Notropic Fonturacetam Hydazide, CAS 77472-71-0, cov qauv molecular yog c12h15n3o2, tus qauv qib dawb, tsis muaj txiaj ntsig lossis tsis muaj ntxhiab tsw me ntsis. Nws yog hom hydrazide derivative ua kom zoo raws li cov qauv ntawm kev ua kom muaj txiaj ntsig, kev ua haujlwm zoo rau kev txhim kho thiab kev kho kom muaj zog thiab kev txhim kho roj ntsha. Nce cov ntshav hauv Ischamic. Txhim kho lub zog ntawm cov nqaij mos yog ua tiav los ntawm kev txhim kho kev siv cov piam thaj. Nws muaj cov nyhuv diuretic me me. Ua kom muaj kev sib haum xeeb ntawm neurotransmitters (serotonin, norsepinephrine, thiab dopamine) nyob rau hauv lub hlwb ntawm gaba-b receptors thiab gaba-ib tug receptors thiab gaba-ib tug receptors.
Notropic Fonturacetam Hydrazide +. coa
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Daim Ntawv Pov Thawj Kev Ntsuam Xyuas |
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Compound npe |
Notropic Fonturacetam Hydazide | |
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Cas Tsis tau. |
77472-71-0 | |
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Teem nqi |
Kws Tshuaj Ntsuam Xyuas | |
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Qho ntau |
Me nyuam | |
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Ntim txheem ntim |
Me nyuam | |
| Tus tsim | Shaanxi Bloom Tech Co., Ltd. | |
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Lauj tsis tau. |
20250109001 |
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Mfg |
Jan 12th 2025 |
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Tus txeeb |
Jan 8th 2029 |
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Lub tsev |
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| Kuaj Tus Qauv | GB / T24768-2009 kev lag luam. Stnndard | |
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Yam |
Kev Lag Luam Kev Lag Luam |
Kev tsom xam tau |
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Kev tshwm sim |
Dawb lossis yuav luag dawb hmoov |
Hloov |
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Dej Cov Ntsiab Lus |
Tsawg dua los yog sib npaug rau 4.5% |
0.30% |
| Poob rau ziab |
Tsawg dua los yog sib npaug rau 1.0% |
0.15% |
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Cov hlau hnyav |
PB tsawg dua lossis sib npaug rau 0.5ppm |
N.D. |
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Tsawg tsawg dua li lossis sib npaug rau 0.5ppm |
N.D. | |
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Hg tsawg dua lossis sib npaug rau 0.5ppm |
N.D. | |
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CD tsawg dua lossis sib npaug rau 0.5ppm |
N.D. | |
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Purity (hplc) |
Ntau dua los yog sib npaug rau 99.0% |
99.5% |
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Ib Leeg Cav |
<0.8% |
0.48% |
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Residue ntawm ignition |
<0.20% |
0.064% |
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TAG NRHO LICBIAL COUNT |
Tsawg dua li lossis sib npaug rau 750cfu / g |
80 |
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E. coli |
Tsawg dua los yog sib npaug rau 2mpn / g |
N.D. |
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Tus ntses siav |
N.D. | N.D. |
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Ethanol (los ntawm gc) |
Tsawg dua los yog sib npaug rau 5000ppm |
400ppm |
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Chaw ntim khoom |
Khaws rau hauv ib qho chaw sib khi, qhov chaw tsaus thiab qhuav ntawm-20 degrees |
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Notropic Fonturacetam Hydazide(CAS naj npawb: 77472-71-0) yog hydrazide derivative ntawm phenylpiretam. Los ntawm kev qhia txog cov pab pawg hydrazide rau cov pab pawg hydrazide rau hauv cov phenycacetam molecule, nws cov bioavailabus, thiab lub hlwb lub hlwb nkag siab tau zoo dua. Raws li cov kev txawj ntse ua tau zoo tshaj
1.1 Kev Kho Mob ntawm Cov Kab Mob Nurodegenerative
PhenyLatpatyd tau qhia tias tseem ceeb ua tau zoo nyob rau hauv kev kho mob ntawm neurodegenerative cov kab mob xws li Alzheimer tus kab mob thiab txoj kab kev ua si avasement. Nws cov tub ntxhais tshuab suav nrog:
Kev cai dopaminergic system: txhim kho ua haujlwm nco txog kev ua haujlwm los ntawm kev txhawb nqa DOPAMUL D1 cov lus qhia tawm hauv lub antept cortex. Piv txwv li, ib qho kev tswj hwm kev sib tham ntawm 60 lub lim tiam ntawm kev kho mob Alzheimer tau nthuav tawm ntau ntxiv los ntawm 2.3 cov ntsiab lus (tswj pab pawg tau nce los ntawm 0.8 cov ntsiab lus, p<0.05), and no dependence or withdrawal reactions were observed.
