CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor. It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.
