Adenosine is released in large amounts during myocardial ischemia and is ca
pable of exerting potent cardioprotective effects in the heart. Although th
ese observations on adenosine have been known for a long time, how adenosin
e acts to achieve its anti-ischemic effect remains incompletely understood.
However, recent advances on the chemistry and pharmacology of adenosine re
ceptor ligands have provided important and novel information on the functio
n of adenosine receptor subtypes in the cardiovascular system. The developm
ent of model systems for the cardiac actions of adenosine has yielded impor
tant insights into its mechanism of action and have begun to elucidate the
sequence of signalling events from receptor activation to the actual exerti
on of its cardioprotective effect. The present review will focus on the ade
nosine receptors that mediate the potent anti-ischemic effect of adenosine,
new ligands at the receptors, potential molecular signalling mechanisms do
wnstream of the receptor, mediators for cardioprotection, and possible clin
ical applications in cardiovascular disorders.