Acetylcholine Synthesis tshaj tawm: Ua kom muaj Choline acetylfTorase (sib tham) nce Hippocphal Acetylcholline li 25% thiab cuam tshuam txog kev nthuav dav spatial mement.
Cov kev sim tsiaj tau pom tias nws cov kev tsis nco qab txog kev ua haujlwm nce hauv kev txhaj tshuaj-ofourt ntau ntawm 6-750 mg / kg.
Kev tiv thaiv kab mob antioxidant: Muaj peev xwm tshem tawm dawb radicals yog nce los ntawm cov qauv tshuaj lom neeg poptoptosis (muaj sia nyob ntawm 60% txog 85%).
1.2 Kho cov mob hlwb
Nyob rau hauv lub hom phiaj xwm pathological xws li mob stroke thiab kev mob siab rau lub hlwb raug mob, Pheetry ua haujlwm rov qab los ntawm cov txheej txheem hauv qab no:
Txhim kho cov ntshav hauv qab ntsim: nce cov ntshav hauv zos nce hauv Ischamic hauv thaj chaw, rov ua cov lus thiab kev ua haujlwm tsis sib haum xeeb. Piv txwv li, hauv Simrulated Cerebral yogchemia qauv, nce qib 15% nce hauv kev caij ntshav ntws nrawm tuaj yeem pom hauv 30 feeb tom qab kev tswj hwm.
Kev ua kom muaj zog ntawm lub zog metabolism: txhawb nqa ATP ntau lawm hauv lub hlwb thiab txhim kho cov dej qab zib kom siv tau. Cov ntaub ntawv kuaj mob qhia tau tias tom qab kev kho mob tom qab kev kho mob, lub hlwb looj roj ntau rau cov neeg mob nce ntxiv los ntawm kev txhim kho kev ua haujlwm ntawm cov qhabncharation.
Neuroprotreective synergy: thaum siv hauv kev sib xyaw ua ke rau kev kho mob ntawm Alzheimer tus cwj pwm los ntawm 35%, ua rau muaj ntau hom phiaj synergistic nyhuv.
1.3 Kev ua raws li cov neeg noj qab nyob zoo
Daim ntawv thov ntawm phenylpatpatiMacetam Hydazine hauv cov tib neeg noj qab nyob zoo tau tsim lub hom phiaj txheej txheem:
Cov pab pawg tub ntxhais kawm: Rau kev siv cov xwm txheej siab, kev pom zoo ntau npaum li cas yog 100-200 mg / hnub, muab faib ua ob koob tshuaj. Cov kev sim kuaj mob tau pom tias tom qab siv 10 hnub tom qab kev siv tas mus li,
Chaw Haujlwm Pabcuam Haujlwm: Hauv kev ua haujlwm siab ua haujlwm ib puag ncig, ib qho ntawm cov kab ntawm 100-6 teev thiab nce txoj kev vam meej ntawm kev ua tiav tiav los ntawm 30%. Piv txwv li, tom qab chernobyl nuclear fais fab cog kev ua haujlwm tu tu cov neeg ua haujlwm noj, cov tsos mob txo ntawm neurasthenia cov tsos mob tau mus txog 72%.
