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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   +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   +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   +8 more
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Cerebral A1 adenosine receptors (A1AR) in liver cirrhosis

European Journal of Nuclear Medicine and Molecular Imaging, 2007
The cerebral mechanisms underlying hepatic encephalopathy (HE) are poorly understood. Adenosine, a neuromodulator that pre- and postsynaptically modulates neuronal excitability and release of classical neurotransmitters via A(1) adenosine receptors (A(1)AR), is likely to be involved.
Boy, Christian   +10 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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A single species of A1 adenosine receptor expressed in Chinese hamster ovary cells not only inhibits cAMP accumulation but also stimulates phospholipase C and arachidonate release.

Molecular Pharmacology, 1994
Chinese hamster ovary cells were transfected with both A1 adenosine receptor and muscarinic type 3 acetylcholine receptor cDNAs. The muscarinic receptor agonist carbachol stimulated phospholipase C activity, resulting in Ca2+ mobilization and ...
M. Akbar   +4 more
semanticscholar   +1 more source

REM sleep deprivation up-regulates adenosine A1 receptors

Brain Research, 1987
Adenosine receptor binding was determined in the brains of rats deprived of rapid eye movement (REM) sleep for 48 and 96 h using [3H]L-phenylisopropyladenosine. Adenosine A1 receptors (Bmax) were significantly increased in the cortex and corpus striatum, and this increase was sleep-specific.
G, Yanik, M, Radulovacki
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