Chemical Name: (3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid
Biological ActivityPotent dual antagonist of TP/DP2 (CRTH2) prostanoid receptors (Ki values are 4.3, 4.5 and > 10000 nM for hDP2, hTP and hDP1 receptors respectively). Suppresses PGD2-induced migration of human eosinophils (IC50 = 170 nM).
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Interactions among three classes of mediators explain antigen-induced bronchoconstriction in the isolated perfused and ventilated guinea pig lung.
Sundstrom et al.
Ramatroban (BAY u3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor.
Ishizuka et al.
Cardiovasc.Drug Rev., 2004;22:71
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
Ulven and Kostenis
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HL-1 cardiomyocytes were pre-incubated with BAY-u 3405 (2 µM, 30 min) followed by treatment with 15d-PGJ2 (15 µM, 30 min) to follow p38 activation using Western blot analysis. BAY-u 3405 completely abolished 15d-PGJ2-induced p38 phosphorylation.