Mechanism of Physiological Activities

The effects of caffeine on the cardiovascular, neurological, and renal systems and on lipolysis are primarily triggered by the blockage of adenosine receptors through competitive antagonism (40). The structural relationship between caffeine and adenine (and therefore adenosine) was shown previously. Other suggested mechanisms such as the inhibition of phosphodiesterases and modification of calcium metabolism may also be operative but are inadequate to explain these effects at reasonable caffeine concentrations. Adenosine and caffeine show contrasting effects on blood pressure, activity of the central nervous system, urine output, and lipolysis. The well-known induction of tolerance to caffeine also becomes explicable by this mechanism since caffeine is known to induce the formation of additional adenosine receptors in the rat (40).

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