasin; Adenosine 3,5-cyclic monophosphate; Adenosine 3,5-cyclic phosphate; Adenosine 3,5-cyclophosphate; Adenosine 3,5-monophosphate; Adenosine 3,5-cyclic monophosphorate; Adenosine 3,5-cyclic monophosphoric acid; Adenosine cyclic monophosphate; Cyclic 3,5-AMP; Cyclic 3,5-adenylate; Cyclic 3,5-adenylic acid; Cyclic adenosine 3,5-phosphate; adenosine cyclic-monophosphate; adenosine-cyclic-phosphate; adenosine-cyclic-phosphoric-acid; ...

Cyclic AMP; 35-cyclic AMP; 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide; Acrasin; Adenosine 3,5-cyclic monophosphate; Adenosine 3,5-cyclic phosphate; Adenosine 3,5-cyclophosphate; Adenosine 3,5-monophosphate; Adenosine 3,5-cyclic monophosphorate; Adenosine 3,5-cyclic monophosphoric acid; Adenosine cyclic monophosphate; Cyclic 3,5-AMP; Cyclic 3,5-adenylate; Cyclic 3,5-adenylic acid; Cyclic adenosine 3,5-phosphate; adenosine cyclic-monophosphate; adenosine-cyclic-phosphate; adenosine-cyclic-phosphoric-acid; ...

Since their discovery approximately 25 years ago, adenosine receptors have now emerged as important novel molecular targets in disease and drug discovery. These proteins play important roles in the entire spectrum of disease from inflammation to immune suppression. Because of their expression on a number of different cell types and in a number of different organ systems they play important roles in specific diseases, including asthma, rheumatoid arthritis, Parkinsons disease, multiple sclerosis, Alzheimers disease, heart disease, stroke, cancer, sepsis, and obesity. As a result of intense investigations into understanding the molecular structures and pharmacology of these proteins, new molecules have been synthesized that have high specificity for these proteins and are now entering clinical trials. These molecules will define the next new classes of drugs for a number of diseases with unmet medical needs.

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Orthoplex Adenosine 60 Tablets contains 100mg of adenosine. Orthoplex Adenosine plays a major role in the production of cellular energy ATP

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Structure, properties, spectra, suppliers and links for: 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide.

6-Amino-1,3-dihydro-2H-purin-2-one; CAS Number: 3373-53-3; Linear Formula: C5H5N5O; find Ambeed, Inc.-AMBH46A96504 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich

You are viewing an interactive 3D depiction of the molecule 5-o-(4,6-dihydroxy-2,4,6-trioxido-1,3,5,2,4,6-trioxatriphosphinan-2-yl)adenosine (C10H14N5O12P3) from the PQR.

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The A3 adenosine receptor (A3AR) has emerged as a therapeutic goal with A3AR agonists to deal with the worldwide problem of neuropathic ache; investigation into their mode of motion is important for ongoing medical growth. A3ARs on immune cells, and their activation throughout pathology, modulates cytokine launch. Thus, immune cells as a mobile substrate for. Read More ...

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What is the molecular mechanism by which lack of adenosine receptor signaling results in a pro-calcific phenotype, and are these pathways applicable to calcification seen in more common diseases ...

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II. CÍL NÁVRHU. Cílem návrhu je umožnit novým členským státům účast v projektu Evropské hlavní město kultury před skončením platnosti stávajícího rozhodnutí v roce 2019. Návrh nemění stávající pořadí pro podávání návrhů členskými státy, ale zavádí se nový systém jmenování dvou členských států oprávněných každý rok počínaje rokem 2009 podat návrhy tak, aby v členských státech mohla být vybrána dvě hlavní města.. III. ROZBOR SPOLEČNÉHO POSTOJE. 1. Obecné poznámky. Rada v návrhu Komise neprovedla žádné změny. Komise zcela přijala 1 změnu z 5 změn navrhovaných Parlamentem (změna 1).. 2. Změny učiněné Evropským parlamentem. 2.1 Změny přijaté Radou. Rada plně potvrdila změnu navrhovanou Parlamentem a přijatou Komisí (změna 1).. 2.2 Změny nezapracované Radou. Rada stejně jako Komise usoudila, že změny 2, 3, 4 a 5 šly nad rámec návrhu, a jejich zapracování nepokládala za vhodné.. III. ZÁVĚRY. Rada se ...

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Genetic information processingProtein synthesistRNA and rRNA base modificationtRNA threonylcarbamoyl adenosine modification protein YeaZ (TIGR03725; HMM-score: 178.6) ...

AKI 1 is an adenosine regulating agent. It was undergoing preclinical studies in the USA with Gensia Sicor for the treatment of inflammatory disorders, however

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