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Adenosine A1 receptor antagonists and the kidney

Current Opinion in Nephrology and Hypertension, 2003
This 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.
Paul S, Modlinger, William J, Welch
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Allosteric modulators for the A1 adenosine receptor

Expert Opinion on Therapeutic Patents, 2004
A review. Allosteric modulators of endogenous adenosine represent an alternative to direct acting adenosine agonists and nucleoside uptake blockers. These compds. can selectively enhance the response to adenosine in only those organs or localized areas of a given organ in which prodn. of adenosine is increased. The present article is an overview of the
BARALDI, Pier Giovanni   +4 more
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Adenosine A1 receptors and erythropoietin production

American Journal of Physiology-Cell Physiology, 1993
N6-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
T, Ohigashi, J, Brookins, J W, Fisher
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Structure of the BoNT/A1 – receptor complex

Toxicon, 2015
Botulinum neurotoxin A causes botulism but is also used for medical and cosmetic applications. A detailed molecular understanding of BoNT/A--host receptor interactions is therefore fundamental for improving current clinical applications and for developing new medical strategies targeting human disorders.
Benoit, Roger M.   +6 more
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Binding of an adenosine A1 receptor agonist and adenosine A1 receptor antagonist to sheep pineal membranes

European Journal of Pharmacology, 1997
The pineal organ of vertebrates produces melatonin and adenosine. In lower vertebrates, adenosine modulates melatonin production. We report herein that 2-chloro-cyclopentyl-[3H]-adenosine ([3H]CCPA: adenosine A1 receptor agonist) and [3H]-cyclopentyl-1,3-dipropylxanthine ([3H]DPCPX: adenosine A1 receptor antagonist), bind specifically to sheep pineal ...
Falcon, J., Privat, K., Ravault, J.P.
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Allosteric modulation of A1-adenosine receptor: a review

Drug Discovery Today: Technologies, 2013
Allosteric 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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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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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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Repetitive stimulation of adenosine A1 receptors in vivo: Changes in receptor numbers, G-proteins and A1 receptor agonist-induced hypothermia

Brain Research, 2008
Adenosine is an important neuromodulator and neuroprotective molecule, which is produced in the brain as a function of neuronal activity, coupling energy expenditure to energy supply. Under conditions of increased need and reduced availability of energy, including hypoxia and prolonged wakefulness, there is an increase in adenosine turnover and ...
Roman, Viktor   +3 more
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