Prostanoid receptor family

The prostanoid receptor family is a group of G protein-coupled receptors (GPCRs) that mediate the biological effects of prostanoids, which are lipid mediators derived from arachidonic acid (IUPHAR/BPS Guide to Pharmacology). The family includes nine well-characterized members: DP1, DP2 (CRTH2), EP1, EP2, EP3, EP4, FP, IP, and TP, each showing preferential binding to specific ligands like prostaglandins D2, E2, F2α, prostacyclin, and thromboxane A2 (PubMed: 7938166). These receptors are widely expressed and regulate critical processes such as vascular tone, platelet aggregation, inflammation, and pain perception (NIH). Therapeutic agents targeting specific subtypes are used for various conditions, including selexipag for pulmonary arterial hypertension and latanoprost for glaucoma (DrugBank). The term "Other prostanoid receptors" is often used as a collective designation for the family or to refer to less common and putative receptors, such as the prostamide receptor, rather than a single specific therapeutic target (Guide to Pharmacology). Beyond the primary GPCRs, some prostanoids may also interact with nuclear receptors like the peroxisome proliferator-activated receptors (PPARs), adding another layer of complexity to their signaling (PubMed: 110168). Drug development in this area focuses on achieving high subtype selectivity to minimize off-target effects, as many prostanoids can cross-react with multiple receptors at higher concentrations.

Other names

Prostaglandin receptorsProstanoid GPCRsEicosanoid receptorsProstamide receptor (putative)

Drugs targeting the prostanoid receptor family function as selective agonists or antagonists of specific subtypes (DP1, DP2, EP1-4, FP, IP, TP) to modulate intracellular signaling pathways, primarily involving the regulation of cyclic AMP (cAMP) levels and calcium mobilization, which in turn control physiological responses such as smooth muscle tone and immune cell activity.