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 huanga anticholeretic me te anti-inflammation. Ko te waikawa Obeticholic ano hoki ka whakaawe 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 fibrosis ate, 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 e kino te mate hypotension. I hono tenei paanga ki te piki haere o te mahi eNOS [3]. I roto i te tauira kiore Dahl o te tote-tairongo takawhita me te insulin-resistance (IR), kai tote teitei (HS) tino whakanui ake te pēhanga toto pūnahanaha me downregulated kiko DDAH whakaaturanga. 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 chenodeoxycholic 6-ethyl, he herenga kaiwhakawhiwhi X farnesoid, i roto i te cholestasis-whakaawe i 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 o te tomokanga 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 whakarei ake i te maarama o te insulin i roto i nga kiore Dahl whangai-nui. 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 te 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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