abẹlẹ

AHU-377 iyo hemicalcium jẹ fọọmu iyọ hemicalcium ti AHU-377. O jẹ onidalẹkun ti neprilysin pẹlu iye IC50 ti 5 nM [1].

AHU-377 ati angiotensin II AT1 olugba antagonist valsartan ṣe akojọpọ LCZ696 ni ipin molar 1:1 kan. LCZ696 jẹ oludena olugba angiotensin neprilysin. O le dinku titẹ ẹjẹ ati pe o le jẹ oogun aramada fun itọju ikuna ọkan. AHU-377 jẹ oogun pro-oògùn, o le ṣe iyipada nipasẹ fifọ enzymatic ti ethyl ester sinu fọọmu ti nṣiṣe lọwọ LBQ657. O royin pe AHU-377 (30 ati 100 mg / kg, PO) le fa ipa antihypertensive ni ọna ti o gbẹkẹle iwọn ni awọn eku DAHI-SS. Ṣugbọn ninu awọn eku haipatensonu DOCA-iyọ, o ṣe afihan idinku alailagbara [2, 3].

Awọn itọkasi:
[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. Ọdun 1995 Oṣu Karun Ọjọ 12; 38 (10): 1689-700.
[2] Voors AA, Dorhout B, van der Meer P. Ipa agbara ti valsartan + AHU377 (LCZ696) ni itọju ikuna ọkan. Amoye Opin Investig Oloro. 2013 Oṣù; 22 (8): 1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Ipa afiwera ti AHU-377, oludena neprilysin ti o lagbara, ni awọn awoṣe eku meji ti haipatensonu ti o gbẹkẹle iwọn didun. BMC Pharmacology 2011, 11 (Ipese 1): P33.

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