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Vol. 305, Issue 1, 347-352, April 2003
Respiratory Diseases Research, and Medicinal Chemistry, Bayer
Yakuhin, Ltd., Kyoto, Japan
Ramatroban (Baynas, BAY u3405), a thromboxane A2
(TxA2) antagonist marketed for allergic rhinitis, has been
shown to partially attenuate prostaglandin (PG)D2-induced
bronchial hyperresponsiveness in humans, as well as reduce
antigen-induced early- and late-phase inflammatory responses in mice,
guinea pigs, and rats. PGD2 is known to induce eosinophilia
following intranasal administration, and to induce eosinophil
activation in vitro. In addition to the TxA2 receptor,
PGD2 is known as a ligand for the PGD2
receptor, and the newly identified G-protein-coupled
chemoattractant receptor-homologous molecule expressed on Th2 cells
(CRTH2). To fully characterize PGD2-mediated inflammatory
responses relevant to eosinophil activation, further analysis of the
mechanism of action of ramatroban has now been performed.
PGD2-stimulated human eosinophil migration was shown to be
mediated exclusively through activation of CRTH2, and surprisingly,
these effects were completely inhibited by ramatroban. This is also the
first report detailing an orally bioavailable small molecule CRTH2
antagonist. Our findings suggest that clinical efficacy of ramatroban
may be in part mediated through its action on this Th2-, eosinophil-,
and basophil-specific chemoattractant receptor.
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