First marketed in Japan in the 1990s, olprinone is a newly developed phosphodiesterase III (PDE III) inhibitor. It can not only increase cardiac contractility and also reduce peripheral vascular resistance without affecting mean arterial pressure and heart rate. At present, olprinone is mainly used in the treatment of acute heart failure and postoperative acute cardiac insufficiency. Through selectively inhibiting the activity of PDE III and increasing the concentration of cyclic adenosine monophosphate (cAMP) by blocking its degradation, olprinone accelerates the influx of Ca2+ in cardiac myocytes, leading to enhancement of myocardial contractility; and on the other hand, decreases the influx of Ca2+ in vascular smooth muscle cells, resulting in dilation of peripheral blood vessels. Recently, a considerable amount of research has been conducted on olprinone in terms of pulmonary hypertension, myocardial ischemia/reperfusion (I/R) injury, and arrhythmia. In this review, we summarize the application of olprinione in acute heart failure, pulmonary hypertension, myocardial I/R injury, and arrhythmia, and analyze its application value and related progress in cardiovascular diseases.