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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]
Adenosine is a key factor in regulating the body's sleep-wake cycle. [39] Adenosine levels rise during periods of wakefulness and lowers during sleep. Higher adenosine levels correlate with a stronger feeling of sleepiness, also known as sleep drive or sleep pressure. [40]
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 receptors are involved in bone formation. [48]
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]
Abundant extracellular adenosine can then bind to the A2A receptor resulting in a G s-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e., PD-1). [56]
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 ...
Adenosinergic means "working on adenosine". An adenosinergic agent (or drug) is a chemical which functions to directly modulate the adenosine system in the body or brain. Examples include adenosine receptor agonists, adenosine receptor antagonists (such as caffeine), and adenosine reuptake inhibitors.
The most probable mechanism for the delay of fatigue is through the obstruction of adenosine receptors in the central nervous system. [23] Adenosine is a neurotransmitter that decreases arousal and increases sleepiness. By preventing adenosine from acting, caffeine removes a factor that promotes rest, and delays fatigue.