Tlhaloso ea Sehlahisoa
Retatrutide ke buka e ncha ea agonist peptide e lebisitsoeng ho glucagon receptor (GCGR), insulinotropic polypeptide receptor (GIPR) e itšetlehileng ka tsoekere, le glucagon-like peptide-1 receptor (GLP-1R). Retatrutide e kenya tšebetsong GCGR, GIPR, le GLP-1R ea motho ka litekanyetso tsa EC50 tsa 5.79, 0.0643, le 0.775 nM, ka ho latellana, le mouse GCGR, GIPR, le GLP-1R e nang le litekanyetso tsa EC50 tsa 2.32, 0.0.191 le nM 0.0.191 E sebetsa e le sesebelisoa sa bohlokoa sa ho etsa lipatlisiso thutong ea botenya le mathata a metabolism.
Retatrutide e kenya tšebetsong tsela ea pontšo ea GLP-1R ka nepo mme e hlohlelletsa secretion ea insulin e itšetlehileng ka tsoekere ka ho sebetsa ho li-receptor tsa GIP le GLP-1. Peptide ena ea maiketsetso e bonts'a thepa e matla ea hypoglycemic mme e ntlafalitsoe joalo ka motsoako o thibelang lefu la tsoekere bakeng sa Mofuta oa 2 oa Lefu la tsoekere (T2D). E khothalletsa ho lokolloa ha insulin le ho hatella secretion ea glucagon ka mokhoa o itšetlehileng ka tsoekere.
Ho phaella moo, Retatrutide e bontšitsoe ho liehisa ho tsoa ka mpeng, ho fokotsa maemo a tsoekere ea ho itima lijo le ka mor'a lijo, ho fokotsa ho ja lijo, le ho etsa hore batho ba nang le T2D ba fokotsehe haholo.
Mosebetsi oa Likokoana-hloko
Retatrutide (LY3437943) ke peptide e le 'ngoe ea lipid-conjugated e sebetsang e le agonist e matla ea GCGR, GIPR, le GLP-1R ea motho. Ha e bapisoa le glucagon ea tlhaho ea motho le GLP-1, Retatrutide e bonts'a matla a tlase ho GCGR le GLP-1R (0.3× le 0.4×, ka ho latellana) empa e bonts'a matla a ntlafalitsoeng haholo (8.9×) ho GIPR ha e bapisoa le insulinotropic polypeptide e itšetlehileng ka tsoekere (GIP).
Mokhoa oa Ts'ebetso
Lithutong tse amang litoeba tse nang le lefu la tsoekere tse nang le nephropathy, tsamaiso ea Retatrutide e fokolitse albuminuria haholo le sekhahla se ntlafalitsoeng sa filthara ea glomerular. Tšireletso ena e bakoa ke ts'ebetso ea tsela ea pontšo e itšetlehileng ka GLP-1R/GR, e hokahanyang liketso tse khahlanong le ho ruruha le tse khahlanong le apoptotic liseleng tsa renal.
Retatrutide e boetse e fetola glomerular permeability ka ho toba, e ntlafatsa bokhoni ba ho tsepamisa mohopolo. Liphuputso tsa pele li fana ka maikutlo a hore, ha ho bapisoa le phekolo e tloaelehileng ea mafu a liphio a sa foleng a kang ACE inhibitors le ARBs, Retatrutide e hlahisa phokotso e hlakileng haholoanyane ea albuminuria ka mor'a libeke tse 'nè feela tsa phekolo. Ho feta moo, e bontšitse katleho e kholo ea ho fokotsa khatello ea mali ea systolic ho feta ACE inhibitors kapa ARBs, ho se na liphello tse bohloko tse bonoang.
Litla-morao
Litla-morao tse atileng haholo tsa Retatrutide ke tsa tlhaho ea mala, ho kenyelletsa ho nyekeloa ke pelo, letšollo, ho hlatsa le ho patoa. Matšoao ana ka kakaretso a bobebe ho isa ho a itekanetseng 'me a atisa ho rarolla ka phokotso ea lethal dose. Hoo e ka bang 7% ea barupeluoa le bona ba tlalehile maikutlo a ho tsikinyeha ha letlalo. Ho eketseha ha lebelo la pelo ho ile ha hlokomeloa libeke tsa 24 lihlopheng tsa litekanyetso tse phahameng, tseo hamorao li ileng tsa khutlela maemong a motheo.