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Regadenoson, a vasodilator which acts on the adenosine A2A receptor, was approved by the United States Food and Drug Administration in 2008 and is currently widely used in the field of cardiology. [80] [81] Both adenosine and dipyridamole, which act on the A2A receptor, are used in myocardial perfusion imaging. [82]
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 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.
A 1 receptors are implicated in sleep promotion by inhibiting wake-promoting cholinergic neurons in the basal forebrain. [6] A 1 receptors are also present in smooth muscle throughout the vascular system. [7] The adenosine A 1 receptor has been found to be ubiquitous throughout the entire body. [citation needed]
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.
Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers . Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity.
In smooth muscle cells of blood vessels the principal effect of activation of these receptors is vasoconstriction. Blood vessels with α 1-adrenergic receptors are present in the skin, the sphincters [4] of gastrointestinal system, kidney (renal artery) [5] and brain. [6] During the fight-or-flight response vasoconstriction results in decreased ...
The α 2-adrenergic receptor binds both norepinephrine released by sympathetic postganglionic fibers and epinephrine (adrenaline) released by the adrenal medulla, binding norepinephrine with slightly higher affinity. [4] It has several general functions in common with the α 1-adrenergic receptor, but also has specific effects of its own.