High-affinity, potent and selective adenosine 2B receptor (A2B) antagonist/inverse agonist.
MRS-1706 is a high-affinity, potent and selective adenosine 2B receptor (A2B) antagonist/inverse agonist (human A1/A2A/A2B/A3 Ki = 157/112/1.39/230 nM; rat A1/A2A Ki = 37.6/548 nM). MRS-1706 (20 nM), but not the A2A antagonist SCH 58261 (20 nM), completely blocks the enhancement of electrically evoked tritium overflow from isolated rat tail artery by 10 μM adenosine receptor agonist NECA in the presence of 30 nM A1 antagonist DPCPX.
European journal of pharmacology, 504(1-2), 17-25 (2004-10-28)
Adenosine receptors involved in the modulation of noradrenaline release from postganglionic sympathetic nerves in rat tail artery were characterized by studying the effects of adenosine-receptor agonists and antagonists on electrically evoked tritium overflow (100 pulses, 5 Hz) and by immunohistochemistry.
The Effect of Adenosine A2A and A2B Antagonists on Tracheal Responsiveness, Serum Levels of Cytokines and Lung Inflammation in Guinea Pig Model of Asthma.
The Journal of pharmacology and experimental therapeutics, 320(2), 637-645 (2006-11-02)
The human adenosine A(2B) receptor belongs to class A G protein-coupled receptors (GPCRs). In our previous work, constitutively active mutant (CAM) human adenosine A(2B) receptors were identified from a random mutation bank. In the current study, three known A(2B) receptor
The A2B Adenosine Receptor Modulates the Epithelial- Mesenchymal Transition through the Balance of cAMP/PKA and MAPK/ERK Pathway Activation in Human Epithelial Lung Cells.
Journal of immunology (Baltimore, Md. : 1950), 202(3), 724-735 (2018-12-28)
This study investigates the mechanism(s) underlying the immunoregulatory activities of placenta-derived human amnion epithelial cells (hAEC). The working hypothesis is that NAD+ and ATP, along with ectoenzymes involved in their metabolism, play a significant role in hAEC-mediated immune regulation. Proof
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