Target intelligence / Profile preview

Prostacyclin (PGI2)

Target
PGI2
Molecular classification
Eicosanoid, Prostanoid, Lipid Molecule
01

Overview

Prostacyclin (PGI2) is a prostanoid produced primarily by endothelial cells. It is a potent vasodilator and inhibitor of platelet aggregation, playing a crucial role in vascular homeostasis. PGI2 is synthesized from arachidonic acid via COX enzymes and prostacyclin synthase. Its effects are mediated by the IP receptor, a G protein-coupled receptor, leading to increased cAMP levels and activation of protein kinase A. Synthetic analogs are used therapeutically for conditions like pulmonary hypertension.

Other names
Prostaglandin I2
02

Mechanism of action

PGI2 binds to the IP receptor, a G protein-coupled receptor, activating adenylate cyclase via Gs proteins, increasing intracellular cAMP levels. This leads to activation of protein kinase A and subsequent physiological effects such as vasodilation and inhibition of platelet aggregation.

03

Biological functions

VasodilationInhibition of platelet aggregationRegulation of inflammationVascular homeostasis
04

Disease associations

Pulmonary hypertensionCardiovascular diseaseThrombosisInflammation
05

Safety considerations

Short half-life in vivoInstability in vivo
06

Interacting drugs

Iloprost

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