Upregulation of A2A adenosine receptor expression by TNF-α in PBMC of patients with CHF: a regulatory mechanism of inflammation

2005 ◽  
Vol 11 (1) ◽  
pp. 67-73 ◽  
Author(s):  
Pier leopoldo Capecchi ◽  
Alessandra Camurri ◽  
Gerarda Pompella ◽  
Alessia Mazzola ◽  
Massimo Maccherini ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Regulatory Mechanism ◽  
Receptor Expression ◽  
A2a Adenosine Receptor ◽  
Tnf Α

scholarly journals Lipopolysaccharide rapidly modifies adenosine receptor transcripts in murine and human macrophages: role of NF-κB in A2A adenosine receptor induction

2005 ◽  
Vol 391 (3) ◽  
pp. 575-580 ◽  
Author(s):  
Lauren J. Murphree ◽  
Gail W. Sullivan ◽  
Melissa A. Marshall ◽  
Joel Linden
Keyword(s):  
Adenosine Receptor ◽  
Acid Methyl Ester ◽  
Fold Increase ◽  
Nuclear Factor Κb ◽  
Receptor Expression ◽  
A2a Adenosine Receptor ◽  
Monocytic Cell ◽  
Human Macrophages ◽  
Primary Mouse ◽  
Receptor Number

The A2A adenosine receptor (A2AAR) mediates anti-inflammatory actions of adenosine in a variety of cell types. LPS (lipopolysaccharide) was reported to induce a small (<2-fold) increase in the expression of A2AAR mRNA in human monocytes and monocytic cell lines. We investigated the effects of LPS on the expression of adenosine receptor mRNAs in primary mouse IPMΦ (intraperitoneal macrophages), human macrophages and Wehi-3 cells. Treatment with 10 ng/ml LPS for 4 h produced a >100-fold increase in A2AAR mRNA. LPS-induced increases in mRNA for A2AAR and TNFα (tumour necrosis factor α) are reduced by 90% in IPMΦ pretreated with the NF-κB (nuclear factor κB) inhibitor, BAY 11-7082 {(E)3-[(4-methylphenyl)sulphonyl]-2-propenenitrile; 10 μM}. In Wehi-3 cells exposed to LPS, A2AAR and A2BAR transcripts are elevated by 290- and 10-fold respectively, the A1AR transcript is unchanged and the A3AR transcript is decreased by 67%. The induction of A2AAR mRNA by LPS is detectable after 1 h, reaches a peak at 6 h at 600 times control and remains elevated beyond 24 h. The ED50 (effective dose) of LPS is 2.3 ng/ml. A2AAR receptor number, measured by 125I-ZM241385 binding to whole cells, is undetectable in naïve cells and increases linearly at a rate of 23 receptors·cell−1·min−1 to a Bmax of 348 fmol/mg (28000 receptors/cell) in 20 h. The increase in receptor number is correlated with an increase in the potency of an A2A agonist (4-{3-[6-amino-9-(5-ethylcarbamoyl-3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-cyclohexanecarboxylic acid methyl ester; referred to as ATL146e) to stimulate cAMP in these cells. After LPS pretreatment, the potency of the A2A agonist, ATL146e, to reduce TNFα release from IPMΦ was increased by 200-fold. The results support the hypothesis that regulation of adenosine receptor expression, especially up-regulation of the A2AAR, is part of a delayed feedback mechanism initiated through NF-κB to terminate the activation of human and mouse macrophages.

Relationship between A2A Adenosine Receptor Expression and Intradialytic Hypotension during Hemodialysis

2006 ◽  
Vol 54 (8) ◽  
pp. 473-477 ◽  
Author(s):  
Philippe Giaime ◽  
Louis Carrega ◽  
Emmanuel Fenouillet ◽  
Laurence Mercier ◽  
Victoria Gerolami ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Receptor Expression ◽  
Intradialytic Hypotension ◽  
A2a Adenosine Receptor

scholarly journals Prognostic impact of CD73 and A2A adenosine receptor expression in non-small-cell lung cancer

Oncotarget ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 8738-8751 ◽  
Author(s):  
Yusuke Inoue ◽  
Katsuhiro Yoshimura ◽  
Nobuya Kurabe ◽  
Tomoaki Kahyo ◽  
Akikazu Kawase ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Adenosine Receptor ◽  
Small Cell ◽  
Receptor Expression ◽  
Prognostic Impact ◽  
Small Cell Lung ◽  
A2a Adenosine Receptor

scholarly journals KD-64 – a new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

2020 ◽  
Author(s):  
Magdalena Kotańska ◽  
Anna Dziubina ◽  
Małgorzata Szafarz ◽  
Kamil Mika ◽  
Karolina Reguła ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Obese Mice ◽  
A2a Adenosine Receptor ◽  
Selective Antagonist ◽  
Adenosine Receptor Antagonist ◽  
Diet Induced Obesity ◽  
Tnf Α ◽  
Obesity In Mice ◽  
Anti Inflammatory

AbstractThe A2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of A2A adenosine receptor – KD-64 as compared to the known non-selective antagonist – caffeine on these two particular processes. Two different inflammation models were induced namely local and systemic inflammation. Obesity was induced in mice by high-fat diet and the tested compounds (KD-64 and caffeine) were administrated for 21 days. KD-64 showed anti-inflammatory effect in both tested inflammation models and administered at the same dose as ketoprofen exerted stronger effect than this reference compound. Elevated levels of IL-6 and TNF-α observed in obese control mice were significantly lowered by the administration of KD-64 and were similar to the values observed in control non-obese mice. Interestingly, caffeine increased the levels of these parameters. In contrast to caffeine which had no influence on AlaT activity, KD-64 administration significantly lowered AlaT activity in the obese mice. Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine A2A receptor antagonist was quite different from that of the non-selective.

scholarly journals Influence of haemodialysis and left ventricular failure on peripheral A2A adenosine receptor expression

2007 ◽  
Vol 22 (3) ◽  
pp. 851-856 ◽  
Author(s):  
L. Carrega ◽  
E. Fenouillet ◽  
P. Giaime ◽  
A. Charavil ◽  
L. Mercier ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Left Ventricular ◽  
Receptor Expression ◽  
Left Ventricular Failure ◽  
Ventricular Failure ◽  
A2a Adenosine Receptor

Ligand-Based Virtual Screening Using Tailored Ensembles: A Prioritization Tool for Dual A2A Adenosine Receptor Antagonists / Monoamine Oxidase B Inhibitors

2016 ◽  
Vol 22 (21) ◽  
pp. 3082-3096 ◽  
Author(s):  
Aliuska Morales Helguera ◽  
Yunierkis Perez-Castillo ◽  
M. Natália D.S. Cordeiro ◽  
Eduardo Tejera ◽  
César Paz-y-Miño ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Monoamine Oxidase ◽  
Adenosine Receptor ◽  
Monoamine Oxidase B ◽  
Receptor Antagonists ◽  
A2a Adenosine Receptor
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