| 应用 |
The biological effects of prostaglandin D (PGD) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP and CRTH2/DP In humans, CRTH2/DP is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD CAY10595, as a racemic mixture, is a potent CRTH2/DP receptor antagonist that binds to the human receptor with a K value of 10 nM. The R enantiomer of CAY10595 is significantly more potent exhibiting K values of 5.3 and 5 nM at the human and murine CRTH2/DP receptor, respectively. The R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD with an IC value of 7.3 nM. |
