Iloprost(ZK36374)isasyntheticanalogueofprostacyclinPGI2.Target:Iloprostisastableprostacyclinanalogcommonlyemployedinthetreatmentofperipheralvasculardiseaseandalsoindicatedinthetreatmentofpatientsaffectedbysystemicsclerosis(SSc)inthepresenceofsevereRaynaud"sphenomenon(RP).[1]Iloprostdilatessystemicandpulmonaryarterialvascularbeds.Iloprostalsoaffectsplateletaggregationbuttherelevanceofthiseffecttothetreatmentofpulmonaryhypertensionisunknown.Thetwodiastereoisomersofiloprostdifferintheirpotencyindilatingbloodvessels,withthe4Sisomersubstantiallymorepotentthanthe4Risomer.[2]Iloprostisastablecarbacyclinderivativeofprostacyclin,wasstudiedduringelectrically-inducedcoronaryarterythrombosisintheopenchestanesthetizedpig.InfusionofZK36374(100ng/kg/min,n=6)hadnoeffectonheartrateandcardiacoutput,butcauseda20%reductioninmeanarterialbloodpressurebyperipheralvasodilation.Inanimalsreceivingsolventornodrugpriortothrombosisinduction,thetimetoocclusivecoronaryarterythrombosis(TOT)was30+/-2minutes(mean+/-SEM,n=17).Pretreatmentwithani.v.infusionofZK36374(100ng/kg/min)prolongedTOTby50%to47+/-7minutes(plessthan0.005,n=6).ThisprolongationofTOTwasnotduetothelowerbloodpressureintheZK36374group,asdihydralazineinadosethatloweredarterialbloodpressuretothesameextenthadnoeffectonTOT(32+/-4minutes,n=4).TheresultsindicatethatZK36374maybeusefulindelaying(orpreventing)occlusivecoronaryarterythrombi.[3]

• [1].DellaBellaS,etal.Novelmodeofactionofiloprost:invitrodown-regulationofendothelialcelladhesionmolecules.ProstaglandinsOtherLipidMediat.2001Jun;65(2-3):73-83.

  [2].vanderGiessenWJ,etal.TheeffectofthestableprostacyclinanalogueZK36374onexperimentalcoronarythrombosisinthepig.ThrombRes.1984Oct1;36(1):45-51.

  [3].AddonizioVPJr,etal.Preventionofheparin-inducedthrombocytopeniaduringopenheartsurgerywithiloprost(ZK36374).Surgery.1987Nov;102(5):796-807.

• [1].DellaBellaS,etal.Novelmodeofactionofiloprost:invitrodown-regulationofendothelialcelladhesionmolecules.ProstaglandinsOtherLipidMediat.2001Jun;65(2-3):73-83.

  [2].vanderGiessenWJ,etal.TheeffectofthestableprostacyclinanalogueZK36374onexperimentalcoronarythrombosisinthepig.ThrombRes.1984Oct1;36(1):45-51.

  [3].AddonizioVPJr,etal.Preventionofheparin-inducedthrombocytopeniaduringopenheartsurgerywithiloprost(ZK36374).Surgery.1987Nov;102(5):796-807.

360.49

C₂₂H₃₂O₄

78919-13-8

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">