Caffeine and adenosine.

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Ribeiro JA, Sebastiao AM

Caffeine and adenosine.

J Alzheimers Dis. 2010;20 Suppl 1:S3-15. doi: 10.3233/JAD-2010-1379.

PubMed ID

20164566 [ View in PubMed

]

Abstract

Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): A1, A2A, A3, and A2B and, as does adenosine, exerts effects on neurons and glial cells of all brain areas. In consequence, caffeine, when acting as an AR antagonist, is doing the opposite of activation of adenosine receptors due to removal of endogenous adenosinergic tonus. Besides AR antagonism, xanthines, including caffeine, have other biological actions: they inhibit phosphodiesterases (PDEs) (e.g., PDE1, PDE4, PDE5), promote calcium release from intracellular stores, and interfere with GABA-A receptors. Caffeine, through antagonism of ARs, affects brain functions such as sleep, cognition, learning, and memory, and modifies brain dysfunctions and diseases: Alzheimer's disease, Parkinson's disease, Huntington's disease, Epilepsy, Pain/Migraine, Depression, Schizophrenia. In conclusion, targeting approaches that involve ARs will enhance the possibilities to correct brain dysfunctions, via the universally consumed substance that is caffeine.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Caffeine	Adenosine receptor A2b	Protein	Humans	Yes	Antagonist	Details
Caffeine	Adenosine receptor A3	Protein	Humans	Yes	Antagonist	Details
Caffeine	Cyclic nucleotide phosphodiesterase (Protein Group)	Protein group	Humans	Unknown	Inhibitor	Details

Food Interactions

Drug	Interaction
Adenosine	Avoid caffeine. Caffeine may antagonise the activity of adenosine.