Shaanxi BLOOM Tech Co., Ltd. yog ib tug ntawm cov uas paub txog manufacturers thiab lwm tus neeg ntawm octreotide ntsiav tshuaj nyob rau hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo octreotide ntsiav tshuaj muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Octreotide ntsiav tshuajyog ib qho khoom siv hluavtaws octapeptide derivative, teej tug mus rau chav kawm ntawm somatostatin analogs. Nws yog dav siv hauv kev kho mob rau kev kho mob ntawm ntau yam kab mob, tshwj xeeb tshaj yog nyob rau hauv cov xwm txheej uas cov tshuaj hormone secretion thiab qog muaj feem xyuam rau cov tsos mob yuav tsum tau tswj, los ntawm mimicking qhov kev txiav txim ntawm ntuj somatostatin. Raws li daim ntawv qhia qhov ncauj ntawm octreotide, octreotide lub hom phiaj los muab txoj hauv kev yooj yim dua thiab tus neeg mob tus phooj ywg ntawm kev tswj hwm. Txawm li cas los xij, tam sim no cov ntaub ntawv tseem ceeb ntawm octreotide nyob rau hauv kev ua lag luam yog kev txhaj tshuaj, suav nrog kev txhaj tshuaj thiab ntev - ua cov tshuaj microsphere, thaum daim ntawv thov ntawm cov ntsiav tshuaj ntawm qhov ncauj yog qhov txwv, feem ntau yog vim kev nqus thiab ruaj khov ntawm octreotide hauv plab hnyuv.
Peb Cov Khoom Muag Khoom
Octreotide COA
Molecular mechanism thiab txoj hauv kev ntawm kev ua ntawm octreotide nyob rau hauv lub zog inhibition ntawm ntau yam tshuaj hormone secretion
Raws li ib tug classic synthetic somatostatin analogue,octreotide ntsiav tshuajtau muaj cov ntaub ntawv kho mob nyob deb dhau qhov chaw pib endocrine txij li lawv tau qhia hauv xyoo 1980s. Kev hloov kho cov qauv ntawm peptide chemistry endows nws nrog metabolic stability superior rau tej yam ntuj tso somatostatin, ua rau nws ib tug tseem ceeb riam phom rau kev kho mob acromegaly, neuroendocrine hlav, thiab tswj esophageal thiab gastric variceal los ntshav.
Cov tshuaj tseem ceeb ntawm octreotide: kev sib xyaw ua ke ntev ntev - ua yeeb yam somatostatin analogs
Octreotide tsis yog cov tshuaj tshiab nrog cov txheej txheem tshiab ntawm kev ua, tab sis cov khoom sib txuas ntawm ntuj somatostatin (SST). Tej yam ntuj tso somatostatin yog ib tug dav tam sim no inhibitory tswj peptide nyob rau hauv tib neeg lub cev, lub luag hauj lwm rau inhibiting ntau tshaj tawm ntawm yuav luag tag nrho cov endocrine thiab exocrine hormones.
Qhov tsis zoo ntawm ntuj somatostatin: luv heev ib nrab-lub neej, tsuas yog 1-3 feeb; Tsis tuaj yeem noj hauv qhov ncauj, tuaj yeem tsuas yog txuas ntxiv mus rau hauv cov hlab ntsha; Cov nyhuv yog luv luv thiab tswj tsis tau cov tshuaj hormone secretion rau lub sijhawm ntev
Octreotide ua tiav peb qhov kev hloov pauv tseem ceeb los ntawm kev hloov kho cov qauv amino acid: ua kom ntev ib nrab -lub neej (txog 90 feeb lossis ntau dua); Lub zog ntawm qhov kev txiav txim yog nce ntau zaus mus rau kaum tawm zaus; Siab receptor affinity thiab muaj zog selectivity
Yog li ntawd, octreotide tuaj yeem nyob ruaj khov, tsis tu ncua, thiab ua haujlwm zoo ntawm cov haujlwm tseem ceeb ntawm somatostatin - broad -spectrum inhibition ntawm cov tshuaj hormones secretion.
Lub hauv paus tseem ceeb rau cov nyhuv inhibitory ntawm octreotide: somatostatin receptor
Somatostatin receptors (SSTRs) tau muab faib ua 5 pawg: SSTR1 / SSTR2 / SSTR3 / SSTR4 / SSTR5
Cov receptors no tau nthuav dav hauv: anterior pituitary caj pas / pancreatic alpha / beta / delta hlwb / plab hnyuv endocrine hlwb / nruab nrab paj hlwb / ntau yam neuroendocrine qog cell membranes
Txhua lub xov tooj ntawm tes nrog kev qhia siab ntawm SSTR tuaj yeem cuam tshuam los ntawm octreotide.
Cov yam ntxwv affinity ntawm octreotide rau receptors
Octreotide muaj qhov sib txuam siab tshaj plaws rau SSTR2, ua raws li SSTR5 thiab SSTR3.
