Platelet P2Y12 receptor inhibitors are crucial in the treatment of patients with acute coronary syndrome or undergoing percutaneous coronary intervention. Ticagrelor is a reversibly binding, potent oral P2Y12 inhibitor that also is a weak inhibitor of the equilibrative nucleoside transporter-1 pathway for cellular adenosine uptake. It is hypothesized that ticagrelor has clinically relevant "off-target" effects, independent of its effect on platelet aggregation and thrombosis. This review considers the pleiotropic effects of ticagrelor and some of the possible mechanisms related to these effects.