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Coffee in Health and Disease Prevention by Victor R. Preedy

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Chapter 91

Adenosine Receptors as the Biochemical Target for Low Doses of Caffeine

B.B. Fredholm     Department of Physiology and Pharmacology, Karolinska Institute, Stockholm, Sweden

Abstract

A careful examination of the potency of caffeine (and also of its metabolite theophylline) showed that blockade of the actions of adenosine was achieved at considerably lower concentrations than other known actions, including blockade of phosphodiesterase, interaction with gamma amino butyric acid receptors, and increased calcium mobilization. Indeed, significant blockade of three of the four adenosine receptors occurs at caffeine concentrations achieved after ingestion of a single cup of coffee. The importance of adenosine receptors (especially A1 and A2A ...

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