Dopamine receptor activation can lead to pronounced changes in cardiovascular function. The myriad of effects produced by dopamine receptor agonists results from the activation of dopamine receptors located at different anatomical sites in the cardiovascular system. Further basic research is required to better characterize these dopamine receptors so as to allow the development of more specific dopamine receptor agonists. Endogenous dopamine may be involved in the physiological control of fluid and electrolyte balance and continuing research efforts in this area should provide for a better understanding of the role of cardiovascular dopamine receptors in the maintenance of overall circulatory homeostasis. Cardiovascular dopamine receptor stimulation represents an important and promising approach for the development of novel therapeutic agents for the treatment of hypertension, angina pectoris, congestive heart failure and acute renal failure.

and adenosine cause frequent side effects as a result of nonspecific adenosine receptor stimulation. Selective agonism of the adenosine A 2A receptor should result in a similar degree of coronary vasodilation (and thus similar perfusion images) with fewer side effects. Methods and Results-In a multicenter, randomized, single-blind, 2-arm crossover trial, 240 patients underwent 2 single photon emission computed tomographic (SPECT) imaging studies in random order, first after pharmacological stress with adenosine and a second study with the selective adenosine A 2A receptor agonist binodenoson, using 1 of 4 dosing regimens. Safety, tolerability, and SPECT image concordance between the 2 agents were examined. Exact categorical agreement in the extent and severity of reversible perfusion defects ranged from 79% to 87%, with kappa values from 0.69 to 0.85, indicating very good to excellent agreement between binodenoson and adenosine. The risk of any safety event/side effect was significantly lower with any dose of binodenoson than with adenosine (PՅ0.01) because of a dose-related reduction in subjective side effects, as objective events were infrequent. There was a reduction in the severity of chest pain, dyspnea, and flushing in all binodenoson doses compared with adenosine (PϽ0.01), and the magnitude of severity reduction was dose-related. Conclusions-The

The potent A2A-selective adenosine receptor agonist WRC-0470 is a short-acting coronary vasodilator with potential utility for pharmacological stress perfusion imaging.