Ingemuva

Usawoti we-AHU-377 we-hemicalcium wusawoti we-hemicalcium we-AHU-377.Kuyi-inhibitor ye-neprilysin enevelu ye-IC50 engu-5 nM [1].

I-AHU-377 kanye ne-angiotensin II AT1 receptor antagonist valsartan bahlanganisa i-LCZ696 ngesilinganiso se-molar esingu-1:1.I-LCZ696 iyi-angiotensin receptor neprilysin inhibitor.Kungehlisa umfutho wegazi futhi kungase kube umuthi omusha wokwelapha ukuhluleka kwenhliziyo.I-AHU-377 iyi-pro-drug, ingaguqulwa ngokuqhekeka kwe-enzymatic ye-ethyl ester ibe ifomu elisebenzayo LBQ657.Kubikwa ukuthi i-AHU-377(30 kanye ne-100 mg/kg, PO) ingabangela umphumela we-antihypertensive ngendlela encike kumthamo kumagundane e-DAHI-SS.Kodwa kumagundane we-DOCA-usawoti we-hypertensive, kubonisa ukunciphisa okubuthakathaka [2, 3].

Izithenjwa:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors.J Med Chem.1995 May 12;38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. Indima engaba khona ye-valsartan + AHU377 (LCZ696) ekwelapheni ukuhluleka kwenhliziyo.I-Expert Opin Investig Drugs.2013 Aug;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al.Ukusebenza ngokuqhathaniswa kwe-AHU-377, i-neprilysin inhibitor enamandla, kumamodeli amabili wamagundane we-hypertension encike kumthamo.I-BMC Pharmacology 2011, 11(Suppl 1):P33.

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