Results 261 to 270 of about 119,693 (290)
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Adenosine A1, but not A2, receptor blockade increases anxiety and arousal in Zebrafish.
Basic & Clinical Pharmacology & Toxicology, 2011Adenosinergic systems have been implicated in anxiety-like states, as caffeine can induce a state of anxiety in human beings. Caffeine is an antagonist at A(1) and A(2) adenosine receptors but it remains unclear whether anxiety is mediated by one or both
C. Maximino +4 more
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Medicinal Chemistry of Adenosine A1 Receptor Ligands
Current Topics in Medicinal Chemistry, 2003In 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.
Ad P. IJzerman +2 more
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The structure and function of A1 and A2B adenosine receptors
Life Sciences, 1998Of the four G protein coupled adenosine receptor (AR) subtypes, the A1 is best suited for studies of reconstitution with G proteins. Recombinant A1 receptors extended with hexahistidine and FLAG have been purified to near homogeneity. In reconstitution assays using pure recombinant G protein subunits, the composition of the gamma subunit influences ...
Joel Linden +3 more
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Effects of enprofylline on A1 and A2 adenosine receptors
European Journal of Pharmacology, 1985The 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.
Ulrich Schwabe +2 more
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A “locked-on,” constitutively active mutant of the adenosine A1 receptor
European Journal of Pharmacology, 2005We studied the wild-type human adenosine A1 receptor and three mutant receptors, in which the glycine at position 14 had been changed into an alanine, a leucine, or a threonine residue. All receptors were characterized in radioligand binding experiments, the wild-type and the Gly14Thr mutant receptor in greater detail.
Rob Leurs +4 more
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Affinity chromatography in purification of A1 adenosine receptors
Journal of Chromatography A, 1992Purification 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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Modulation of A1 adenosine receptor signaling by peroxynitrite
Biochemical Pharmacology, 2004Nitric oxide (NO) is a gaseous free radical involved in many pathophysiological processes. During oxidative stress, NO, its derivatives and adenosine are released. Considering adenosine neuroprotective role in the central nervous system (CNS) and toxicity of NO, we investigated the effect of a NO/peroxynitrite (ONOO(-)) donor, 3-morpholinosydnonimine ...
Giuntini J +3 more
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A1 Adenosine Receptor: Role in Diabetes and Obesity
2009Adenosine mediates its diverse effects via four subtypes (A(1), A(2A), A(2B) and A(3)) of G-protein-coupled receptors. The A(1) adenosine receptor (A(1)AR) subtype is the most extensively studied and is well characterized in various organ systems. The A(1)ARs are highly expressed in adipose tissue, and endogenous adenosine has been shown to tonically ...
Jeffrey W. Chisholm +3 more
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Adenosine A1-receptor occupancy predicts A1-receptor antagonist effects of N-0861*
Clinical Pharmacology & Therapeutics, 1998To 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 ...
Satoru Nagashima +5 more
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A1 Adenosine Receptors in Human Neutrophils
1998Adenosine is an ubiquitous nucleoside that mediates several important physiological effects, trough the binding of three pharmacologically distinct receptor subtypes, named A1 A2 and A 3 .1 Adenosine receptor subtypes has been distinguished on the basis of the effect of adenosine on the cellular content of cAMP: occupancy of A2 adenosine receptors ...
MARTINI, CLAUDIA +7 more
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