Invitro | MRE-269boundtothehumanIPreceptorwithhighaffinity(bindingaffinity(Ki)of20nM)andwithmorethan130-foldselectivityoverotherprostanoidreceptors(prostaglandinEreceptors,EP1−4;prostaglandinDreceptor,DP1;prostaglandinF2receptor,FP;thromboxaneA2receptor,TP).Inpulmonaryarterialsmoothmusclecells(PASMCs),MRE-269potentlyinducesaccumulationofintracellularcAMP,leadingtolong-lasting(>10h)membranehyperpolarization(EC50=32nM)whichcontributestocellrelaxation.Italsocauseslong-lastingandpronouncedrelaxationofPASMCs[1]. |
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Invivo | AfterOralAdministration(1mg/kg)tomonkeys,theTmax(timetoreachmaximumobservedplasmaconcentration),Cmax(maximumobservedplasmaconcentration),AUC0−24h(areaunderthecurvefrom0to24hafterdosing)andT1/2(apparentterminalhalf-life)are2.3h,105ng/mL,652ng·h/mLand5.6h,respectivelyforMRE-269[1]. |
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