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.Obeticholic acid sidoo kale waxay 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 reseptors 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 door ah oo leh firfircoonida choleretic [1].Obeticholic Acid waa soosaar bile acid semisynthetic iyo ligand FXR awood leh.Jiirka cholestasis ee estrogen-ku keeno, 6-ECCDCA waxay ka ilaalisay cholestasis ay keentay 17a-ethynylestradiol (E217α) [2].Noocyada jiirka ee cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) waxay dib u kicisay dariiqa calaamadaynta FXR ee 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 caabbinta insulin-ta (IR), cuntada milixda badan (HS) waxay si weyn u kordhisay cadaadiska dhiigga ee nidaamka iyo muujinta unugyada hoos u dhaca ee DDAH.INT-747 waxay xoojisay dareenka insulin 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 uu keeno estrogen.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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