Platelet-activating Factor Receptor Antagonists Small Molecules and Peptides

Platelet-activating factor receptor (PAF-R) is a G_q/G₁₁-coupled-protein receptor that has a role in a wide range of biological processes such as vasodilation, superoxide formation, cell proliferation, angiogenesis and regulation of the inflammatory response. PAF-R is linked to multiple intracellular signaling pathways, including the p38 MAPK and PI 3-K pathways, through increasing intracellular calcium mobilization, increasing IP₃ synthesis and decreasing cAMP formation.

PAF-R has a wide biological distribution with high expression levels in the spleen and skeletal muscles and lower concentrations in the small intestine, lung, heart and liver. The human gene encoding the PAF-R is located on chromosome 1p35-34.3