TXA2R Inhibitors

TXA2R inhibitors are a group of chemicals that either directly bind to and inhibit the thromboxane A2 receptor (TXA2R) or indirectly lead to its inhibition by interfering with the production of its natural ligand, thromboxane A2 (TXA2). These inhibitors can be categorized into several classes based on their structures and mechanisms of action. The first class includes direct antagonists of TXA2R, such as ifetroban, sulotroban, seratrodast, terbogrel, ramatroban, S-145, GR 32191, BMS-180,291, SQ 29,548, and torasemide. These chemicals work by binding to TXA2R and blocking the binding of TXA2, thus preventing the activation of the receptor. Some of these inhibitors, such as terbogrel and ramatroban, also have antagonist activity at other receptors, such as the prostacyclin receptor and the CRTH2 receptor, respectively. The second class includes chemicals that inhibit the production of TXA2, such as picotamide and ozagrel. Picotamide is a dual antagonist of the TP receptor and the thromboxane synthase enzyme. It not only prevents the activation of TXA2R by blocking the binding of TXA2, but also reduces the production of TXA2 by inhibiting the activity of thromboxane synthase.