Title:Adenosine Receptor Antagonists: Structures and Potential Therapeutic Applications
Volume: 2
Issue: 5
Author(s): C. E. Muller*B. Stein
Affiliation:
- Institut fur Pharmazie und Lebensmittelchemie, Pharmazeutische Chemie, Universität Wurzburg, D-97074 Wurzburg, Germany
Abstract: Adenosine Receptors (AR) are widely distributed in the human body. Four distinct AR subtypes, designated A1, A2a, A2b, and A3, have been identified on a pharmacological basis (affinity profile of agonists and antagonists; second messenger systems) as well as on a molecular level (cloning from various species, including humans). The current article focusses on recent advances in the development of subtype-selective AR antagonists, structure-activity relationships (SAR) of xanthine and non-xanthine A1-, A2a-, A2b- and A3-AR antagonists, and their in-vivo actions. Special attention is given to the cardiovascular effects mediated by AR agonists and antagonists. Potential therapeutic applications for AR ligands, particularly antagonists, in the cardiovascular area and other fields (e.g. CNS, kidney) are discussed.
