Adenosine receptors in GtoPdb v.2023.1

Abstract

Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [112]) are activated by the endogenous ligand adenosine (potentially inosine also at A₃ receptors). Crystal structures for the antagonist-bound [155, 316, 224, 62], agonist-bound [379, 205, 206] and G protein-bound A_2A adenosine receptors [49] have been described. The structures of an antagonist-bound A₁ receptor [130] and an adenosine-bound A₁ receptor-G_i complex [87] have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A₁ receptor obtained with X-ray crystallography has also been reported [58]. The structure of the A_2B receptor has also been elucidated [57]. caffeine is a nonselective antagonist for adenosine receptors, while istradefylline, a selective A_2A receptor antagonist, is on the market for the treatment of Parkinson's disease.