Abstract

The A1 adenosine receptors (A1AR), belonging to the rhodopsin-like superfamily of the G-protein-coupled receptors (GPCRs), may regulate many various cellular processes in cardiovascular, renal, and central nervous systems. In addition, since the A1AR possesses antilipolytic properties, numerous A1AR agonists and antagonists have been developed, but only some of them with the most promising selective properties in vitro have been advanced to animal studies and clinical trials. In this review, we have summarized the studies on the utility of A1AR selective agonists and antagonists in the regulation of lipid and carbohydrate metabolism and their potential therapeutic applications in diabetes.

Keywords: Adenosine receptors, agonists, antagonists, diabetes, insulin resistance, lipolysis