Laropiprant(MK 0524) is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM; exhibits >1,000 fold selectivity over DP2 receptor (Ki=0.75 uM).
1.Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N et al.. (2007) Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).. J Med Chem, 50 (4):(794-806). [PMID:17300164]
2.Cheng K, Wu TJ, Wu KK, Sturino C, Metters K, Gottesdiener K, Wright SD, Wang Z, O'Neill G, Lai E et al.. (2006) Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans.. Proc Natl Acad Sci USA, 103 (17):(6682-7). [PMID:16617107]
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