Papamuri

Ko te tote hemicalcium AHU-377 he momo tote hemicalcium o AHU-377. He aukati o te neprilysin me te uara IC50 o te 5 nM [1].

Ko te AHU-377 me te angiotensin II AT1 kaitawhai antagonist valsartan i tito LCZ696 i roto i te 1:1 molar ratio. Ko te LCZ696 he angiotensin receptor neprilysin inhibitor. Ka taea te whakaheke i te pehanga toto, a he rongoa hou pea mo te maimoatanga o te ngoikore o te ngakau. Ko te AHU-377 he rongoa rongoa, ka taea te huri ma te wehenga enzymatic o te ethyl ester ki te ahua kaha LBQ657. E ai ki te korero ko te AHU-377(30 me te 100 mg/kg, PO) ka taea te whakaputa i te paanga antihypertensive i roto i te tikanga o te horopeta i roto i nga kiore DAHI-SS. Engari i roto i te DOCA-tote hypertensive kiore, e whakaatu ana i te whakahekenga ngoikore [2, 3].

Tohutoro:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide aukati endopeptidase kūpapa. J Med Chem. 1995 Mei 12; 38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. Ko te kaha o te valsartan + AHU377 (LCZ696) ki te maimoatanga o te ngoikore o te ngakau. Tohunga Opin Investig Drugs. 2013 Akuhata;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Ko te kaha whakatairite o te AHU-377, he aukati neprilysin kaha, i roto i nga tauira kiore e rua o te takawhita e whakawhirinaki ana ki te rōrahi. BMC Pharmacology 2011, 11(Suppl 1):P33.

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