Adenosine receptors are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for the antagonist-bound [1,2,3,4], agonist-bound [5,6,7] and G protein-bound A2A adenosine receptors  have been described. The structures of an antagonist-bound A1 receptor  and an adenosine-bound A1 receptor-Gi complex  have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A1 receptor obtained with X-ray crystallography has also been reported . caffeine is a nonselective antagonist for adenosine receptors, while istradefylline, a selective A2A receptor antagonist, is on the market for the treatment of Parkinson's disease.
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