Platelet-activating factor receptor (PAFR) (PAFR)

The Platelet-activating factor receptor (PAFR) is a G protein-coupled receptor (GPCR) that mediates the biological effects of platelet-activating factor (PAF), a potent phospholipid mediator of inflammation and thrombosis (UniProt P25105). PAFR is expressed on various cell types, including platelets, leukocytes, and vascular endothelial and smooth muscle cells (PubMed: 10409156). Upon activation, PAFR triggers intracellular signaling cascades involving phospholipase C and calcium mobilization, leading to diverse physiological responses such as platelet aggregation, inflammatory cell activation, and potent vasoconstriction (StatPearls: Platelet Activating Factor). In the context of vasoconstriction, PAFR activation on smooth muscle cells leads to contraction, contributing to the pathophysiology of conditions like pulmonary hypertension, anaphylaxis, and systemic shock (PubMed: 15655402). Pharmacological targeting of PAFR primarily involves the use of antagonists, such as lexipafant and rupatadine, to treat inflammatory and allergic disorders (PubChem: CID 10168). These drugs work by competitively inhibiting the binding of PAF to the receptor, thereby dampening the downstream inflammatory and vascular signaling (PubMed: 9204064).

Other names

PTAFRPAF receptorPlatelet-activating factor receptorPAFR

Antagonism of the platelet-activating factor receptor to block the binding of the pro-inflammatory phospholipid PAF.