Description
EfonidipineisamixtureofR(-)andS(+)isomersthatexertslongactingblockingactionsonbothT-typeandL-typecalciumchannels.IthasnoblockingeffectsonN-,P/Q-andR-typeCa(2+)channels.WhiletheS(+)isomerisanactiveblockerofboththeT-typeandL-typecalciumchannels,theactionofwhichissimilartotheracemicmixture,itsR(-)isomerselectivelyblockstheT-typechannelonly.InthepreventionofcardiovasculardiseaseefonidipineinhibitsinadosedependentmannertheAngII-andK+-inducedaldosteronesecretion.ItsuppressesAng-IIandK+-inducedmRNAexpressionof11-beta-hydroxylaseandaldosteronesynthaseandinducestheproductionofDHEAsulfate,whichhasanti-atheroscleroticactions.
References
FurukawaT.,MiuraR,HondaM,etal.IdenficationofR(-)-isomerofefonidipineasaselectiveblockerofT-typeCa2+channels.Br.JPharmacol.2004Dec;143(8):1050-7.PIMD:15545287,PMCID:PMC1575949.
TanakaH,ShigenobuK.Efonidipinehydrochloride:adualblockerofL-andT-typeca(2+)channels.CardiovascvDrugRev.2002Winter;20(1):81-92.PMID:12070536.
ImafawaK,OkayamaS,TakaokaM,etalInhibitoryeffectofefonidipineonaldosteronesynthesisandsecretiononhumanadrenocarcinoma(H195R)cells.JCardiovascPharmacol.2006Jan;47(1):133-8.PMID:16424797.
IkedaK,SaitoT,TojoK.Efonidipine,aCa(2+)-channelblocker,enhancestheproductionofdehydroepiandrosteronesulfateinNCI-H195Rhumanadrenocorticalcarcinomacells.TohokuJExpMed.2011;224(4):263-71.PMID:21757861.
