Opiorphin ntsiav tshuajyog peptide tsim los ntawm peb cov amino acids uas muaj cov khoom tiv thaiv neuroprotective. Cov mis mos Molecular C29H48N12O8, CAS 864084-88-8, tuaj yeem tiv thaiv kev sib sau ntawm cov pa oxygen reactive (ROS) thiab inhibit qhov ua kom ERK 1/2. Nws tuaj yeem txhawb kev ua haujlwm ntawm lub ntsiab cellular Cheebtsam ntawm lub hlwb cov ntaub so ntswg thiab txo cov cell tuag. Tiv thaiv cov me nyuam ntawm nas los ntawm prenatal hyperhomocysteineemia. Cov ntsiab lus no yog rau kev tshawb fawb txog kev tshawb fawb nkaus xwb. Tsis txhob siv ncaj qha rau tib neeg lub cev!
Cov khoom tsim
Opiorphin COA
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| Certificate of Analysis | ||
| Compound npe | Opiorphin | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 864084-88-8 | |
| Ntau | 60g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090088 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.98% |
| Ib leeg impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500ppm ua |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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| Chemical Formula: | C29H48N12O8 |
| Exact Mass: | 692 |
| Molecular Luj: | 693 |
| m/z: | 692 (100.0%), 693 (31.4%), 694 (4.7%), 693 (4.4%), 694 (1.6%), 694 (1.4%) |
| Elemental Analysis: | C, 50.28; H, 6.98; N, 24.26; O, 18.48 |
Opiorphin ntsiav tshuajyog ib qho tshuaj peptide nrog cov tshuaj muaj zog analgesic thawj zaug pom hauv tib neeg cov qaub ncaug, thiab nws cov qauv tshuaj lom neeg tshwj xeeb thiab cov txheej txheem ntawm kev ua tau coj kev cia siab tshiab rau kev tswj kev mob.
Inhibition ntawm enkephalin degrading enzyme
1. Kev ua haujlwm thiab degradation ntawm enkephalin
Enkephalin yog ib qho endogenous opioid peptide uas tuaj yeem khi rau opioid receptors hauv lub cev thiab tsim cov teebmeem analgesic. Txawm li cas los xij, nyob rau hauv ib txwm muaj, enkephalins yog degraded sai heev los ntawm ob enkephalin degrading enzymes - human neutral endopeptidase (hNEP, enzyme code EC 3.4.24.11) thiab human exogenous aminopeptidase (hAP-N, enzyme code 1 EC 3.2), 1. Cov txheej txheem degradation no txwv tsis pub muaj cov nyhuv analgesic ntawm enkephalin hauv lub cev.
2. Inhibition nyhuv
Raws li lub zog inhibitor ntawm tib neeg enkephalin inactivating zinc heteropeptidase, nws tuaj yeem khi rau hNEP thiab hAP-N, inhibiting lawv degradation ntawm enkephalin. Tshwj xeeb, los ntawm kev tuav cov chaw nquag ntawm cov enzymes no, lawv raug tiv thaiv los ntawm kev khi rau enkephalin, yog li tiv thaiv enkephalin los ntawm degradation. Cov txheej txheem no tswj hwm qhov siab ntawm enkephalin nyob rau hauv lub cev, tsis tu ncua activating endogenous opioid nyob ntawm kev sib kis thiab thaum kawg tsim cov teebmeem analgesic.
3. Cov ntaub ntawv pov thawj
Ntau qhov kev sim hauv vitro tau lees paub qhov inhibitory nyhuv ntawm Opiorphin ntawm hNEP thiab hAP-N. Piv txwv li, hauv ex vivo colon thwmsim hauv nas, Opiorphin (1-100 μ M) tuaj yeem ua rau lub plab hnyuv loj hauv cov nas nyob rau hauv ib qho kev sib koom ua ke thiab txhim kho qhov kev cog lus teb los ntawm methionine enkephalin. Qhov no qhia tau hais tias nws muaj peev xwm tiv thaiv enkephalin los ntawm degradation, yog li txhim kho nws physiological muaj nuj nqi. Tsis tas li ntawd, inhibition ntawm enzymatic hydrolysis ntawm recombinant hNEP ntawm lub xovtooj ntawm tes hauv Mca-BK2 ua rau IC50 tus nqi ntawm 33 μ M, thiab inhibition ntawm Ala pNA cleavage ntawm hAP-N ua rau IC50 tus nqi ntawm 65 μ M, ntxiv rau nws cov inhibitory nyhuv ntawm ob.
