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Binding thermodynamics at A1 and A2a adenosine receptors

Life Sciences, 1996
Only 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, 2022
Adenosine, 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 Enhancers for A1 Adenosine Receptor

Mini-Reviews in Medicinal Chemistry, 2007
Allosteric 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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Adenosine receptors and cardiovascular disease: the adenosine-1 receptor (A1) and A1 selective ligands.

Cardiovascular toxicology, 2004
Adenosine has often been cited as a universal retaliatory metabolite against the destructive cellular mechanisms that are initiated during metabolic/oxidative stress. Despite this billing, clinical application of adenosine has been limited to rather specific cardiovascular indications (e.g., paroxysmal supraventricular tachycardia).
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Effects of enprofylline on A1 and A2 adenosine receptors

European Journal of Pharmacology, 1985
The effects of enprofylline were studied on A1 adenosine receptors of rat fat cells and on A2 adenosine receptors of human platelets and of guinea-pig lung. Enprofylline antagonized the 5'-N-ethylcarboxamidoadenosine (NECA)-induced stimulation of platelet adenylate cyclase activity with a KB of 130 microM.
D, Ukena, C G, Schirren, U, Schwabe
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Desensitization of A1 Adenosine Receptors

1995
It is well known that exposure of sensitive cells to receptor agonists can cause a progressive reduction in their capacity to respond to this and related agonists. This phenomenon has been observed with cells expressing receptors from different superfamilies, and has been termed desensitization, refractoriness,tolerance, or tachyphylaxis [1].
Edmund Hoppe, Martin J. Lohse
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Alterations of adenosine A1 receptors in morphine dependence

Brain Research, 1994
The 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 ...
G B, Kaplan   +2 more
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Adenosine receptor modelling. A1/A2a selectivity

European Journal of Medicinal Chemistry, 2006
Three-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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Partners for adenosine A1 receptors.

Journal of molecular neuroscience : MN, 2005
G protein-coupled receptors (GPCRs) are targets for therapy in a variety of neurological diseases. Using adenosine A1 receptors (A1Rs) as paradigm of GPCRs, this review focuses on how protein-protein interactions, from monomers to heteromers, can contribute to hormone/neurotransmitter/neuromodulator regulation.
Franco R   +9 more
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Affinity chromatography in purification of A1 adenosine receptors

Journal of Chromatography A, 1992
Purification of A1 adenosine receptor of rat brain membranes was performed using a newly developed affinity gel employing xanthine amine congener (XAC) as an immobilized ligand. The A1 adenosine receptor was solubilized with digitonin-cholate from brain membranes and then purified by a sequential use of affinity chromatography on XAC-agarose ...
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