Laropiprant (MK-0524) is a potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.
Laropiprant shows weaker affinity for TP (Ki=2.95 nM), no significant activity on EP1, EP2, EP3, EP4, FP, and IP.
Laropiprant inhibits the accumulation of cAMP in washed platelets and in plateletrich plasma challenged with PGD with IC50 of 0.09 nM and 4 nM, respectively.
Laropiprant displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.
