Adenosine actions and adenosine receptors after 1 week treatment with caffeine

Acta Physiol Scand. 1982 Jun;115(2):283-6. doi: 10.1111/j.1748-1716.1982.tb07078.x.


After one week treatment with caffeine (20 mg/kg i.p.) the number of adenosine receptors, as determined by specific binding of (3H)-L-PIA, in rat cerebral cortical membranes was increased by about 25%. Cyclic AMP accumulation induced by adenosine analogues in slices of rat hippocampus was unaffected by caffeine treatment. The inhibition of lipolysis in rat fat cells by 2-chloro-adenosine was similarly unaffected. The potency of caffeine as an antagonist of these adenosine-receptor mediated effects was not altered by caffeine treatment. It is concluded that at least some adenosine receptors are up-regulated as a consequence of prolonged caffeine treatment, but that the increase in receptor number is not related to changes in at least two effects of adenosine and caffeine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives
  • Adenosine / pharmacology*
  • Adipose Tissue / metabolism
  • Animals
  • Caffeine / pharmacology*
  • Cyclic AMP / metabolism
  • Dose-Response Relationship, Drug
  • Hippocampus / metabolism
  • Male
  • Rats
  • Rats, Inbred Strains
  • Receptors, Cell Surface / drug effects*
  • Receptors, Cell Surface / metabolism
  • Receptors, Purinergic
  • Time Factors


  • Receptors, Cell Surface
  • Receptors, Purinergic
  • Caffeine
  • Cyclic AMP
  • Adenosine