A1 and A3 adenosine receptor agonists: an overview

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Abstract
Adenosine regulates several physiological functions through specific cell membrane receptors. On the basis of pharmacological studies and molecular cloning, four distinct adenosine receptors have been identified and classified as A1, A2A, A2B and A3. These adenosine receptors are members of the G-protein coupled receptor family, but while A2A and A2B receptors stimulate adenylyl cyclase with a consequent increase of cAMP levels, A1 and A3 receptor subtypes produce the opposite effect. Intense efforts made over the last 20 years have led to the synthesis of a variety of selective adenosine agonists. In general, all of the compounds thus far identified are related to the adenosine structure. The A1 receptors are usually found on the working cells of tissues (e.g., neurones and cardiomyocytes) and mediate decreases in oxygen demand; for these reasons A1 agonists could be useful for the treatment of, for example, renal failure, arrhythmias, diabetes Type II, myocardial ischaemia and neurodegenerative disorder...