In a recent prospective, double-blind, randomized multicenter phase 3 trial, ADVANCE (Adenosine versus Regadenoson Comparative Evaluation for Myocardial Perfusion Imaging), the A2A selective adenosine receptor agonist, regadenoson, was shown to be noninferior to the nonselective vasodilator, adenosine, for detecting myocardial ischemia (1). The overall visual agreement was comparably low (in the low 60% range) for the adenosine-regadenoson and for the adenosine-adenosine comparisons. Conversely, when quantitative analysis was applied, regadenoson induced virtually identical results to adenosine-regarding the size and severity of left ventricular perfusion defect size and extent of ischemia (2). What are the regulatory implications of these findings? Should the regulatory bodies rely on subjective visual interpretation of myocardial perfusion studies, on objective quantitative programs to appraise the comparability between vasodilators, or both? What is the true standard?. In order to avoid the ...

The ITU World Radiocommunication Conference 2012 (WRC-12) ran between 23 January and 17 February 2012, but preparation started shortly after the previous Conference, WRC-07 set its agenda.. A key Agenda Item was AI-1.23 - 500kHz. The result was the creation of the 472-479kHz allocation to the service. It also set the agenda for the following conference, WRC-15, which considered a 5MHz allocation.. Here you will find reports on the progress of the WRC-12 Conference from UK/RSGB delegate Colin Thomas G3PSM ...

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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 ...

Effects of adenosine receptor agonists of the A1, A2A and A3 subtypes on the proinflammatory activity of human neutrophils in ...

A series of new 2-alkynyl and 2-cycloalkynyl derivatives of adenosine-5-N-ethyluronamid(NECA) and of N-ethyl-l-deoxy-l-(6-amino-2-hexynyl-9H-purin-9-yl)-b-D-ribofuranuronamid(1e, HENECA), bearing hydroxy, amino, chloro, and cyano groups in the side chain, were synthesized. The compounds were studied in binding and functional assays to assess their potency for the A2 compared to A1 adenosine receptor. The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to compounds endowed with sub-nanomolar affinity in binding studies. However, these analogues also possess good A1 receptor affinity resulting in low A2 selectivity. From functional experiments the 4-hydroxy-l-butynyl(6) and the 4-(2-tetrahydro-2H-pyranyloxy)-l-butynyl (16) derivatives appear to be very potent in inducing vasorelaxation without appreciable effect on heart rate. The new compounds were also tested as inhibitors of platelet aggregation induced by ADP. ...

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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 ...

... -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

Thank you for sharing this Journal of Pharmacology and Experimental Therapeutics article.. NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.. ...

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Letter Letter to FCC Chairman Pai Requesting any Technical Analysis that the FCC has Conducted or Reviewed on Out-of-Band Emissions Limits Follow up to September 30 Letter Sent to FCC Chairmain Pai Attachments U.S. Proposal on WRC-19 Agenda Item 1.13, submitted by FCC on March 19 Slide deck from the 3rd ITU Inter-regional Workshop on WRC-19 Preparation, dated September 5, 2019 Study prepared by NOAA and NASA, Results from NASA/NOAA Sharing Studies on WRC-19 Agenda Item 1.13 Study … Continue Reading September 12, 2019 ...

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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 ...

Recent evidence indicates that topical application of adenosine A(2A) receptor agonists, unlike growth factors, increases the rate at which wounds close in normal animals and promotes wound healing in diabetic animals as well as growth factors, yet neither the specific adenosine receptor involved no …

37] Liaison statement to Joint Task Group 4-5-6-7 (copy to Working Parties (4A, 4B, 4C 5B, 5C, 5D, 6A, 7B, 7C, 7D, 1A, 3K, 3M) for information) - WRC-15 Agenda item 1.1 - Sharing considerations for the 5-6 GHz frequency range for WRC-15 Agenda item 1.1 ...

ITU HFBC software is consistent with the general principles set out in Article 12 and the specifications in Res.535(Rev.WRC-03) . It was developed in close consideration with Administrations, broadcasters, and existing HFBC regional coordination groups. ...

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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 ...

