Imvelaphi

Ityuwa ye-AHU-377 ye-hemicalcium yindlela yetyuwa ye-hemicalcium ye-AHU-377.Yi-inhibitor ye-neprilysin enexabiso le-IC50 le-5 nM [1].

I-AHU-377 kunye ne-angiotensin II AT1 i-receptor antagonist i-valsartan iqulunqa i-LCZ696 kwi-1: i-1 molar ratio.I-LCZ696 yi-angiotensin receptor neprilysin inhibitor.Inokunciphisa uxinzelelo lwegazi kwaye inokuba liyeza elitsha lokunyanga ukusilela kwentliziyo.I-AHU-377 yi-pro-drug, inokuguqulwa nge-enzymatic cleavage ye-ethyl ester kwifom esebenzayo LBQ657.Kuxelwa ukuba i-AHU-377 (30 kunye ne-100 mg / kg, PO) inokubangela umphumo we-antihypertensive ngendlela exhomekeke kwi-dose kwiigundane ze-DAHI-SS.Kodwa kwi-DOCA-ityuwa ye-hypertension rats, ibonisa ukunciphisa obuthathaka [2, 3].

IiReferensi:
[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 ngoMeyi 12;38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. Indima enokwenzeka ye-valsartan + AHU377 (LCZ696) kunyango lwentliziyo.Ingcali Opin Investig Drugs.2013 Aug;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al.Ukusebenza okuthelekisayo kwe-AHU-377, i-neprilysin inhibitor enamandla, kwiimodeli ezimbini zeegundane zoxinzelelo lwegazi oluxhomekeke kumthamo.BMC Pharmacology 2011, 11(Suppl 1):P33.

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