Abstract: Thrombin, collagen, platelet activating factor, arachidonic acid, adenosine diphosphate, adrenaline, serotonin and other platelet agonists can stimulate platelet to generate a series of complex signal transduction and then cause platelet physiological responses including deformation, granule release and aggregation etc. Although platelet activation and aggregation at sites of vascular injury is an essential step in coagulation process, excessive platelet accumulation leads to the formation of occlusive thrombi, which are responsible for acute ischemic events. Therefore, anti-platelet therapy is an important approach for the treatment of thrombotic diseases. Currently used anti-platelet drugs, which primarily act through receptors and/or signaling molecules in activation pathways, achieving their effects by inhibiting platelet receptors or blocking signal transmission. In this review, the targets of the above-mentioned platelet agonists and their specific activation mechanisms are introduced; receptor antagonists and other anti-platelet drugs are also summarized.