Cov ntaub ntawv qhov chaw: Sohu, CSDN Blog, Chemical Instrument Network
Ua kom endogenous opioid nyob ntawm kev sib kis
1. Ua kom cov kab mob endogenous opioid
Los ntawm inhibiting enkephalin degrading enzymes, endogenous enkephalins muaj kev tiv thaiv los ntawm degradation, yog li activating endogenous opioid nyob ntawm kev sib kis. Lub endogenous opioid system suav nrog endogenous opioid peptides xws li enkephalin thiab dynorphin, nrog rau opioid receptors xws li μ, δ, thiab κ. Nws tsis ncaj qha ua rau opioid receptors, tab sis tsis ncaj qha activates opioid receptors los ntawm kev ua kom cov concentration ntawm enkephalin, ua rau analgesic teebmeem.
2. Kev sim tshuaj xyuas cov nyhuv analgesic
Tsiaj thwmsim tau pom cov teebmeem analgesic tseem ceeb. Hauv kev sim nas, txhaj tshuaj sib txawv ntawm Opiorphin (1.25-10 μ g / kg) rau hauv cov hlab ntsha tuaj yeem ua rau muaj zog ua kom muaj zog hauv koob - thiab nyob ntawm lub sijhawm.
Ntawm 10 feeb tom qab txhaj tshuaj, muaj qhov hloov pauv loj hauv feem pua ntawm tail flick latency (TWL) hauv ntau pawg, nrog 28.90% hauv 1.25 mg / kg pawg thiab siab li 91.89% hauv 10 mg / kg pawg. Qhov no qhia tiasopiorphin ntsiav tshuajmuaj peev xwm zoo rau kev kho mob.
3. Kev sib piv nrog cov tshuaj opioid ib txwm muaj
Piv nrog rau cov tshuaj opioid ib txwm siv xws li morphine, nws muaj kev pheej hmoo tsawg dua thiab kev zam. Qhov no yog vim hais tias nws ua rau cov teebmeem analgesic los ntawm kev tiv thaiv endogenous enkephalins, es tsis ncaj qha activating opioid receptors. Yog li ntawd, nws txo qhov muaj feem ntawm kev quav tshuaj thiab kev vam khom, muab cov kev xaiv tshiab rau kev tswj qhov mob.
Cov ntaub ntawv xov xwm: Sohu, Baijiahao, Chemical Instrument Network
Regulating nyhuv ntawm cov hlab plawv system
1. Kev soj ntsuam kev soj ntsuam ntawm cov hlab plawv
Ntxiv nrog rau nws cov nyhuv analgesic, nws kuj muaj qee yam cuam tshuam rau cov hlab plawv. Cov kev sim tau pom tias kev txhaj tshuaj hauv cov hlab ntsha tuaj yeem txhaj tshuaj raws li qhov ua rau muaj qhov nce siab ntawm cov hlab ntsha thiab lub plawv dhia hauv Uratan tshuaj loog nas. Cov lus teb ntawm cov hlab plawv no tuaj yeem cuam tshuam nrog kev tswj hwm ntawm endogenous circulating angiotensin qib, nyob rau hauv uas lub paj hlwb koom nrog.
3. Cov kab mob opioid tsis cuam tshuam nrog kev mob plawv
Nws yog ib nqi sau cia hais tias lub opioid system tsis koom nyob rau hauv lub plawv teb tshwm sim. Qhov kev sim pom tau hais tias qhov tsis xaiv opioid receptor antagonist naloxone tsis muaj qhov cuam tshuam loj rau cov kab mob plawv tshwm sim. Qhov no qhia tau hais tias lub mechanism ntawm kev txiav txim nyob rau hauv lub plawv system yog txawv los ntawm nws cov nyhuv analgesic.
