Tlhaloso

Obeticholic acid (INT-747) ke agonist e matla, e khethang le ea molomo ea FXR e nang le EC50 ea 99 nM. Obeticholic acid e na le anticholeretic le anti-inflammation effect. Obeticholic acid e boetse e etsa hore motho a ikutloe a le mong [1] [2] [3].

Ka morao

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) ke agonist e matla le e khethang ea FXR e nang le boleng ba EC50 ba 99 nM [1].

Farnesoid X receptor (FXR) ke receptor ea nyutlelie ea bile acid e amehang ho bile acid homeostasis, sebete fibrosis, ho ruruha ha sebete le mala le lefu la pelo [2].

Obeticholic Acid ke FXR agonist e matla le e khethang e nang le ts'ebetso ea anticholeretic [1]. Obeticholic Acid ke semisynthetic bile acid e nkiloeng le FXR ligand e matla. Likhotong tsa cholestasis tse bakoang ke estrogen, 6-ECDCA e sirelelitsoe khahlanong le cholestasis e bakoang ke 17α-ethynylestradiol (E217α) [2]. Mefuteng ea litoeba tsa cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) e ile ea tsosolosa tsela ea pontšo ea FXR e theohelang tlaase le ho fokotsa khatello ea li-portal ka ho theola kakaretso ea intrahepatic vascular resistance (IHVR) ntle le ho senya systemic hypotension. Phello ena e ne e amahanngoa le ts'ebetso e eketsehileng ea eNOS [3]. Moetsong oa Dahl rat oa khatello ea mali e nang le letsoai-sensitive hypertension le insulin-resistance (IR), lijo tse nang le letsoai le phahameng (HS) li ile tsa eketsa haholo khatello ea mali ea tsamaiso le polelo ea DDAH ea lisele tse theohileng. INT-747 e matlafalitse kutloisiso ea insulin mme e thibela ho fokotseha ha polelo ea DDAH [4].

Litšupiso:
[1]. Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECCDA), FXR agonist e matla le e khethang e nang le ts'ebetso ea anticholestatic. J Med Chem, 2002, 45 (17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, et al. Tšireletso ea 6-ethyl chenodeoxycholic acid, farnesoid X receptor ligand, ho cholestasis e bakoang ke estrogen. J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3]. Verbeke L, Farre R, Trebicka J, et al. Obeticholic acid, farnesoid X receptor agonist, e ntlafatsa khatello ea mali ea portal ka litsela tse peli tse fapaneng ho likhoto tsa cirrhotic. Hepatology, 2014, 59 (6): 2286-2298.
[4]. Ghebremariam YT, Yamada K, Lee JC, et al. FXR agonist INT-747 e laola polelo ea DDAH mme e ntlafatsa kutloisiso ea insulin ho likhoto tsa Dahl tse nang le letsoai le phahameng. PLoS One, 2013, 8(4): e60653.

Tlhahiso ea Sehlahisoa

• 1. Selina Costa. "Ho hlahisa Ligand ea Novel bakeng sa Farnesoid X Receptor e sebelisang Transgenic Zebrafish." Univesithi ea Toronto. Phup-2018.
• 2. Kent, Rebeka. "Liphello tsa Fenofibrate ho CYP2D6 le Taolo ea ANG1 le RNOSE4 ke FXR Agonist Obeticholic Acid." indigo.uic.edu.2017.

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