SSTR2 yog qhov tseem ceeb tshaj plaws subtype mediating hormone inhibitory teebmeem: kev loj hlob hormone (GH) inhibition; inhibit insulin thiab glucagon; Inhibit gastrin VIP, Gastrointestinal hormones xws li pancreatic secretin; Kev sib raug zoo siab =tsis tshua muaj siab tuaj yeem ua tau zoo khi thiab qhib cov cim inhibitory.
Qhov no yog lub hauv paus txheej txheem ntawm octreotide lub peev xwm los inhibit cov tshuaj hormones hauv cov koob tshuaj me me, nrog rau ntev - kav ntev thiab dav - spectrum cuam tshuam.
Txoj hauv kev zoo tshaj plaws ntawm octreotide inhibiting hormone secretion
Kauj Ruam 1: Kev khi nrog SSTR ntawm lub cell membrane
Octreotide ua raws li ligand thiab khi rau SSTR (tsuas yog SSTR2) nyob rau saum npoo ntawm lub hom phiaj cell membrane.
Tom qab kev sib txuas, cov receptor conformation hloov, pib intracellular inhibitory signals.
Kev sib txuas ceev ceev, qeeb dissociation ceev → ntev - cov nyhuv kav ntev.
Kauj Ruam 2: Ua kom inhibitory G protein (Gi / o protein)
SSTR belongs rau G protein coupled receptors (GPCRs).
Tom qab ua kom tiav, Gi / o inhibitory G protein yog nyiam ua ke.
Tom qab Gi/o activation, ob qhov teebmeem tseem ceeb raug tsim:
Inhibition ntawm adenylate cyclase (AC)
Txo cov kev tsim tawm ntawm intracellular cAMP
CAMP yog tus xa xov tseem ceeb thib ob uas txhawb nqa kev zais ntawm cov tshuaj hormones feem ntau.
Yog li, cAMP ↓=hormone secretion yog inhibited heev.
Kauj Ruam 3: Inhibit voltage-gated Ca ² ⁺ channels thiab txo cov calcium ion influx
Hormone secretion cia siab rau extracellular Ca ² ⁺ influx kom ua rau vesicle tso.
Octreotide ntsiav tshuajncaj qha inhibits voltage-gated Ca ² ⁺ channels los ntawm Gi/o proteins.
Ca ² ⁺ influx txo qis → intracellular Ca ² ⁺ concentration tsis tuaj yeem ncav cuag qhov pib zais cia.
Qhov tshwm sim: Hormone vesicles tsis tuaj yeem tso tawm → zais zais cia.
Kauj Ruam 4: Ua kom K ⁺ channels rau hyperpolarize cell membrane
Octreotide activates inward rectifying potassium raws (GIRK).
K ⁺ efflux nce → cell membrane hyperpolarization.
Cells yog qhov nyuaj rau excite thiab tsim kom muaj peev xwm ua.
Hyperpolarized xeev → Cells nyob rau hauv 'so inhibitory hom' → Hormone basal secretion thiab stimulated secretion ob qho tib si txo.
Kauj Ruam 5: Inhibit proliferation pathways xws li MAPK/ERK thiab txo cov tshuaj hormone synthesis
Octreotide tsis tsuas yog inhibits cov tshuaj hormones tso tawm, tab sis kuj suppresses cov tshuaj hormones synthesis.
Los ntawm inhibiting txoj kev MAPK/ERK thiab PI3K/Akt txoj kev
Cov txiaj ntsig: Hormone gene transcription ↓, hormone protein translation ↓, cell proliferation ntau dhau ↓
Qhov no ua rau octreotide txo qis cov tshuaj hormones los ntawm qhov chaw.
Lub zog inhibitory mechanism ntawm octreotide ntawm ntau yam tshuaj hormones
Muaj zog inhibition ntawm pituitary loj hlob hormone (GH) secretion
Pituitary txoj kev loj hlob hormone hlwb heev nthuav qhia SSTR2 thiab SSTR5.
Tom qab khi nrog octreotide: cAMP ↓, Ca ² ⁺ influx ↓, cell membrane hyperpolarization, muaj zog inhibiting pulsatile thiab basal secretion ntawm GH.
Ib txhij inhibiting GH noob transcription thiab txo synthesis.
Thaum kawg, nws ua rau txo qis hauv cov ntshav GH thiab IGF-1, tswj acromegaly.
Muaj zog inhibition ntawm thyroid stimulating hormone (TSH) secretion & muaj zog inhibition ntawm insulin secretion
Cov thyroid stimulating hormone hlwb kuj qhia SSTR.
Octreotide tuaj yeem cuam tshuam qhov txawv txav ntawm TSH.
Siv rau cov qog pituitary tsawg xws li cov qog TSH kom txo qis TSH theem sai.
Pancreatic beta hlwb qhia SSTR.
Octreotide inhibits cov piam thaj hauv insulin tso tawm.
Mechanism: inhibit Ca ² ⁺ influx, txo cAMP, thiab inhibit insulin vesicle exocytosis
Muaj zog inhibition ntawm glucagon secretion & muaj zog inhibition ntawm gastrin secretion
Pancreatic alpha hlwb kuj inhibited los ntawm octreotide.
Oversecretion ntawm glucagon yuav ua rau cov ntshav qab zib nce ntxiv thiab ua rau mob ntshav qab zib ntau ntxiv.
