Sharaxaada

Obeticholic acid (INT-747) waa FXR xoog leh, door ah oo hadal firfircoon leh oo leh EC50 ee 99 nM. Obeticholic acid waxay leedahay saameyn anticholeretic iyo anti-bararka. Obeticolic acid waxay sidoo kale keentaa autophagy [1] [2] [3].

Asalkii hore

Obeticholic acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECCDCA, INT-747) waa agonist awood leh oo xulashada FXR oo leh EC50 qiimaha 99 nM [1].

Farnesoid X reseptor (FXR) waa reseptor bile acid nukliyeer ah oo ku lug leh homeostasis bile acid homeostasis, beerka fibrosis, caabuqa beerka iyo xiidmaha iyo cudurada wadnaha [2].

Obeticholic acid waa agonist FXR awood leh oo la xushay oo leh firfircoonida choleretic [1]. Obeticholic Acid waa xuubka bile acid-ka-soo-baxa iyo ligand FXR awood leh. Jiirka cholestasis ee estrogen-ku keeno, 6-ECCDCA waxay ka ilaalisay cholestasis ay keentay 17a-ethynylestradiol (E217α) [2]. Moodooyinka jiirka ee cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) waxay dib u kicisay FXR dariiqa calaamadaynta hoose waxayna hoos u dhigtay cadaadiska portal iyadoo hoos loo dhigayo wadarta iska caabbinta xididada xididada hepatic (IHVR) iyada oo aan lahayn hypotension nidaamsan. Saamayntan ayaa la xiriirta kororka dhaqdhaqaaqa eNOS [3]. Qaabka Dahl rat ee dhiig-karka xasaasiga ah ee cusbada iyo iska caabinta insulin-ta (IR), cuntada milixdu sarreeyso (HS) waxay si weyn u kordhisay cadaadiska dhiigga ee nidaamka iyo muujinta unugyada hoos u dhaca ee DDAH. INT-747 waxay xoojisay dareenka insulinta waxayna joojisay hoos u dhaca muujinta DDAH [4].

Tixraacyo:
[1] Pellicciari R, Fiorucci S, Camaioni E, iyo al. 6alpha-ethyl-chenodeoxycholic acid (6-ECCDCA), FXR agonist xoog leh oo la xushay oo lagu siiyay waxqabadka anticholestatic. J Med Chem, 2002, 45 (17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, iyo al. Saamaynta ilaalinta ee 6-ethyl chenodeoxycholic acid, ligand farnesoid X reseptor ligand, ee cholestasis ee estrogen-ku keeno. J Pharmacol Exp Ther, 2005, 313 (2): 604-612.
[3] Verbeke L, Farre R, Trebicka J, iyo al. Obeticholic acid, farnesoid X reseptor agonist, waxay wanaajisaa hypertension portal laba dariiqo oo kala duwan ee jiirka cirrhotic. Hepatology, 2014, 59 (6): 2286-2298.
[4] Ghebremariam YT, Yamada K, Lee JC, iyo al. FXR agonist INT-747 waxay hagaajisaa muujinta DDAH waxayna xoojisaa dareenka insulin ee jiirka Dahl ee la quudiyo milix badan. PLoS One, 2013, 8 (4): e60653.

Tixraaca Alaabta

• 1. Selina Costa. "Astaamaynta novel Ligand ee Farnesoid X soo dhaweynta iyadoo la adeegsanayo Zebrafish Transgenic." Jaamacadda Toronto. Jun-2018.
• 2. Kent, Rebecca. "Saamaynta Fenofibrate ee CYP2D6 iyo Xeerarka ANG1 iyo RNASE4 ee FXR Agonist Obeticholic Acid." indigo.uic.edu.2017.

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