Description
Aliskirenisadirectrenininhibitorthatexhibitsantihypertensive,antithrombotic,andanti-angiogenicactivities.AliskirenbindstotheS3bpbindingsiteofrenin,inhibitingitsABIlitytocleaveangiotensininintoangiotensinI,thereforepreventingtheformationofangiotensinIIandresultingcontractionofarterialsmoothmuscle.Thiscompoundisavasodilator,decreasingplasmavolumeandbloodpressureinvivo.Inanimalmodelsoflupusnephritis,aliskirenattenuatedproteinuriabydecreasinginflammatorycytokinelevelsandglomerularinflammation.Additionally,inseparateanimalstudies,aliskirendecreasesVEGFlevels,improvesinsulinresistance,andpreventsdevelopmentofvenousthrombosis.
References
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GandhiS,SrinivasanB,AkarteAS.AliskirenimprovesinsulinresistanceandamelioratesdiabeticrenalvascularcomplicationsinSTZ-induceddiabeticrats.JReninAngiotensinAldosteroneSyst.2013Mar;14(1):3-13.PMID:22791702.
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