Octreotide tuaj yeem sib npaug ntawm insulin thiab glucagon ib txhij.
Gastric antral G hlwb qhia SSTR.
Octreotide ncaj qha inhibits gastrin tso tawm.
Gastrin → gastric acid secretion.
Siv rau Zollinger Ellison syndrome (gastrinoma) thiab refractory ulcers.
Cov txheej txheem tshwj xeeb uas cov tshuaj no txo qhov siab ntawm lub portal
Thaum lub siab ua rau lub siab ua rau lub cev muaj zog, lub cev muaj kev cuam tshuam loj heev ntawm cov neurohumoral, uas ntxiv dag zog rau visceral vascular dilation, nce ntshav txaus, thiab ua rau cov ntshav siab ntxiv.Octreotide ntsiav tshuajinhibits qhov tso tawm ntawm ntau yam vasodilator ntsig txog cov tshuaj hormones, tswj kev sib npaug ntawm neurohumoral, tsis ncaj qha txo cov ntshav visceral, thiab txo qis portal siab.
Vasoactive plab hnyuv peptide (VIP) yog lub zog vasodilator. Thaum lub sij hawm portal hypertension nyob rau hauv daim siab cirrhosis, lub secretion ntawm VIP los ntawm endocrine hlwb nyob rau hauv lub plab hnyuv ib ntsuj av tau nce (2-3 zaug siab dua li ib txwm). VIP activates VIP receptors ntawm vascular du leeg hlwb, txhawb vascular dilation, nce visceral ntshav txaus, thiab exacerbates portal siab.
Octreotide zoo inhibits kev sib txuas thiab tso tawm ntawm VIP los ntawm kev khi rau SSTR2 ntawm endocrine hlwb hauv plab hnyuv, txo VIP concentration hauv cov ntshav los ntawm 30% -40%, yog li txo VIP mediated visceral vasodilation, indirectly txhim kho visceral vasoconstriction, txo cov ntshav txaus, thiab txo qhov portal siab.
inhibit glucagon secretion thiab sib npaug vascular nro
Glucagon tseem yog ib qho tseem ceeb vasodilator. Nyob rau hauv cirrhosis nrog portal hypertension, pancreatic alpha hlwb secrete ntau glucagon, uas inhibits cov leeg nqaij contraction thiab txhawb tsis muaj ntau lawm, ua rau visceral vasodilation thiab nce ntshav txaus.
Octreotide muaj cov nyhuv inhibitory ntawm glucagon, uas tuaj yeem txo qhov concentration ntawm glucagon hauv cov ntshav los ntawm 40% -50%, txo cov nyhuv vasodilation ntawm glucagon ntawm cov hlab ntsha visceral, thiab sib npaug ntawm qhov sib piv ntawm insulin rau glucagon, tsis txhob cuam tshuam ncaj qha rau vascular tone los ntawm cov ntshav qabzib hloov pauv thiab ntxiv stabilizing portal siab.
Thaum lub portal hypertension tshwm sim nyob rau hauv cirrhosis, lub sympathetic paj hlwb tseem muaj kev zoo siab, ua rau muaj kev nce nyob rau hauv lub secretion ntawm catecholamines xws li norepinephrine thiab adrenaline. Txawm hais tias cov tshuaj no lawv tus kheej muaj qhov cuam tshuam vasoconstrictive, ntev -lub sij hawm sympathetic paj hlwb excitation tuaj yeem ua rau txo qis ntawm cov hlab ntsha hauv cov hlab ntsha mus rau cov teeb liab contraction (desensitization), thaum txhawb kev tso tawm ntawm cov kab mob inflammatory (xws li TNF - , IL-6), indirectly ua rau cov hlab ntsha.
Octreotide activates SSTR ntawm lub hauv nruab nrab lub paj hlwb, inhibits ntau excitation ntawm lub sympathetic paj hlwb, txo cov secretion ntawm catecholamines, inhibits kev tso tawm ntawm inflammatory yam, tsis txhob desensitization ntawm visceral hlab ntsha, txhim khu lub rhiab heev ntawm cov hlab ntsha mus rau contraction signals, visceral hlab ntsha.
Tswj renin angiotensin aldosterone system (RAAS) thiab txo cov dej thiab sodium retention
Hauv cirrhotic portal hypertension, RAAS system dhau lawm, thiab kev tso tawm ntawm renin, angiotensin II, thiab aldosterone nce, ua rau dej thiab sodium tuav thiab nce ntshav ntim. Cov ntshav ntim ntau dhau yuav ua rau cov ntshav visceral nce ntxiv thiab ua rau cov ntshav siab ntxiv.
Octreotide inhibits qhov tso tawm ntawm renin, txo qhov tsim ntawm angiotensin II thiab aldosterone, txhawb dej thiab sodium excretion, thiab txo cov ntshav ntim (uas tuaj yeem txo cov ntshav ntim los ntawm 10% -15%), yog li txo qis cov ntshav visceral, txo cov ntshav ntws ntawm cov hlab ntsha portal, thiab txo cov ntshav siab.
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