2. Kev tshawb nrhiav cov txheej txheem ntawm cov hlab plawv
Cov kev tshawb fawb ntxiv tau pom tias cov tshuaj tiv thaiv kab mob plawv tuaj yeem ua rau muaj kev cuam tshuam loj heev los ntawm angiotensin -hloov enzyme inhibitor Captopril thiab angiotensin II hom 1 receptor antagonist Valsartan. Qhov no qhia tau hais tias renin-angiotensin system (RAS) cuam tshuam rau cov hlab plawv ntawm cov khoom no. Tsis tas li ntawd, intravenous pre txhaj ntawm alpha adrenergic receptor antagonist phentolamine thiab beta adrenergic receptor antagonist propranolol kuj tuaj yeem cuam tshuam qhov nce siab ntawm cov hlab ntsha siab los ntawm lawv. Txawm li cas los xij, propranolol tuaj yeem cuam tshuam qhov tachycardia teb nws ua, thaum phentolamamine tsis tuaj yeem. Qhov no qhia tau hais tias nws cov teebmeem ntawm cov hlab plawv tuaj yeem cuam tshuam nrog ntau lub tswv yim, suav nrog kev ua kom RAS thiab kev tswj hwm ntawm lub paj hlwb sympathetic.
Cov ntaub ntawv qhov chaw: Docin.com Douding.com, tsis muaj (sab saum toj 30 cov ntaub ntawv muaj feem xyuam hauv Suav Teb Phau Ntawv Teev Npe Tag Nrho Cov Ntaub Ntawv)
Antidepressant nyhuv
1.Kev tshawb pom ntawm cov tshuaj tiv thaiv kev nyuaj siab
Ntxiv nrog rau nws cov tshuaj analgesic thiab kab mob plawv, nws kuj muaj cov tshuaj tiv thaiv kev nyuaj siab. Hauv kev sim ua luam dej ntawm cov nas, kev txhaj tshuaj Opiorphin (50, 100, 200, thiab 300 μ g / kg) rau hauv cov tshuaj ventricle lateral dependently shortened lub sij hawm immobility ntawm nas, qhia tias Opiorphin muaj antidepressant zog.
3. cuam tshuam rau kev ua haujlwm ywj pheej
Txhawm rau tshem tawm qhov ua tau tias nws cov tshuaj tiv thaiv kev ntxhov siab hauv kev sim ua luam dej yog tshwm sim los ntawm cov hlab ntsha excitation, qhov kev sim kuj tau tshuaj xyuas nws cov kev cuam tshuam rau kev ua haujlwm ntawm cov nas. Cov txiaj ntsig tau pom tias tsis muaj kev cuam tshuam rau kev ua haujlwm ywj pheej ntawm cov nas uas tsis hloov pauv ua ntej, tab sis me ntsis txhim kho kev muaj peev xwm ua haujlwm ntawm cov nas uas yoog ua ntej. Qhov no qhia tau hais tias nws cov nyhuv antidepressant tsis ua tiav los ntawm cov hlab ntsha excitatory.
2. Kev tshawb fawb ntawm cov txheej txheem ntawm cov nyhuv antidepressant
Cov kev tshawb fawb ntxiv qhia tias nws cov nyhuv antidepressant yog kho los ntawm txoj kev opioid ntawm enkephalin. Cov uas tsis yog xaiv opioid receptor antagonist naloxone, thaum siv ua ke, tuaj yeem cuam tshuam tag nrho cov tshuaj tiv thaiv kev ntxhov siab ntawm cov tshuaj no. Muab hais tias enkephalin muaj ob lub receptors, μ - thiab δ -, kev sim ntxiv yuav siv μ - thiab δ - opioid receptor selective antagonists - DNA thiab naltrindole ua ke los tshawb xyuas cov receptor tshwj xeeb. Cov txiaj ntsig tau pom tias δ receptor antagonist naltrindle tuaj yeem cuam tshuam tag nrho nws cov tshuaj tiv thaiv kev ntxhov siab, thaum lub μ receptor antagonist - RNA ib nrab inhibited cov nyhuv no. Qhov no qhia tau hais tias nws ua rau kom cov extracellular concentration ntawm enkephalin los ntawm inhibiting nws degradation, indirectly activating μ thiab δ opioid receptors rau exert antidepressant los.
