Pharmacology of adenosine receptors in the vasculature

Abstract

Adenosine is widely distributed in mammals. One of the primary roles of adenosine within the cardiovascular system is to directly control the functions of both cardiac and vascular tissues. Recently, there has been considerable interest in the subclassification of adenosine receptors. Characterization of a heterogeneous population of receptors for adenosine could provide an opportunity for the development of novel compounds of therapeutic value. Adenosine is released from cells as a result of metabolism, and its release can be increased dramatically from cells that are metabolically stressed. This implies that adenosine can be released from a variety of cells throughout the body, as a result of increased metabolic rates, in concentrations that can have a profound impact on blood vessel function and, consequently, blood flow. It is recognized that the actions of this nucleoside on the vasculature are most prominent when oxygen demand is high and there is a reduction in oxygen tension at the site in question. Therefore, it is not surprising that adenosine has been shown to be an important regulator of blood vessel tone under hypoxic conditions. Furthermore, the activation of adenosine receptors on blood vessels can result in relaxation and/or contractions. The nature of the response subsequent to the activation of adenosine receptors is primarily dependent on the type of blood vessel involved and basal tone. This review will focus on the characterization of subtypes of adenosine receptors in blood vessels, as well as the effect of the stimulation of adenosine receptors on the peripheral circulation.