Description
Temocaprilisathiazepineprodrugthatinhibitsangiotensin-convertingenzyme(ACE).Temocaprilexhibitsantihypertensive,anti-diabetic,anti-hyperglycemic,andanti-atheroscleroticactivities.Temocaprildecreasesbloodpressurewithoutaffectingheartrateorcardiacoutputandimprovesendothelialdysfunction,vascularremodeling,insulinresistance,andrenalfunction.Inanimalmodels,temocaprilinhibitselevationsinthefastingplasmaglucoselevelandlossofpancreaticβ-cells,preventingthedevelopmentofhyperglycemia.Instroke-pronehypertensiverats,temocaprilprolongssurvivalrates.Inotheranimalmodels,thiscompoundinhibitsoxidativestressandatheroscleroticremodeling.Temocaprilalsoinhibitsmatrixmetalloproteinase2(MMP2),decreasingperitonealsolutetransportinanimalmodelsduringperitonealdialysis,indicatingpotentialbenefitinpreventionofperitonealinjury.
References
YamamotoD,TakaiS,AkimotoT,etal.Matrixmetalloproteinase-2inhibitionbytemocaprilanditsimportantroleinperitonealtransport.ClinExpPharmacolPhysiol.2012Oct;39(10):864-8.PMID:23013132.
KaiharaM,NakamuraY,SugimotoT,etal.OlmesartanandtemocaprilpreventedthedevelopmentofhyperglycemiaandthedeteriorationofpancreaticisletmorphologyinOtsuka-Long-Evans-TokushimaFattyrats.ActaMedOkayama.2009Feb;63(1):35-42.PMID:19247421.
NozawaM,SugimotoK,OhmoriM,etal.Dosingtime-dependenteffectoftemocaprilonthemortalityofstroke-pronespontaneouslyhypertensiverats.JPharmacolExpTher.2006Jan;316(1):176-81.PMID:16174798.
TsudaM,IwaiM,LiJM,etal.InhibitoryeffectsofAT1receptorblocker,olmesartan,andestrogenonatherosclerosisviaanti-oxidativestress.Hypertension.2005Apr;45(4):545-51.PMID:15723967.
YasunariK,MaedaK,NakamuraM,etal.Pharmacologicalandclinicalstudieswithtemocapril,anangiotensinconvertingenzymeinhibitorthatisexcretedinthebile.CardiovascDrugRev.2004Fall;22(3):189-98.PMID:15492767.
OizumiK,KoikeH,SadaT,etal.PharmacologicalprofilesofCS-622,anovelangiotensinconvertingenzymeinhibitor.JpnJPharmacol.1988Nov;48(3):349-56.PMID:2851680.
