Ibisobanuro

Acide ya Obeticholike (INT-747) ni agoniste FXR ikomeye, itoranya kandi ikora mu kanwa hamwe na EC50 ya 99 nM.Acide ya Obeticholike igira anticholeretike na anti-inflammation.Acide ya 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 uhitamo FXR ifite EC50 ifite agaciro ka 99 nM [1].

Farnesoid X reseptor (FXR) ni reseptor ya aside irike igira uruhare muri acide homeostasis, umwijima fibrosis, gutwika umwijima no munda hamwe n'indwara z'umutima-mitsi [2].

Acide ya Obeticholike ni agoniste ikomeye kandi ihitamo ibikorwa bya anticholeretique [1].Acide Obeticholic Acide ni semisynthetic aside aside ikomoka hamwe na ligand ikomeye ya FXR.Imbeba ya estrogene iterwa na cholestasis, 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 wurururururururururuririro rugabanya umuvuduko ukabije wamaraso (IHVR) nta hypotension ya sisitemu.Ingaruka zajyanye no kongera ibikorwa bya 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 imvugo.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 acide (6-ECDCA), agoniste ikomeye kandi ihitamo 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-etil chenodeoxycholic aside, farnesoid X reseptor ligand, muri cholestasis iterwa na estrogene.J Pharmacol Ikwirakwiza, 2005, 313 (2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, n'abandi.Acide ya Obeticholic, farnesoid X reseptor agonist, itezimbere hypertension portal 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 ugaburira 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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