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1 ngwa (10 Vials)
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▎ Ọdịdị Retatrutid
Isi mmalite: PubChem |
Usoro: YA⊃1;QGTFTSDYSI-L⊃2;LDKK⁴AQA⊃1;AFIEYLLEGGPSSGAPPPS⊃3; Ụdị mkpụrụ ndụ: C 221H 342N 46O68 Ibu ibu: 4731 g/mol Nọmba CAS: 2381089-83-2 PubChem CID: 171390338 Ndị otu: LY3437943 |
▎ Nnyocha Retatrutid
Kedu ihe ndabere nyocha nke Retatrutid?
Nchọpụta nyocha nke Retatrutid nwere njikọ chiri anya na nsogbu zuru ụwa ọnụ na-arịwanye elu nke oke ibu na ọrịa shuga, yana njedebe nke ọgwụ ọgwụgwọ dị ugbu a: oke ibu na ọrịa shuga na-ebute ahụike ọha na eze egwu, yana ọnụ ọgụgụ oke ibu zuru ụwa ọnụ ga-eru ijeri 4.005 site na 2035 yana ọnụ ọgụgụ ndị ọrịa shuga na-abawanye ruo nde 592, na-akpata ahụike zuru ụwa ọnụ. Multi- target receptor agonist peptides apụtala dị ka ihe ngwọta, nke nwere ike igbochi oke ibu, na-agwọ ọrịa shuga, na izere mmetụta ndị na-egbu egbu nke ọgwụ ndị dị adị, na-eme ka ha bụrụ usoro na mmepe nke oke ibu na ọgwụgwọ ọrịa shuga.
Kedu ihe bụ usoro Retatrutid?
Na-achịkwa metabolism ike site na ịgbalite multi-receptor
Retatrutid bụ agonist atọ na-anabata ihe na-elekwasị anya na insulinotropic polypeptide receptor (GIPR), glucagon-like peptide-1 receptor (GLP-1R), na onye na-anabata glucagon (GCGR). Ọ n'out oge activates ndị a atọ anabata, na-achịkwa ike metabolism site multiple ụzọ.
GIPR agonist ọrụ:
GIP bụ hormone na-ezobe insulin nke eriri afọ nke mkpụrụ ndụ eriri afọ K na-ewepụta ma wepụta ya mgbe nri gasịrị. Retatrutid na-arụ ọrụ GIPR, na-akwalite mmepụta insulin, na-eme ka mmetụta insulin dịkwuo elu, ma si otú a na-enyere ahụ ahụ aka ịmịkọrọ ma jiri glucose mee ihe nke ọma, si otú ahụ na-ebelata ọkwa glucose ọbara. Na mgbakwunye, GIP nwere ike imetụta metabolism abụba site na ịhazi ọrụ adipocyte na ibelata mkpokọta abụba [1].
Ọrụ agonist GLP-1R:
GLP-1 bụ hormone peptide nke sel intestinal L na-emepụta. Mgbe ịgbalite GLP-1R, Retatrutid na-emepụta mmetụta bara uru dị iche iche. Ọ nwere ike kpalite mmepụta insulin n'ụzọ dabere na mkpokọta glucose, si otú a na-ebelata ọkwa shuga dị n'ọbara. Ọ nwere ike igbu oge mkpofu afọ, mụbaa satiety, ma belata oriri. GLP-1R agonism nwekwara ike na-arụ ọrụ na Central ụjọ usoro, na-achịkwa agụụ na ume itule, si otú na-enyere aka na ibu ibu [2].
Mmetụta GCGR agonist:
Glucagon na-abawanye ọkwa glucose ọbara, mana n'okpuru mmetụta nke Retatrutid, GCGR agonism na-arụpụta mmetụta dị iche iche. Ọ na-akwalite glycogenolysis na gluconeogenesis na imeju. N'okpuru mmetụta jikọtara ọnụ nke Retatrutid, ahụ anaghị enwe mmụba dị mfe na ọkwa glucose ọbara kama kama ọ na-achịkwa metabolism ike iji mee ka mmebi abụba dịkwuo elu, si otú a na-enweta ibu ibu na mma metabolism. GCGR agonism nwekwara ike imetụta metabolism lipid imeju, na-ebelata mkpokọta abụba imeju [3].
Mmetụta na Usoro Mmekọahụ metụtara Metabolism
Site n'ime otu oge na ndị nnata atọ ahụ a kpọtụrụ aha, Retatrutid na-emetụta ọtụtụ usoro physiological metụtara metabolism.
