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Coffee in Health and Disease Prevention by Victor R. Preedy

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Chapter 90

Pharmacology of Caffeine

The Main Active Compound of Coffee

Franciszek Burdan     Experimental Teratology Unit, Human Anatomy Department; Medical University of Lublin, Lublin, Poland

Abstract

Caffeine (1,3,7-trimethylxanthine), the main active ingredient of coffee, is a natural methylxanthine derivative that acts as an antagonist of adenosine A1, A2A, and A2B receptors. Unlike metabolism, caffeine absorption, distribution, and excretion are similar in humans and most laboratory animals. Because of rapid absorption, slight binding with protein, the alkaloid crosses intercellular barriers and is well distributed in tissues and organs. Caffeine is metabolized mainly in the liver and the crucial step (i.e., demethylation) is catalyzed by CYP1A2. ...

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