Gundhig

AHU-377 cusbada kiimikada ah waa nooc cusbada kiimikada ah ee AHU-377. Waa ka-hortagga neprilysin oo leh qiimaha IC50 ee 5 nM [1].

AHU-377 iyo angiotensin II AT1 receptor antagonist valsartan waxay soosaaraan LCZ696 oo kujira saamiga molar 1: 1. LCZ696 waa daawada loo yaqaan 'angiotensin receptor neprilysin inhibitor'. Waxay yareyn kartaa cadaadiska dhiigga waxayna noqon kartaa daawo ugub ah oo lagu daaweeyo wadnaha oo shaqeynaya. AHU-377 waa daawo-yaqaan, waxaa loogu rogi karaa kala-goynta enzymatic ee ethyl ester-ka oo loo beddelayo qaabka firfircoon ee LBQ657. Waxaa lagu soo warramey in AHU-377 (30 iyo 100 mg / kg, PO) ay sababi karto saameyn antihypertensive oo qaab qaadasho ku tiirsan jiirka DAHI-SS ah. Laakiin jiirka dhiig-karka ee 'DOCA-salt', wuxuu muujinayaa hoos u dhac daciif ah [2, 3].

Tixraacyo:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide dhexdhexaad endopeptidase inhibitors. J Med Chem. 1995 Meey 12; 38 (10): 1689-700.
[2] Voors AA, Dorhout B, van der Meer P. Doorka suurtagalka ah ee valsartan + AHU377 (LCZ696) ee daaweynta wadnaha oo shaqeynaya. Khabiirka Opin Investig Mukhaadaraadka. 2013 Agoosto; 22 (8): 1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Waxtarka isbarbardhiga ee AHU-377, oo ah xakameyn neprilysin ah oo xoog leh, oo ku jira laba nooc oo jiir ah oo ah heer-kulka ku-tiirsan mugga. Farmashiga BMC 2011, 11 (Qalabka 1): P33.

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