Cov neeg laus neeg: Rau cov laj thawj laus, siv koob tshuaj 200 mg / hnub rau 12 lub lis piam tuaj yeem txhim kho lub cim xeeb kev sib xyaw muaj peev xwm nce txog 18%).
2.1 Zog metabolism kho kom zoo
Notropic Fonturacetam HydazideTxhim kho kev ua kom muaj kev ua siab ntev los ntawm txoj hauv kev hauv qab no:
Txhim kho Mitochondrial muaj nuj nqi: nce mitochondrial atptses tus nqi los ntawm 15% hauv cov leeg hlwb, thiab ntev ua luam dej mus txog 30% hauv nas.
Lactic acid metabolism cov kev cai: inhibits lactate accitulation, txo cov ntshav lactate ntau los ntawm 22% tom qab tawm dag zog, thiab qeeb qhov tshwm sim ntawm kev qaug zog. Piv txwv li, hauv kev simulated siab ib puag ncig (5000 meters) sim, qhov siab tshaj plaws oxygen uptake (vo ₂ max) ntawm cov kev kawm nce los ntawm 12%.
2.2 Kev yoog rau ib puag ncig heev
Rau cov xwm txheej tshwj xeeb xws li cov kev ua haujlwm tshawb fawb ncov qaum ntuj thiab cov kev ua haujlwm siab, PhenylPiretam hydazine cov khoom pov thawj tshwj xeeb:
Kev txhim kho ntawm cov khaub thuas tsis kam: los ntawm kev txhim kho kev ua haujlwm ntawm hypothalamic punitary Axis, lub cev muaj peev xwm tswj hwm tus tub ntxhais kawm qib siab tau nce 20%.
Kev xav txog kev xav txog kev xav: hauv kev sim siab heev kev ntxhov siab, lub siab ruaj khov rau cov neeg siv tau nce 35% thiab qhov kev txiav txim siab yuam kev tsawg ntawm 28%.
2.3 Kev Kho Mob Ua Si
Cov kws sim tsiaj tau qhia tias phenycacetam hydazine tuaj yeem nrawm rov qab raug mob rau kev ntaus pob ncaws pob:
Inhibition ntawm mob teb chaws
Collagen synthesis kev tshaj tawm: nce qib lus
3.1 antioxidant wurense system
PhenylpatiG Hydazine unceviates oxidative kev puas tsuaj los ntawm cov txheej txheem hauv qab no:
Dawb radical lom zem: ncaj qha tawm tsam cov pa oxygen, Ros) radicals, nce neuronal desournival tus nqi los ntawm 60% nyob rau hauv h ₂ o ₂ - tus qauv ua qauv.
Antioxidant enzyme ua kom lub zog: Upregulation ntawm enzyme cov haujlwm xws li Sold thiab GSH PX ua rau ib qib MDA tsawg hauv cov ntaub so ntswg.
3.2 Kev Txaus Siab Toxicity Inhibition
Nyob rau hauv lub glutamate induced neuronal kev puas qauv, phenypatpatiMacetam hydazine tsom cov teebmeem tseem ceeb:
NMDA Receptor Cov Kev Cai: Los ntawm Inhibiting CA ² ⁺ Inflex, cov qib ntawm cov calcium hluav taws xob hauv calcium overload yog txo los ntawm 50%.
Mitochondrial Mitochondrial Membrane nyob rau hauv ib txwm muaj, txo cytochrome c tso tawm, thiab inhibiting shecade ntawm apoptosis regionals.
