Many radiopharmaceuticals have been developed and wildy used in the imaging cardiac function. Myocardial perfusion imaging (MPI) is a well established noninvasive method of assessing coronary blood flow and has been widely used in patients diagnosed or suspected with coronary artery diseases. The innovation of radiopharmaceuticals used in the cardiac imaging is one of the most important contributors to the development of nuclear cardiology. Thallium-201 and various technetium-99m agents have been globally used for myocardial perfusion SPECT, and N-13 ammonia (13NH3), rubidium-82 (82Rb), O-15 water (H215O) for myocardial perfusion PET. As well as the cardiac perfusion studies, new radiopharmaceuticals that visualize fat metabolism or receptors of the sympathetic nervous system have successfully been applied to clinical practice. Useful information can be obtained for diagnosing coronary artery disease, evaluating patients' condition, or assessing therapeutic effects. In this review, we describe the characteristics and clinical usefulness of radiopharmaceuticals used for cardiac SPECT and PET. (Nucl Med Mol Imaging 2009;43(3):174-178)