Nkọwa

Obeticholic acid (INT-747) bụ onye nwere ike, nhọrọ na ọnụ na-arụ ọrụ FXR agonist nwere EC50 nke 99 nM.Obeticholic acid nwere mmetụta anticholeretic na mgbochi mkpali.Obeticholic acid na-ebutekwa autophagy[1] [2] [3].

ndabere

Obeticholic acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECCDCA, INT-747) bụ agonist nwere ike na nhọrọ nke FXR nwere EC50 uru nke 99 nM [1].

Farnesoid X receptor (FXR) bụ onye na-anabata bile acid nuklia na-etinye aka na bile acid homeostasis, fibrosis imeju, ịba ọcha n'anya na eriri afọ na ọrịa obi [2].

Obeticholic acid bụ FXR agonist dị ike ma họrọ nke nwere ọrụ anticholeretic [1].Obeticholic acid bụ ihe na-emepụta bile acid semisynthetic yana ligand FXR nwere ike.N'ime oke cholestasis nke estrogen kpatara, 6-ECDCA na-echebe megide cholestasis sitere na 17a-ethynylestradiol (E217α) [2].N'ụdị ọbara mgbali elu cirrhotic portal (PHT), INT-747 (30 mg / kg) megharịrị ụzọ akara ngosi FXR dị ala ma belata nrụgide portal site na ibelata mkpokọta intrahepatic vaskụla nguzogide (IHVR) na-enweghị hypotension systemic.Ejikọtara mmetụta a na mmụba eNOS [3].N'ihe atụ Dahl oke nke ọbara mgbali elu na-enwe mmetụta nke nnu na insulin-resistance (IR), nri nnu dị elu (HS) mụbara ọbara mgbali sistemu na okwu DDAH anụ ahụ mebiri emebi.INT-747 kwalitere mmetụta insulin ma gbochie mbelata okwu DDAH [4].

Ntụaka:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), FXR agonist nwere ike na nhọrọ nke enyere ọrụ anticholestatic.J Med Chem, 2002, 45 (17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Mmetụta nchebe nke 6-ethyl chenodeoxycholic acid, ligand farnesoid X na-anabata ya, na cholestasis nke estrogen kpatara.J Pharmacol Exp Ther, 2005, 313 (2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.Obeticholic acid, farnesoid X agonist anabata, na-eme ka ọbara mgbali elu portal dịkwuo mma site n'ụzọ abụọ dị iche iche na oke cirrhotic.Hepatology, 2014, 59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.FXR agonist INT-747 na-akwalite okwu DDAH ma na-eme ka mmetụta insulin dịkwuo elu na oke Dahl nri nnu.PLoS Otu, 2013, 8 (4): e60653.

Ndepụta ngwaahịa

• 1. Selina Costa."Ịmepụta Ligand novel maka onye na-anabata Farnesoid X site na iji Transgenic Zebrafish."Mahadum Toronto.Jun-2018.
• 2. Kent, Rebecca."Mmetụta nke Fenofibrate na CYP2D6 na Iwu nke ANG1 na RNASE4 site na FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

Nchekwa

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