Results 221 to 230 of about 74,938 (266)

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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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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Inverse agonism at adenosine A1 receptors

International Congress Series, 2003
Abstract 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.
Rianne A.F de Ligt, Anna Lorenzen, Adriaan P IJzerman   +2 more
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Cellular localization of adenosine A1 receptors in rat forebrain: Immunohistochemical analysis using adenosine A1 receptor‐specific monoclonal antibody

The Journal of Comparative Neurology, 1999
Monoclonal antibodies were generated against the adenosine A1 receptor (A1R) purified from rat brain. In immunoblot analyses of purified or partially purified A1R preparations from rat brain, these antibodies recognized a solitary band, the size of which corresponded to that expected for A1R.
T, Ochiishi, L, Chen, A, Yukawa, Y, Saitoh, Y, Sekino, T, Arai, H, Nakata, H, Miyamoto   +7 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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Interactions between adenosine A1- and histamine H1-receptors

International Journal of Biochemistry, 1994
The interactions or "cross-talk" between adenosine A1-receptors and receptors coupled to phospholipase C (leading to the hydrolysis of inositol phospholipids) have been well documented in the literature. For example, activating the A1-receptor selectively potentiates the histamine H1-receptor stimulated hydrolysis of inositol phospholipids in guinea ...
J M, Dickenson, S J, Hill
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A novel non-xanthine adenosine A1 receptor antagonist

European Journal of Pharmacology, 1995
FK453, (+)-(R)-[(E)-3-(2-phenylpyrazolo[1,5-alpha]pyridin-3-yl) acryloyl]-2-piperidine ethanol, was examined for adenosine receptor antagonistic activity using isolated guinea-pig atria and aorta and for affinity for adenosine receptors in the rat cerebral cortex and striatum in comparison with FR113452 (S enantiomer of FK453), PD116948 (1,3-dipropyl-8-
T, Terai, Y, Kita, T, Kusunoki, T, Shimazaki, T, Ando, H, Horiai, A, Akahane, Y, Shiokawa, K, Yoshida   +8 more
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