Results 251 to 260 of about 119,693 (290)
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Adenosine A1 receptors and erythropoietin production
American Journal of Physiology-Cell Physiology, 1993N6-cyclopentyladenosine (CPA), a selective adenosine A1 receptor agonist, in a concentration range of 10(-9) to 10(-7) M, produced a significant decrease in erythropoietin (EPO) levels in a human hepatocellular carcinoma (Hep G2) cell culture (medium levels of EPO, 91.81 +/- 1.61 and 94.36 +/- 0.97% of control, respectively) after 24 h incubation in a
James W. Fisher+2 more
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Adenosine A1 receptor antagonists and the kidney
Current Opinion in Nephrology and Hypertension, 2003This review will examine the most recent evidence that adenosine receptors in the kidney can alter kidney function. Adenosine A(1)-receptors located in the afferent arteriole and proximal tubule can contribute to fluid retaining disorders by mediating tubuloglomerular feedback, afferent arteriole vasoconstriction or direct sodium absorption.
William J. Welch, Paul S Modlinger
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Binding thermodynamics at A1 and A2a adenosine receptors
Life Sciences, 1996Only recently the binding equilibrium of a number of ligands at adenosine A1 and A2a receptors has been analyzed from a thermodynamic point of view. This approach presents the advantage, with respect to usual affinity constant measurements, of a greater capability to give information about the molecular mechanisms underlying the binding process.
BOREA, Pier Andrea+4 more
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The role of adenosine A1 receptor on immune cells
Inflammation Research, 2022Adenosine, acting as a regulator by mediating the activation of G protein-coupled adenosine receptor families (A1, A2A, A2B, and A3), plays an important role under physiological and pathological conditions. As the receptor with the highest affinity for adenosine, the role of adenosine A1 receptor (A1R)-mediated adenosine signaling pathway in the ...
Lingyu, Zhong, Qiao, Peng, Xun, Zeng
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Allosteric modulation of A1-adenosine receptor: a review
Drug Discovery Today: Technologies, 2013Allosteric modulators of adenosine receptors represent an alternative to direct-acting adenosine agonists and nucleoside uptake blockers, preferably those can selectively modulate the response to adenosine in only those organs or localized areas of a given organ in which production of adenosine is increased.
M. Kimatrai Salvador+2 more
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Adenosine receptor modelling. A1/A2a selectivity
European Journal of Medicinal Chemistry, 2006Three-dimensional models of the A(1) and A(2a) adenosine receptors (AR) were constructed by means of a homology procedure, using bovine rhodopsin as a template. In order to validate the two models, a docking analysis of selective agonists was carried out.
TUCCINARDI, TIZIANO+4 more
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4 The Adenosine A1 Receptor and its Ligands
2009Publisher Summary This chapter discusses the adenosine A1 receptor and its ligands. The adenosine A1 receptor is a G-protein-coupled receptor of about 36 kDa with even transmembrane domain structure. Adenosine and adenosine A1 receptors are involved in the modulation of several physiological effects in heart, kidney, CNS, and lipid metabolism ...
Barbara Albrecht-Küpper, Peter Nell
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Allosteric Enhancers for A1 Adenosine Receptor
Mini-Reviews in Medicinal Chemistry, 2007Allosteric enhancers at the adenosine A(1) receptor have received attention as anti-arrhythmic cardiac agents, and, more recently, as anti-lipolytic agents. In addition, allosteric modulators at the adenosine A(1) receptor have therapeutic potential as analgesics and neuroprotective agents.
BARALDI, Pier Giovanni+9 more
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Inverse agonism at adenosine A1 receptors
International Congress Series, 2003Abstract Inverse agonism at adenosine A1 receptors was studied in a variety of experimental set-ups. As a read-out, the binding of [35S]GTPγS to membranes of either CHO or COS-7 cells expressing human adenosine A1 receptors was used. When wild-type receptors were studied, inverse agonism could only be detected at higher levels of receptor expression.
Anna Lorenzen+2 more
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Alterations of adenosine A1 receptors in morphine dependence
Brain Research, 1994The possibility that central adenosine A1 and A2a receptors mediate opiate dependence was examined in morphine-treated mice using radioligand binding methods. Mice treated with morphine for 72 h demonstrated significant increases in naloxone precipitated abstinence behaviors of jumping, wet-dog shakes, teeth chattering, forepaw trends, forepaw tremors ...
Gary B. Kaplan+2 more
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