Thromboxane A2 receptor is a member of the G protein-coupled receptor superfamily. It performs an essential role in hemostasis by interacting with thromboxane A2 to induce platelet aggregation. Thromboxane A2 is an arachidonic acid metabolite produced by the action of thromboxane synthase on prostaglandin endoperoxide H(2) (PGH(2)), which results from the enzymatic transformation of arachidonic acid by the cyclooxygenases (COX-1 and COX-2). In humans Thromboxane A2 signals through two distinct Thromboxane A2 receptor isoforms which differ only in their C-terminal tails: alpha form (placenta) and beta form (endothelium). The interaction between Thromboxane A2 receptor and Thromboxane A2 is involved in the pathogenesis of numerous cardiovascular diseases such as atherosclerosis. Consequently, designing Thromboxane A2 receptor antagonists remains of great interest in cardiovascular medicine.