Ibisobanuro

Acide Obeticholike (INT-747) ni agoniste FXR ikomeye, itoranya kandi ikora mu kanwa hamwe na EC50 ya 99 nM. Acide Obeticholike igira anticholeretique na anti-inflammation. Acide Obeticholique nayo itera autofagy [1] [2] [3].

Amavu n'amavuko

Acide ya Obeticholike (6alpha-Ethyl-chenodeoxycholic aside, 6-ECDCA, INT-747) ni agoniste ukomeye kandi utoranya wa FXR ufite EC50 ifite agaciro ka 99 nM [1].

Farnesoid X reseptor (FXR) ni reseptor ya aside irike igira uruhare muri acide aside homeostasis, fibrosis yumwijima, gutwika umwijima n amara nindwara zifata umutima-mitsi [2].

Acide ya Obeticholike ni agoniste ikomeye kandi ihitamo ibikorwa bya anticholeretique [1]. Acide Obeticholike ni semisynthetic aside aside ikomoka hamwe na ligand ikomeye ya FXR. Imbeba ya cholestasis iterwa na estrogene, 6-ECDCA yarinze cholestasis iterwa na 17α-ethynylestradiol (E217α) [2]. Muri cirrhotic portal hypertension (PHT) yerekana imbeba, INT-747 (30 mg / kg) yongeye gukora inzira ya FXR yamanuka yerekana inzira kandi igabanya umuvuduko wurubuga igabanya ubukana bwimitsi itwara imitsi (IHVR) idafite hypotension idasobanutse. Izi ngaruka zajyanye no kwiyongera kwa eNOS [3]. Muburyo bwimbeba ya Dahl yumuvuduko ukabije wumunyu hamwe na insuline-irwanya insuline (IR), indyo yumunyu mwinshi (HS) yongereye cyane umuvuduko wamaraso hamwe na tissue DDAH itagabanije. INT-747 yongereye imbaraga za insuline kandi ibuza kugabanuka kwimvugo ya DDAH [4].

Reba:
[1]. Pellicciari R, Fiorucci S, Camaioni E, n'abandi. 6alpha-Ethyl-chenodeoxycholic aside (6-ECDCA), agoniste ukomeye kandi watoranije FXR yahawe ibikorwa bya anticholestique. J Med Chem, 2002, 45 (17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, n'abandi. Ingaruka zo gukingira 6-Ethyl chenodeoxycholic acide, ligand ya farnesoid X reseptor ligand, muri cholestase iterwa na estrogene. J Pharmacol Ikwirakwiza, 2005, 313 (2): 604-612.
[3]. Verbeke L, Farre R, Trebicka J, n'abandi. Acide Obeticholike, farnesoid X reseptor agonist, itezimbere hypertension portal n'inzira ebyiri zitandukanye mumbeba za cirrhotic. Indwara ya Hepatologiya, 2014, 59 (6): 2286-2298.
[4]. Ghebremariam YT, Yamada K, Lee JC, n'abandi. FXR agonist INT-747 igenga imvugo ya DDAH kandi ikongerera insuline mumunyu mwinshi wagaburiwe imbeba za Dahl. PLOS Umwe, 2013, 8 (4): e60653.

Ibicuruzwa byatanzwe

• 1. Selina Costa. "Kuranga Ligand ya Novel kuri Receptor ya Farnesoid X ukoresheje Zebrafish ya Transgenic." Kaminuza ya Toronto. Jun-2018.
• 2. Kent, Rebecca. "Ingaruka za Fenofibrate kuri CYP2D6 no Gutegeka ANG1 na RNASE4 na Acide ya FXR Agonist Obeticholic." indigo.uic.edu.2017.

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