The involvement of a guanine-nucleotide-binding regulatory protein (G protein) in the relaxing responses to adenosine receptor agonists was investigated in bovine coronary vessels. Ring segments of left anterior descending artery branches were suspended in organ baths for measurement of isometric tension. The adenosine analogs, 5-N-ethylcarboxamidoadenosine (NECA) and 2-chloroadenosine (CAD) caused concentration-dependent relaxations of coronary rings contracted with KCl. The relaxing effects of NECA and CAD were antagonized by the adenosine receptor antagonist 8-phenyltheophylline indicating the involvement of an adenosine receptor. In a separate series of experiments, incubation with cholera toxin inhibited the relaxing responses to NECA, CAD and isoproterenol but not those produced by sodium nitroprusside. Treatment with forskolin did not reduce the relaxing responses to NECA or CAD. N-ethylmaleimide and NaF/AlCl3 caused significant inhibition of the relaxations produced by both NECA and ...

Corresponding Author: Anaclet Ngezahayo Department of Cell Physiology and Biophysics, Institute of Cell Biology and Biophysics, Leibniz University Hannover, Herrenhäuser Straße 2, Hannover, 30419 (Germany ...

SMC announces that Can-Fite BioPharma has published the results of a study using STAM™ model in International Journal of Molecular Medicine.. Title: The A3 adenosine receptor agonist, namodenoson, ameliorates non-alcoholic steatohepatitis in mice. The A3 adenosine receptor agonist, namodenoson, ameliorates non‑alcoholic steatohepatitis in mice (spandidos-publications.com). ...

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Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.

Agenda Item 1.23 - 500kHz Progress through Committee 4 (COM4) was a little easier than expected and the frequency band 472-479kHz will be allocated to the amateur service, on a Secondary basis. This is subject to no further objections being received during the two final readings through the plenary meetings, of which the first blue reading is […]. Continue Reading. ...

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人們在19世紀末時同時使用著三個不同的電單位制，分別為：CGS靜電單位制，又稱高斯單位制，簡稱ESU；CGS電機械單位，簡稱EMU；以及用於配電系統的米-千克-秒制（國際單位制）。[24]在試圖根據因次分析用長度、質量及時間表達電單位時，科學家遇到了諸多困難──在使用ESU或EMU時，物理量會具有不同的因次。[16]1900年，喬瓦尼·吉奧爾吉（英语：Giovanni Giorgi）發表了一篇論文，提倡在當時的三個基本單位以外，再加一個基本單位，電單位不一致的問題迎刃而解。這第四個單位可以是電流、電壓和電阻中的其中一個。[25]. 19世紀後期至20世紀初期，人們採用了一系列不一致的單位制，在質量上有的用克，有的用公斤；在長度上有的用厘米，有的用米。例如有：表達功率的「Pferdestärke」（公制馬力）、[26][註 3]表達滲透性（英语：Permeability (earth ...

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 ...

Nicholls, J, Skene, DJ and Hourani, SMO (1997) Use of a newly developed technique to isolate rat pinealocytes and study the effects of adenosine agonists on melatonin production ...

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This is a pretty good hit rate. Generally virtual screening campaigns are lucky to have a hit rate of a few percent. Curiously, the authors also found a similarly high hit rate during a past VS campaign against the well-known β2 adrenergic receptor. What could be responsible for this high hit rate against GPCRs? The reasons are interesting. One reason could be that GPCRs are very well adapted to bind small molecules in compact pockets, enclosing them and forming many kinds of productive interactions. But more intriguingly, as the authors have noted earlier, there is biogenic bias in favor of certain target-specific chemotypes in commercial libraries that are screened, both during VS as well as HTS. This in turn reflects the biases of medicinal chemists in picking and synthesizing certain kinds of chemotypes based on the importance of drug targets and past successes in hitting these targets. GPCRs clearly are enormously important, and GPCR-friendly ligand chemotypes thus constitute a large ...

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Adenosine acts as a break in biological systems, having inhibiting effects, but caffeine doesnt just stop this break, it also makes other neurotransmitters more active. For instance, it prevents breakdown of acetylcholine (ACh), so ACh sticks around longer, increasing its effect ...

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