title: Allosteric modulation of adenosine receptors.
abstract: Allosteric modulators for adenosine receptors may have potential therapeutic advantage over orthosteric ligands. Allosteric enhancers at the adenosine A(1) receptor have been linked to antiarrhythmic and antilipolytic activity. They may also have therapeutic potential as analgesics and neuroprotective agents. A(3) allosteric enhancers are postulated to be useful against ischemic conditions or as antitumor agents. In this review, we address recent developments regarding the medicinal chemistry of such compounds. Most efforts have been and are directed toward adenosine A(1) and A(3) receptors, whereas limited or no information is available for A(2A) and A(2B) receptors. We also discuss some findings, mostly receptor mutation studies, regarding localization of the allosteric binding sites on the receptors.
authors.affiliation: Division of Medicinal Chemistry, Leiden/Amsterdam Center for Drug Research, P.O. Box 9502, 2300, RA, Leiden, The Netherlands.
authors.forename: Anikó
authors.initials: A
authors.lastname: Göblyös
authors.forename: Ad P
authors.initials: AP
authors.lastname: Ijzerman