产品描述:
MK-0524 is a potent, selective prostaglandin D2 (PGD2) receptor DP1 antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.{14713} It 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.{14713} In a sheep model of allergic rhinitis, 0.1 mg/kg MK-0524 completely blocked PGD2-induced nasal congestion.{14713} At a dose of 4 mg/kg, MK-0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a mouse model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia.{15245} In an in vitro model of amyotrophic lateral sclerosis, MK-0524 has been shown to partially protect cultured motor neurons from PGD2-induced toxicity.{33495,33496}