Prostacyclin receptor (IP) (IP)

The Prostacyclin receptor, also known as the IP receptor, is a member of the G protein-coupled receptor (GPCR) family that plays a critical role in cardiovascular homeostasis (UniProt P43119). It is primarily expressed in vascular smooth muscle cells and platelets, where it serves as the primary receptor for prostacyclin (PGI2), a potent lipid mediator derived from arachidonic acid (PubMed: 15554141). Upon binding its ligand, the IP receptor activates the Gs-adenylyl cyclase pathway, resulting in elevated intracellular cyclic AMP (cAMP) levels (PubChem CID 115164). This signaling cascade triggers profound vasodilation and inhibits platelet aggregation, thereby preventing thrombosis and maintaining vascular tone (NCBI Gene: 5739). In diseases such as pulmonary arterial hypertension (PAH), the prostacyclin pathway is often impaired, leading to excessive vasoconstriction and vascular remodeling (StatPearls: Pulmonary Hypertension). Therapeutic intervention typically involves the use of prostacyclin analogs or selective IP receptor agonists like selexipag to restore these protective effects (PubMed: 26699167). While highly effective in improving patient outcomes, targeting the IP receptor can lead to systemic side effects such as flushing, jaw pain, and hypotension (Wikipedia: Prostacyclin receptor).

Other names

PTGIRProstaglandin I2 receptorProstanoid IP receptorPGI2 receptor

Agonism of the IP receptor activates Gs proteins, which stimulate adenylyl cyclase to increase intracellular cAMP levels, leading to vasodilation and inhibition of platelet aggregation (PubMed: 15554141).