Usoro nchịkwa glucose ọbara:
Site na ịgbalite GIPR na GLP-1R iji kwalite mmepụta insulin, yana ịhazi GCGR nke ọma, Retatrutid nwere ike belata ọkwa glucose ọbara. A na-akpọ mmetụta hypoglycemic ya mgbe ọkwa glucose ọbara dị elu, ebe o yighị ka ọ ga-ebute hypoglycemia mgbe glucose ọbara dị mma, nke bara uru maka njikwa glucose ọbara n'ime ndị ọrịa nwere ọrịa shuga ..
Njikwa ibu:
Retatrutid na-egosipụta nrụpụta dị ukwuu na njikwa ibu. Site na ịgbalite GLP-1R, ọ na-ebelata mkpofu afọ, na-abawanye satiety, ma na-ebelata oriri; site n'ịchịkwa abụba metabolism, ọ na-akwalite mmebi abụba na mmefu ume, si otú a na-enweta ibu ibu. Nnwale ụlọ ọgwụ egosila na ndị ọrịa buru ibu ma ọ bụ ndị buru oke ibu na Retatrutid na-enweta oke ibu dị arọ n'ime oge ụfọdụ [5,6].
Iwu Lipid:
Ọgwụgwọ Retatrutid na-eme ka profaịlụ lipid ndị ọrịa dịkwuo mma. Ọ na-ebelata triglyceride (TG), cholesterol lipoprotein dị obere (LDL-C), yana oke lipoprotein cholesterol (VLDL-C) dị obere, na-achịkwa apolipoproteins, dị ka iweda apolipoprotein B (apoB) na apolipoprotein C -III (apoC-by) na-ebelata ọkwa nke lipoproteins, na-ebelata ọnụ ọgụgụ lipoproteins nke lipoproteins, na-ebelata ọnụ ọgụgụ lipoproteins nke lipoproteins. na-akwalite ahụ ike obi [7].
Melite metabolism lipid imeju:
Maka ndị ọrịa nwere ọrịa imeju na-adịghị egbu egbu (NAFLD) metụtara dysfunction metabolic, Retatrutid na-ebelata nke ukwuu ọdịnaya abụba imeju. N'ime ule ụlọ ọgwụ dị mkpa, ndị ọrịa na-eji ọgwụ dị iche iche nke Retatrutid gosipụtara mbelata nke ukwuu na abụba imeju ma e jiri ya tụnyere ntọala, na-egosi na Retatrutid nwere mmetụta nchịkwa dị mma na metabolism abụba imeju, nke bara uru maka imeziwanye ọrụ imeju [3]..
Ọgụgụ 1 Usoro nke Retatrutid [8].
Kedu ihe bụ ngwa Retatrutid?
Ọgwụgwọ oke ibu:
Ibu ibu aghọwo isi okwu ahụike ọha na eze zuru ụwa ọnụ, jikọtara ya na mmalite na ọganihu nke ọrịa dị iche iche na-adịghị ala ala. Retatrutid egosila nrụpụta dị ukwuu na ọgwụgwọ oke ibu. Ndị ọrịa buru ibu ejiri Retatrutid gwọọ ha nwetara mbelata pụtara ìhè na ịdị arọ ahụ. N'ime izu 48 nke ọmụmụ oke ibu nke Phase 2, ndị ọrịa na-agwọ 8mg na 12mg nke Retatrutid nwetara mbelata ịdị arọ nke 22.8% na 24.2%, n'otu n'otu. N'ọkwa ọzọ nke abụọ kpuru ìsì abụọ, randomized, ebe a na-achịkwa ebebo, ndị ọrịa nọ n'ìgwè dose dị iche iche nwetara ogo dị iche iche nke ịdị arọ na izu 24 na izu 48. Otu 12mg nwetara mbelata ibu nke 24.2% na izu 48, ebe otu placebo naanị hụrụ mbelata -2.1%. Retatrutid na-ebelata ibu ahụ nke ọma na ndị ọrịa buru ibu, na-enye ngwa ọhụrụ dị ike maka ọgwụgwọ oke ibu. Usoro ọgwụgwọ Retatrutid maka oke ibu ọ bụghị naanị na-ebelata ibu ahụ kamakwa ọ nwekwara ike imeziwanye nsogbu ahụike ndị ọzọ metụtara oke ibu, dị ka ibelata nrụgide nkwonkwo na iwepụ ihe mgbaàmà nke ọrịa nkwonkwo metụtara oke ibu site na nkwụsị ibu; Mbelata ibu ahụ nwekwara ike inye aka melite nsogbu ndị metụtara oke ibu dị ka apnea ụra [3,6].
