Adenosine receptor

Adenosine receptors, and A receptors, P1 or P1 - purinoceptors called receptors are receptors which are activated by the purine nucleoside, adenosine. The four currently known representatives of this group of purinoceptors, which are referred to as A1, A2A, A2B and A3, in the central nervous system and in the regulation of cardiovascular functions and immune responses play a role. These effects are caused by a receptor-mediated activation of G - proteins. The effects of the xanthines, caffeine, theophylline and theobromine can be at least partially explained by interaction with adenosine receptors. The A2A receptor antagonist Istradefyllin is used for the treatment of Parkinson's disease. With the first A2A agonist regadenoson in 2008 was approved in the U.S. for treatment. Other antagonists and agonists are being developed as potential drugs.

History

Alan Drury and Szent- Györgyi Albert of Nagyrapolt discovered in 1929 that adenosine can affect various body functions. These effects were originally attributed to transport proteins and intracellular processes. Contrary to this dogma postulated 1974 L. Bruce Cobbin that specific receptors are responsible for these effects. The fact that at the adenosine receptor is not just a single receptor, but that several isoforms exist in the late 1970s has been demonstrated. Looking for new G protein-coupled receptors, the first adenosine receptors have been cloned by chance, with the A1 and the A2A receptor in the late 1980s. The three-dimensional structure of an adenosine receptor, the A2A receptor, could be cleared up in 2008 as a fusion protein with the help of the X-ray structure analysis. This makes this receptor a first G- protein coupled receptors, are present in the detailed information about its three-dimensional structure.