Uncovering Caffeine’s Adenosine A2A Receptor Inverse Agonism in Experimental Parkinsonism

  title={Uncovering Caffeine’s Adenosine A2A Receptor Inverse Agonism in Experimental Parkinsonism},
  author={V{\'i}ctor Fern{\'a}ndez-Due{\~n}as and Maricel G{\'o}mez-Soler and Marc L{\'o}pez-Cano and Jaume J. Taura and Catherine Ledent and Masahiko Watanabe and Kenneth A. Jacobson and Jean-Pierre Vilardaga and Francisco Ciruela},
  booktitle={ACS chemical biology},
Caffeine, the most consumed psychoactive substance worldwide, may have beneficial effects on Parkinson's disease (PD) therapy. The mechanism by which caffeine contributes to its antiparkinsonian effects by acting as either an adenosine A2A receptor (A2AR) neutral antagonist or an inverse agonist is unresolved. Here we show that caffeine is an A2AR inverse agonist in cell-based functional studies and in experimental parkinsonism. Thus, we observed that caffeine triggers a distinct mode, opposite… CONTINUE READING
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