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Overview
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Background
Laropiprant(Cardaptive; MK 0524) is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 μM for the DP1 and DP2 receptors, respectively. Laropiprant(Cardaptive; MK 0524) inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09 and 4.0 nM, respectively. In a sheep model of allergic rhinitis, 0.1 mg/kg MK 0524 completely blocked PGD2-induced nasal congestion. At a dose of 4 mg/kg, MK 0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a murine model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia.
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