Results 241 to 250 of about 83,344 (312)

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, ORTORE, GABRIELLA MARIA PIA, MANERA, CLEMENTINA, SACCOMANNI, GIUSEPPE, MARTINELLI, ADRIANO   +4 more
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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, MOORMAN ALLAN R., AGHAZADEH TABRIZI, Mojgan, PAVANI, Maria Giovanna, ROMAGNOLI, Romeo   +4 more
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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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Medicinal Chemistry of Adenosine A1 Receptor Ligands

Current Topics in Medicinal Chemistry, 2003
In this review the latest developments in ligand design for the adenosine A(1) receptor are summarized. Novel series of agonists and antagonists are discussed, leading to the conclusion that ligands truly selective for the human adenosine A(1) receptor are still scarce.
Willem, Soudijn, Ineke, van Wijngaarden, Ad P, IJzerman   +2 more
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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, IACONINOTO, Antonietta, MOORMAN AR, CARRION MD, CARA CL, PRETI, Delia, LOPEZ OC, FRUTTAROLO, Francesca, AGHAZADEH TABRIZI, Mojgan, ROMAGNOLI, Romeo   +9 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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Adenosine A1-receptor occupancy predicts A1-receptor antagonist effects of N-0861*

Clinical Pharmacology & Therapeutics, 1998
To evaluate the relationship between dose of N-0861 ([+/-]N6-endo-norbornan-2-yl-9-methyladenine), N-0861 plasma concentrations, and antagonism of adenosine-induced slowing of atrioventricular nodal conduction and to evaluate A1-receptor occupancy by antagonist present in plasma of subjects after administration of N-0861 to determine A1-selectivity of ...
S U, Yasuda, S, Nagashima, E, Douyon, R E, Benton, R L, Woosley, J T, Barbey   +5 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, DALPIAZ, Alessandro, VARANI, Katia, GESSI, Stefania, GILLI, Gastone   +4 more
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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, BARALDI, Pier Giovanni, ROMAGNOLI, Romeo   +2 more
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Adenosine attenuates calcium paradox injury: role of adenosine A1 receptor

American Journal of Physiology-Cell Physiology, 1995
The present study was conducted to test the hypothesis that adenosine attenuates the Ca2+ paradox (PD) injury via stimulation of adenosine A1 receptors linked to Gi proteins in the isolated rat heart. Treatment of adenosine reduced maximum lactate dehydrogenase release and ATP loss compared with regular Ca2+ PD.
J, Suleiman, M, Ashraf
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