Ọgwụgwọ ụdị ọrịa shuga 2:
Ụdị ọrịa shuga 2dị nke abụọ bụ ọrịa metabolic na-adịghị ala ala nke e ji nguzogide insulin na ụkọ insulin ezughi oke. Retatrutid nwere ike itinye uru na ọgwụgwọ ụdị ọrịa shuga 2. Ọ na-akpali mmepụta insulin site na ịgbalite onye na-anabata GLP-1, na-eme ka nguzogide insulin dịkwuo mma, na-ebelata ọkwa glucose ọbara. Mmetụta mbelata ibu ya na-enyekwa aka melite ọnọdụ nke ndị ọrịa shuga 2dị nke abụọ, n'ihi na oke ibu bụ ihe dị mkpa dị ize ndụ maka ụdị ọrịa shuga 2, na mbelata ibu nwere ike ime ka mmetụta insulin dịkwuo elu, na-enyere aka n'ịchịkwa glucose ọbara. N'ime ọmụmụ ihe metụtara ndị ọrịa nwere ụdị ọrịa shuga 2, Retatrutid butere oke ibu na mbelata ọkwa haemoglobin A1c (HbA1c), yana HbA1c na-agbada site na 1.64% ma e jiri ya tụnyere placebo. Nke a na-egosi na Retatrutid abụghị naanị na-achịkwa ọkwa glucose ọbara nke ọma kamakwa ọ na-eme ka ọnọdụ ndị ọrịa nwere ụdị ọrịa shuga 2 dịkwuo mma site n'ọtụtụ usoro, gụnyere oke ibu, si otú ahụ na-eme ka ndụ ha dịkwuo mma ..
Ọgwụgwọ ọrịa imeju na-adịghị egbu egbu (NAFLD):
NAFLD bụ mmerụ ahụ nke imeju na-akpata nrụgide metabolic jikọtara ya na nguzogide insulin na ike mkpụrụ ndụ ihe nketa, na-agụnye ọnọdụ dị iche iche gụnyere imeju abụba na-abụghị mmanya na-aba n'anya, steatohepatitis na-abụghị mmanya na-aba n'anya, na cirrhosis metụtara ya. Retatrutid na-egosi ikike na-ekwe nkwa na ọgwụgwọ NAFLD. Na a randomized, okpukpu abụọ-ìsì, placebo-achịkwa ikpe metụtara ndị sonyere na metabolic dysfunction-metụtara abụba imeju ọrịa na imeju abụba ọdịnaya ≥10%, na 24 izu, pụtara ikwu mgbanwe n'ime imeju abụba ọdịnaya si baseline dị nnọọ iche n'ofe Retatrutid dose dị iche iche: -81.4% na 8mg otu, -82.4% na otu +1.bo. Nke a na-egosi na Retatrutid nwere ike belata ọdịnaya abụba imeju nke ọma, nke dị oke mkpa maka imezi usoro imeju nke ndị ọrịa NAFLD. Ọ na-ekwe nkwa dị ka nhọrọ ọgwụgwọ ọhụrụ maka NAFLD, nwere ike ibelata ọganihu ọrịa yana ibelata ihe ize ndụ nke nsogbu siri ike dị ka cirrhosis [3].
Mmechi
Retatrutid na-egosi ikike na-ekwe nkwa imeziwanye ọnọdụ ọrịa imeju nke ndị ọrịa NAFLD, na-eme ihe site n'ọtụtụ usoro gụnyere ịhazi metabolism ike, melite nguzogide insulin, mmetụta mgbochi mkpali, na mezie metabolism lipid.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Rosenstock, J bụ ọkà mmụta pụtara ìhè nke ọrụ ya nwere njikọ chiri anya na ọtụtụ ụlọ ọrụ ama ama, gụnyere Mahadum Texas Southwestern Medical Center, Mahadum Texas Dallas, na Canadian VIGOR Center. Nnyocha ya gbasara ọtụtụ ngalaba dị ka Endocrinology & Metabolism, General & Internal Medicine, Cardiovascular System & Cardiology, Pharmacology & Pharmacy, na Research & Experimental Medicine. Ntụnye dị ịrịba ama o nyere ndị obodo agụmakwụkwọ emeela ka ọ nweta nkwanye ùgwù zuru oke, dị ka egosipụtara site na nhọpụta ya ugboro ugboro dị ka onye nyocha nke ọma na ngalaba nke Clinical Medicine site na 2017 ruo 2024, na-egosipụta ọkwa ya dị ịrịba ama na mmetụta dị ukwuu na nyocha ahụike ụlọ ọgwụ. Edepụtara Rosenstock J na ntụaka ntụaka [4].
