Description
MK-0524isaspecificprostaglandinD2receptor(DP1)inhibitorthatfunctionsasaninverseagoNIST.MK-0524decreasesniacin-inducedflushingduringniacintreatmentofdyslipidemiaandismostoftenstudiedincombinationwithniacin.TheABIlityofMK-0524toinhibitDP1preventsPGD2-inducedhyaluronsynthesis,yieldingbeneficialresultsinpreventingpathologicalchangesassociatedwiththyroideyedisease.Thiscompoundalsohasantithromboticactivity,displayingweakinhibitoryactionagainstthethromboxaneA2receptor,inhibitingplateletactivationathighconcentrations.
References
LabrecqueP,RoySJ,FréchetteL,etal.InverseagonistandpharmacochaperonepropertiesofMK-0524ontheprostanoidDP1receptor.PLoSOne.2013Jun10;8(6):e65767.PMID:23762421.
PhiliposeS,KonyaV,LazarevicM,etal.LaropiprantattenuatesEP3andTPprostanoidreceptor-mediatedthrombusformation.PLoSOne.2012;7(8):e40222.PMID:22870195.
GuoN,BagloleCJ,O"LoughlinCW,etal.Mastcell-derivedprostaglandinD2controlshyaluronansynthesisinhumanorbitalfibroblastsviaDP1activation:implicationsforthyroideyedisease.JBiolChem.2010May21;285(21):15794-804.PMID:20308056.
LuoWL,CrumleyT,EbelD,etal.Singletherapeuticandsupratherapeuticdosesoflaropiprant,aselectiveprostaglandinD2receptor1antagonist,donotprolongtheQTcFintervalinhealthyvolunteers.JClinPharmacol.2010Nov;50(11):1273-9.PMID:20107202.
PaoliniJF,BaysHE,BallantyneCM,etal.Extended-releaseniacin/laropiprant:reducingniacin-inducedflushingtobetterrealizethebenefitofniacininimprovingcardiovascularriskfactors.CardiolClin.2008Nov;26(4):547-60.PMID:19031552.