Open AccessAdenosine receptors in GtoPdb v.2021.2
Author(s) -
Bertil B. Fredholm,
Bruno G. Frenguelli,
Rebecca Hills,
Adriaan P. IJzerman,
Kenneth A. Jacobson,
KarlNorbert Klotz,
Joel Linden,
Christa E. Müller,
Ulrich Schwabe,
Gary L. Stiles
Publication year - 2021
Publication title -
iuphar/bps guide to pharmacology cite
Language(s) - English
Resource type - Journals
ISSN - 2633-1020
DOI - 10.2218/gtopdb/f3/2021.2
Subject(s) - adenosine receptor , adenosine , antagonist , receptor , competitive antagonist , agonist , adenosine a1 receptor , caffeine , chemistry , adenosine a2b receptor , pharmacology , adenosine a2a receptor , endocrinology , biology , biochemistry
Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [110]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for the antagonist-bound [153, 313, 221, 61], agonist-bound [375, 203, 204] and G protein-bound A2A adenosine receptors [49] have been described. The structures of an antagonist-bound A1 receptor [128] and an adenosine-bound A1 receptor-Gi complex [86] have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A1 receptor obtained with X-ray crystallography has also been reported [57]. 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.