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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]
The A 1 receptors couple to G i/o and decrease cAMP levels, while the A 2 adenosine receptors couple to G s, which stimulates adenylate cyclase activity. In addition, A 1 receptors couple to G o , which has been reported to mediate adenosine inhibition of Ca 2+ conductance, whereas A 2B and A 3 receptors also couple to G q and stimulate ...
CGS-15943 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A 1 and A 2A, having a K i of 3.3nM at A 2A and 21nM at A 1.It was one of the first adenosine receptor antagonists discovered that is not a xanthine derivative, instead being a triazoloquinazoline.
nonselective adenosine receptor antagonists [10] But different analogues show varying potency at the numerous subtypes, and a wide range of synthetic xanthine derivatives (some nonmethylated) have been developed in the search for compounds with greater selectivity for phosphodiesterase enzyme or adenosine receptor subtypes.
The molecular target of the active metabolite of ADP receptor inhibitors is the P2Y 12 receptor. [17] P2Y 12 receptor is a G-coupled receptor and is activated by adenosine diphosphate . ADP binds to the P2Y 12 receptor that leads to inhibition of adenyl cyclase and thereby decreases the intracellular levels of cAMP.
The actions of the A 2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A 2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity.
Adenosine A 3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during cardiac ischemia, it is involved in the inhibition of neutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and ...
An adenosine receptor agonist is a drug which acts as an agonist of one or more of the adenosine receptors. Examples include the neurotransmitter adenosine , its phosphates , adenosine monophosphate (AMP), adenosine diphosphate (ADP), and adenosine triphosphate (ATP), and the pharmaceutical drug regadenoson .