Cov ntaub ntawv qhov chaw: Wanfang Cov Ntaub Ntawv Kev Paub Txog Kev Pabcuam Platform, tsis muaj (sab saum toj 30 cov ntaub ntawv cuam tshuam hauv Suav Teb Phau Ntawv Teev Npe Tag Nrho Cov Ntaub Ntawv)
Lwm yam teebmeem
1. Kev cuam tshuam rau kev mob plab hnyuv
Ntxiv nrog rau cov teebmeem saum toj no, nws kuj tau pom qhov chaw hauv kev tshawb fawb txog kev mob plab. Kev tshawb fawb tau pom tias nws tuaj yeem txhim kho txoj hnyuv teb rau methionine enkephalin, uas tuaj yeem muab txoj hauv kev tshiab rau kev kho mob los ntawm cov kab mob xws li mob plab plob tsis so tswj. Nyob rau hauv ex vivo colon sim ntawm nas,opiorphin ntsiav tshuaj(1-100 μ M) tuaj yeem ua rau mob plab hnyuv loj hauv cov nas nyob rau hauv ib qho kev sib koom ua ke thiab txhim kho cov lus teb cuam tshuam los ntawm methionine enkephalin.
2. cuam tshuam rau lub cev tiv thaiv kab mob
Txawm hais tias tam sim no tsis muaj kev tshawb fawb txog kev cuam tshuam rau lub cev tiv thaiv kab mob, lwm yam khoom hauv cov qaub ncaug xws li lysozyme thiab mucin muaj peev xwm ntxuav qhov txhab thiab tiv thaiv kab mob. Qhov no qhia tau hais tias cov khoom hauv cov qaub ncaug ua lub luag haujlwm tseem ceeb hauv kev tiv thaiv kab mob. Cov kev tshawb fawb yav tom ntej tuaj yeem tshawb nrhiav ntxiv seb nws puas tseem koom nrog hauv cov txheej txheem tiv thaiv kab mob.
Cov ntaub ntawv qhov chaw: Sohu, Weibo
FAQ
Puas yog opiorphin muaj zog dua morphine?
Hauv kev koom tes nrog pab pawg ETAP los ntawm Nancy-Brabois Technopole, Institut Pasteur cov kws tshawb fawb tau pom nyob rau hauv vivo tias, rau tib koob tshuaj, Opiorphin tsim cov tshuaj muaj zog sib piv xws li morphine, hauv ob qho tib si thermal thiab mechanical mob mob thiab hauv tshuaj lom neeg{1}.
Koj puas tuaj yeem rho tawm opiorphin los ntawm qaub ncaug?
HFBA-raws li SUPRAS yog, yog li ntawd, muaj peev xwm ua tau zoo tshem tawm opiorphin los ntawm cov qaub ncaug cov qauv thiab qhia tau hais tias muaj peev xwm loj rau kev txiav txim siab ntawm ntau cov amino acids thiab oligopeptides los ntawm cov qauv lom neeg.
Dab tsi yog qhov tshuaj tua neeg muaj zog tshaj plaws?
Nws yog qhov muaj zog tshaj opioid muaj nyob rau hauv cov chaw kho mob, ua 50 mus rau 100 lub sij hawm ntau zog tshaj morphine. Carfentanyl, ib qho fentanyl analog yog suav tias yog qhov muaj zog tshaj plaws opioid, kwv yees li 10,000 npaug zog dua morphine. Vim nws qhov muaj zog heev, carfentanil tsis tshua siv rau tib neeg kev kho mob.
Cim npe nrov: Tuam Tshoj opiorphin ntsiav tshuaj manufacturers, lwm tus neeg
