Fa'amatalaga

Obeticholic acid (INT-747) o se malosi, filifilia ma tautala fa'amalosi FXR agonist ma le EC50 o le 99 nM.Obeticholic acid ei ai le anticholeretic ma le anti-inflammation aafiaga.Obeticholic acid e fa'aosofia ai fo'i le autophagy[1][2][3].

Talaaga

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) o se agonist malosi ma filifilia o le FXR ma le tau EC50 o le 99 nM [1].

O le farnesoid X receptor (FXR) o se faʻamaʻi faʻamaʻi faaniukilia o loʻo aʻafia i le homeostasis acid, ate fibrosis, ate ma le intestinal mumū ma maʻi cardiovascular [2].

Obeticholic Acid o se agonist FXR malosi ma filifilia ma le anticholeretic gaioiga [1].Obeticholic Acid o se semisynthetic bile acid e maua mai ma malosi FXR ligand.I le estrogen-induced cholestasis rats, 6-ECDCA puipuia mai cholestasis fa'aosoina e le 17α-ethynylestradiol (E217α) [2].I fa'ata'ita'iga o isumu o le toto toto maualuga (PHT), INT-747 (30 mg/kg) toe fa'agaoioia le ala fa'ailoga FXR i lalo ma fa'aitiitia le mamafa o le faitoto'a e ala i le fa'aitiitia o le fa'ato'a fa'ato'a toto toto (IHVR) e aunoa ma le fa'aleagaina o le toto maualuga.O lenei aafiaga na fesoʻotaʻi ma le faʻateleina o le eNOS [3].I le faʻataʻitaʻiga a le Dahl rat o le maualuga o le masima maʻaleʻale ma le inisalini-resistance (IR), meaʻai maualuga masima (HS) faʻateleina le faʻatupuina o le toto toto ma faʻaititia le faʻaaliga DDAH.INT-747 faʻaleleia le faʻaogaina o le inisalini ma faʻalavelaveina le faʻaitiitia o le faʻamatalaga DDAH [4].

Fa'asinomaga:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), o se agonist FXR malosi ma filifilia ua faʻamanuiaina i le gaioiga anticholestatic.J Med Chem, 2002, 45(17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.O a'afiaga puipuia o le 6-ethyl chenodeoxycholic acid, o le farnesoid X receptor ligand, i le estrogen-induced cholestasis.J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.Obeticholic acid, ose fanesoid X receptor agonist, fa'aleleia le toto toto maualuga e ala i auala ma'oti se lua i isumu cirrhotic.Hepatology, 2014, 59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.FXR agonist INT-747 faʻaleleia le faʻamatalaga DDAH ma faʻaleleia le faʻaogaina o le inisalini i luga o le masima fafaga Dahl rats.PLoS Tasi, 2013, 8(4): e60653.

Fa'amatalaga o oloa

• 1. Selina Costa."Faʻailogaina o se Ligand Novel mo le Farnesoid X Receptor faʻaaogaina Transgenic Zebrafish."Iunivesite o Toronto.Iuni-2018.
• 2. Keni, Repeka."Aafiaga o Fenofibrate i luga ole CYP2D6 ma Tulafono Faʻatonu a ANG1 ma RNASE4 e le FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

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