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The adenosine A2A receptor has also been shown to play a regulatory role in the adaptive immune system. In this role, it functions similarly to programmed cell death-1 (PD-1) and cytotoxic t-lymphocyte associated protein-4 ( CTLA-4 ) receptors, namely to suppress immunologic response and prevent associated tissue damage.
Caffeine keeps you awake by blocking adenosine receptors. Each type of adenosine receptor has different functions, although with some overlap. [3] For instance, both A 1 receptors and A 2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A 2A receptor also has broader anti-inflammatory effects throughout the body. [4]
Adenosine A 2A receptor locations in the body could help us to understand the possible therapeutic applications in the future. They can be found in the lungs, white blood cells, sympathetic nervous system, striatum, tuberculum olfactorium, coronary, lymphatic, brain and other blood vessels, platelets and kidneys.
These receptors enable the regulation of multiple processes such as cell proliferation, differentiation, function, and death. [47] The activation of the adenosine A1 receptor is required for osteoclast differentiation and function, whereas the activation of the adenosine A2A receptor inhibits osteoclast function. The other three adenosine ...
Cancer Therapy by Inhibition of Negative Immune Regulation (CTLA4, PD1) A2AR & A2BR: The Adenosine A2A receptor is regarded as an important checkpoint in cancer therapy because adenosine in the immune microenvironment, leading to the activation of the A2a receptor, is negative immune feedback loop and the tumor microenvironment has relatively high concentrations of adenosine. [27]
SCH-58261 is a drug which acts as a potent and selective antagonist for the adenosine receptor A 2A, with more than 50x selectivity for A 2A over other adenosine receptors. [1] It has been used to investigate the mechanism of action of caffeine, which is a mixed A 1 / A 2A antagonist, and has shown that the A 2A receptor is primarily responsible for the stimulant and ergogenic effects of ...
It is a xanthine and a derivative of the non-selective adenosine receptor antagonist caffeine. [ 1 ] [ 2 ] The affinities (K i ) of MSX-2 for the human adenosine receptors are 5.38 to 14.5 nM for the adenosine A 2A receptor, 2,500 nM for the adenosine A 1 receptor (172- to 465-fold lower than for the A 2A receptor), and >10,000 nM for the ...
ZM-241,385 is a high affinity antagonist ligand selective for the adenosine A 2A receptor. [1]In animal models, ZM-241,385 has been shown to protect against beta amyloid neurotoxicity and therefore may be useful as a treatment for Alzheimer's disease. [2]