Thromboxane A2 receptor (TP) (TP)

The Thromboxane A2 receptor (TP) is a G protein-coupled receptor (GPCR) that plays a critical role in cardiovascular homeostasis and inflammatory responses (UniProt: P21708). It is primarily expressed in platelets and vascular smooth muscle cells, where it serves as the principal receptor for thromboxane A2 (TXA2), a potent pro-thrombotic and vasoconstrictive lipid mediator (IUPHAR/BPS Guide to Pharmacology). Activation of the TP receptor stimulates Gq and G12/13 signaling pathways, leading to increased intracellular calcium and activation of Rho-kinase, which ultimately triggers platelet aggregation and smooth muscle contraction (NCBI Gene: 6915). Pathologically, excessive TP receptor activation is implicated in various conditions, including myocardial infarction, stroke, hypertension, and bronchial asthma (PubMed: PMID 21937752). Therapeutic strategies targeting this receptor focus on TP receptor antagonists, such as terutroban and seratrodast, which aim to mitigate thrombotic and inflammatory risks (PubChem: CID 115240). Unlike aspirin, which inhibits TXA2 synthesis, direct TP receptor antagonists block the effects of both TXA2 and other ligands like isoprostanes, potentially offering broader clinical utility in treating cardiovascular and respiratory diseases (StatPearls: NBK537241).

Other names

TP receptorProstanoid TP receptorThromboxane receptorTXA2 receptorTBXA2RBDPLT13

Competitive antagonism of the thromboxane A2 receptor to inhibit platelet aggregation and vascular smooth muscle contraction.