Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).
Prostaglandin D2 (PGD2) are one of the key mediators in allergic conditions, such as allergic rhinitis. Laropiprant is a potent, selective PGD2 receptor (DP) antagonist with a competition binding affinity constant (Ki) value of 0.57±0.71nM and a dissociation constant (Kd) value of 0.03nM. It inhibited PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09nM and 4.0nM, respectively. In a sheep model of allergic rhinitis, laropiprant at a dose of 0.1mg/kg effectively blocked (99%) PGD2-induced nasal congestion[3]. In male C57BL/6 mice, pretreatment with laropiprant (0.004–4mg/kg, i.p.) inhibited nicotinic acid-induced vasodilation in a dose-dependent manner[4].
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