Vasodilator stress myocardial perfusion imaging accounts for approximately half of the stress studies in the USA. Regadenoson, a selective A2A receptor agonist, was recently approved for clinical use by the US FDA. By contrast, compared with adenosine, regadenoson is administered as a single- and fixed-dose bolus, has comparable hyperemic effect and a better tolerability profile. This article will address and highlight the various regadenoson attributes, properties and the preclinical and clinical studies that have been conducted to date.