Whakaahuatanga

Ko te waikawa Obeticholic (INT-747) he agonist FXR kaha, whiriwhiri me te waha me te EC50 o 99 nM.Ko te waikawa Obeticholic he anticholeretic me te huanga anti-inflammation.Ko te waikawa Obeticholic hoki e whakaawe ana i te autophagy[1][2][3].

Papamuri

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) he agonist kaha me te whiriwhiri o te FXR me te uara EC50 o 99 nM [1].

Ko te Farnesoid X receptor (FXR) he kaikawe waikawa karihi karihi e uru ana ki te homeostasis waikawa bile, te ate fibrosis, te mumura ate me te intestinal me te mate cardiovascular [2].

Ko te Obeticholic Acid he agonist FXR kaha me te whiriwhiri me te mahi anticholeretic [1].Ko te Obeticholic Acid he huanga waikawa peera semisynthetic me te kaha FXR ligand.I roto i te estrogen-induced cholestasis kiore, 6-ECDCA i parea ki te cholestasis na te 17α-ethynylestradiol (E217α) [2].I roto i nga tauira kiore cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) i whakakorikorihia te ara tohu tohu FXR ki raro me te whakaheke i te pehanga o te tomokanga ma te whakaheke i te tapeke o te aukati vascular intrahepatic (IHVR) me te kore he whakahekenga kino.I hono tenei paanga ki te pikinga o te mahi eNOS [3].I roto i te tauira kiore Dahl o te tote-tairongo takawhita me te insulin-resistance (IR), te tote teitei (HS) kai i tino piki ake te pehanga toto nahanaha me te whakaputanga DDAH kiko.Ko te INT-747 te whakanui ake i te tairongo o te insulin me te aukati i te heke o te whakaaturanga DDAH [4].

Tohutoro:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), he agonist FXR kaha me te whiriwhiri kua whakawhiwhia ki te mahi anticholestatic.J Med Chem, 2002, 45(17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Ko nga paanga whakamarumaru o te waikawa 6-ethyl chenodeoxycholic, he ligand kaikawe X farnesoid, i roto i te cholestasis i whakaawehia e te estrogen.J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.Ko te waikawa Obeticholic, he agonist kaiawhina X farnesoid, he whakapai ake i te takawhita kuaha ma nga ara motuhake e rua i roto i nga kiore cirrhotic.Hepatology, 2014, 59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.Ko te FXR agonist INT-747 e whakatika ana i te whakaaturanga DDAH me te whakanui ake i te tairongo o te insulin i roto i nga kiore Dahl whangai nui-tote.PLoS One, 2013, 8(4): e60653.

Tohunga Hua

• 1. Selina Costa."Whakaahua i te Novel Ligand mo te Farnesoid X Receptor ma te whakamahi i te Transgenic Zebrafish."Te Whare Wananga o Toronto.Hune-2018.
• 2. Kent, Ripeka."Ko nga paanga o Fenofibrate i runga i te CYP2D6 me te Ture o ANG1 me te RNASE4 na te FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

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