Caffeine pp 142-150 | Cite as

Caffeine and the Cardiovascular Effects of Physiological Levels of Adenosine

  • W. R. von Borstel
  • R. J. Wurtman


In spite of the widespread use of the methylxanthines caffeine and theophylline as food constituents and as drugs, the biochemical events mediating their pharmacological actions are not well understood. On the basis of experiments performed mainly upon isolated tissue or organ preprations in vitro, several detailed mechanisms have been proposed which might underlie the effects of methylxanthines on neural, cardiovascular, renal, and respiratory processes; however, the precise actions and potencies of methylxanthines observed in vivo have often been at variance with those observed in in vitro studies (Rall 1980; Neims and von Borstel 1983). Thus the hypothesis, widely held until recently, that caffeine and theophylline act in vivo mainly by inhibiting cyclic AMP (cAMP) phosphodiesterase is untenable given caffeine’s relatively low potency as an inhibitor of the enzyme compared with its potency in modulating physiological processes in vivo. Even relatively high doses of methylxanthines fail to increase tissue cAMP levels in intact animals (Burg and Warner 1975). Similarly, differences between the in vivo and in vitro potencies of methylxanthines diminish the likelihood that caffeine acts as a cardiac and CNS stimulant by direct effects upon calcium storage or translocation (Rall 1980).


Mean Arterial Pressure Adenosine Receptor Adenosine Infusion Adenosine Level Endogenous Adenosine 
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© Springer-Verlag Berlin Heidelberg 1984

Authors and Affiliations

  • W. R. von Borstel
  • R. J. Wurtman

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