Hōʻike huahana
ʻO Retatrutide kahi peptide triple agonist hou e kuhikuhi ana i ka glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), a me ka glucagon-like peptide-1 receptor (GLP-1R). Hoʻoikaika ʻo Retatrutide i ke kanaka GCGR, GIPR, a me GLP-1R me nā waiwai EC50 o 5.79, 0.0643, a me 0.775 nM, a me ka ʻiole GCGR, GIPR, a me GLP-1R me nā waiwai EC50 o 2.32, 0.191, a me 0. He mea hana noiʻi koʻikoʻi ia i ke aʻo ʻana i ka momona a me nā maʻi metabolic.
Hoʻoikaika maikaʻi ʻo Retatrutide i ke ala hōʻailona GLP-1R a hoʻoulu i ka huna ʻana o ka insulin i hilinaʻi i ka glucose ma o ka hana ʻana i nā mea loaʻa GIP a me GLP-1. Hōʻike kēia peptide synthetic i nā waiwai hypoglycemic ikaika a ua hoʻomohala ʻia ma ke ʻano he pūhui anti-diabetic no ka Type 2 Diabetes (T2D). Hoʻoikaika ia i ka hoʻokuʻu ʻana o ka insulin a hoʻopaʻa i ka huna ʻana o ka glucagon ma ke ʻano pili i ka glucose.
Hoʻohui ʻia, ua hōʻike ʻia ʻo Retatrutide e hoʻopaneʻe i ka hoʻokaʻawale ʻana o ka ʻōpū, e hoʻohaʻahaʻa i nā pae glucose hoʻokē ʻai a me ka postprandial glucose, hoʻemi i ka ʻai ʻana i ka meaʻai, a hoʻoulu i ke kaumaha nui o ke kino i nā poʻe me T2D.
Hana Ola
ʻO Retatrutide (LY3437943) kahi peptide lipid-conjugated hoʻokahi e hana ana ma ke ʻano he agonist ikaika o ke kanaka GCGR, GIPR, a me GLP-1R. Hoʻohālikelike ʻia me ka glucagon kanaka maoli a me ka GLP-1, hōʻike ʻo Retatrutide i ka haʻahaʻa haʻahaʻa ma GCGR a me GLP-1R (0.3 × a me 0.4 ×, kēlā me kēia) akā hōʻike i ka mana hoʻonui nui (8.9 ×) ma GIPR i hoʻohālikelike ʻia me ka glucose-dependent insulinotropic polypeptide (GIP).
Mechanism of Action
I nā haʻawina e pili ana i nā ʻiole diabetic me ka nephropathy, ʻo ka hoʻokele Retatrutide i hōʻemi nui i ka albuminuria a hoʻomaikaʻi i ka helu kānana glomerular. Hoʻopili ʻia kēia hopena pale i ka hoʻāla ʻana o ke ala hōʻailona hilinaʻi GLP-1R/GR, e hoʻopili ana i nā hana anti-inflammatory a me anti-apoptotic i loko o ka ʻiʻo renal.
Hoʻololi pololei ʻo Retatrutide i ka glomerular permeability, e hoʻonui ai i ka hiki ke hoʻopaʻa i ka mimi. Hōʻike nā ʻike mua, ke hoʻohālikelike ʻia me nā maʻi maʻi maʻi maʻamau e like me ka ACE inhibitors a me ARBs, hoʻopuka ʻo Retatrutide i kahi hōʻemi ʻoi aku o ka albuminuria ma hope o ʻehā pule o ka mālama ʻana. Eia kekahi, ua hōʻike ʻo ia i ka ʻoi aku ka maikaʻi o ka hōʻemi ʻana i ke koko systolic ma mua o nā ACE inhibitors a i ʻole ARBs, me ka ʻike ʻole ʻia o nā hopena ʻino.
Nā hopena ʻaoʻao
ʻO nā hopena ʻaoʻao maʻamau o Retatrutide he gastrointestinal ma ke ʻano, me ka nausea, ka ʻōpū, ka luaʻi, a me ka constipation. ʻO kēia mau hōʻailona maʻamau he ʻoluʻolu a haʻahaʻa a hoʻoholo ʻia me ka hoʻemi ʻana i ka nui. Ma kahi o 7% o nā mea i hōʻike pū ʻia i ka ʻili o ka ʻili. Ua ʻike ʻia ka piʻi ʻana o ka puʻuwai puʻuwai i nā wiki he 24 i nā pūʻulu kiʻekiʻe-dose, a ua hoʻi hou i nā pae kumu.