Papa kāʻei kua

ʻO ka AHU-377 hemicalcium paʻakai kahi paʻakai hemicalcium o AHU-377. He mea kāohi ia o neprilysin me ka waiwai IC50 o 5 nM [1].

ʻO AHU-377 a me ka angiotensin II AT1 receptor antagonist valsartan e haku LCZ696 i ka lakio molar 1: 1. ʻO LCZ696 kahi mea loaʻa i ka mea ʻenemi angiotensin neprilysin. Hiki iā ia ke hoʻemi i ke kahe o ke koko a lilo paha i lāʻau lapaʻau no ka mālama ʻana i ka maikaʻi ʻole o ka naʻau. ʻO ka AHU-377 kahi lāʻau lapaʻau pro-pro, hiki ke hoʻololi ʻia e ka cleavage enzymatic o ka etyl ester i loko o ka palapala hana LBQ657. Ua hōʻike ʻia ʻo AHU-377 (30 a me 100 mg / kg, PO) hiki ke hana i ka hopena antihypertensive i kahi ʻano hilinaʻi ma ka lāʻau ma nā ʻiole DAHI-SS. Akā i nāʻiole hypertensive DOCA-paʻakai, hōʻike ia i kahi hōʻemi nāwaliwali [2, 3].

Nā kūmole:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide kūpale endopeptidase nā mea kūpale. ʻO J Med Chem. 1995 Mei 12; 38 (10): 1689-700.
[2] Voors AA, Dorhout B, van der Meer P. Ke kuleana kūpono o valsartan + AHU377 (LCZ696) i ka mālama ʻana i ka naʻau ʻole. ʻO nā lāʻau lapaʻau Opin Investig Expert. 2013 ʻAuk; 22 (8): 1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. ʻO ka pono hoʻohālikelike o AHU-377, kahi mea hoʻokiwaliwali neprilysin ikaika, i loko o nā ʻano ʻiole ʻelua o ke kiʻekiʻe kiʻekiʻe hilinaʻi nui. BMC Pharmacology 2011, 11 (Hōʻawi 1): P33.

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