prostacyklinproduktionen

Prostacyclin receptor is a G protein–coupled receptor (GPCR) that binds prostacyclin (PGI2), a potent vasodilator and inhibitor of platelet aggregation. The receptor is encoded by the gene IPR1 in humans and is also known as the prostaglandin I2 receptor or the prostacyclin (PGI2) receptor. It is expressed predominantly in vascular endothelial cells, smooth muscle cells, platelets, and various endocrine tissues.

Ligand binding to the prostacyclin receptor activates the Gαs protein, leading to stimulation of adenylate cyclase and an increase in intracellular cyclic AMP. The elevated cyclic AMP levels activate protein kinase A, which phosphorylates target proteins that mediate vasodilation and inhibit platelet activation. In endothelial cells, the receptor also influences the production of nitric oxide and regulates cellular adhesion molecules.

The receptor plays an essential role in cardiovascular homeostasis, maintaining vascular tone, and preventing thrombosis. Genetic knock‑out of the receptor in mice results in hypertension and increased platelet aggregation, highlighting its protective function. In diseases such as pulmonary arterial hypertension and atherosclerosis, dysregulation of prostacyclin signaling has been implicated. Thus, the prostacyclin receptor is a target for therapeutic agents. Drugs such as iloprost, beraprost, and treprostinil are synthetic PGI2 analogues that stimulate the receptor to treat pulmonary hypertension and peripheral arterial disease. Inhibitors of the receptor are being studied for their potential to modulate platelet function and inflammatory responses.

The receptor physiologically interacts with other prostanoid receptors, and cross‑talk with endothelin and nitric oxide pathways fine‑tunes vascular responses. The high affinity of the receptor for natural and synthetic ligands underlines its clinical relevance, and ongoing research seeks to develop selective modulators with improved efficacy and safety profiles.