3.3 Nenogenesis kev tshaj tawm
Cov kev sim tsiaj tau pom tias kev siv ntev ntawm phenylpatpatiMetam Hydazine tuaj yeem nce Hippocampal Neurogenesis:
Uprovulation ntawm BDNF kev qhia: Ntau dua BDNF MRNA theem hauv cov hniav Gyrus ntawm 40% thiab txhawb nqa cov khoom muaj cai ntawm cov neural prefursor hlwb.
Txhim kho cov khoom siv synaptic: nce dendritic spine ceev los ntawm 25% thiab txhim kho lub potentiation ntev (LTP) teebmeem.
4.1 Txij Nkawm Ntawm Kev Ua Haujlwm
Hauv kev simulated microgegravity ib puag ncig ntawm qhov chaw, phenympatam hydazine tuaj yeem:
Kev Txhim Kho Cov Kev Qhia Txog Kev Ncaj Ncees: Txo qhov ua yuam kev ntawm cov kev kawm "peb-seem spatial rotation xeem los ntawm 30%.
Kev nthuav dav ntawm kev ua haujlwm nco muaj peev xwm: los ntawm FMRI nrhiav tau, nws tau pom tias thaj chaw qhib ntawm lub tshuab ua ntej cortex nce los ntawm 20%.
4.2 physiological kev ntxhov siab tsis kam
Rau qhov chaw hnyav xws li kub thiab siab noo, nws cov haujlwm muaj xws li:
Kev ntsuas ntsuas kub ua haujlwm: nce hws evaporation efficiency los ntawm 15% nyob rau hauv 35℃ib puag ncig, tswj ruaj khov lub cev kub.
Tswj cov dej ntsev tshuav nyiaj: los ntawm kev tswj hwm Adh zais cia, hloov pauv ntau ntawm cov zis tso zis yog txo los ntawm 40%.
4.3 Kev Xav Txog Kev Ntsiag Ntshaw
Hauv kev kawm ua tub rog, PhenylpatpatiMacetam Hydazine tau pom cov teebmeem tseem ceeb:
Txhim kho kev xav ruaj khov: Txo qhov kev ntsuas tus kheej kev ntxhov siab (SAS) tau txog 25%.
Kev txiav txim siab nrawm-kev txiav txim siab nrawm: hauv txoj haujlwm ua haujlwm nyuaj, lub sijhawm tiv thaiv tau luv los ntawm 0.3 vib nas this (P<0.01).
5.1 Neuroscience Cov Cuab Yeej
Notropic Fonturacetam Hydazide, raws li dopamine system sojntsuam, yog siv dav rau:
Receptor binding assay: Its D1 receptor affinity (Ki=12 nM) makes it an important tool for studying reward circuits.
Cov Qauv Tsiaj Qauv: Hauv kev ntsuam xyuas xws li Morris tus neeg tau lees paub, cov txiaj ntsig tshiab txog kev ua tau zoo raws li cov tshuaj uas tswj tau zoo.
5.2 Kev txhim kho cov kws tshuaj nruab nrab
Raws li derivative ntawm phenymacetam, nws pab pawg hydrazide muab cov chaw ua haujlwm kom muaj kev hloov kho dua tshiab:
Protrug Tsim: Lub hom phiaj xa tawm tuaj yeem tsim tau los ntawm Esterification lossis kev coj noj coj ua los txhim kho cov ntaub so ntswg hluav taws xob.
Kev tsim kho ntawm Combinatorial Chemstore Chemston, raws li cov tub ntxhais lub cev pob txha, dhau 50 tus txiv neej tau muab ua ke, ntawm 3 tau nkag mus rau qhov kev tshawb fawb preclinical theem.
5.3 Kev Siv Hluav Taws Xob Muaj
Hauv kev thaj teb cov organic synthesis, Phenycacetam Hydazine cov khoom pov thawj tshwj xeeb cov kev cuam tshuam:
Asymmetric catalysis: raws li ib chairal ligand, nws nce qhov enantioselectivity mus rau 95% ee hauv palladium catalling kev tawm tsam.
Polymer Khoom Hloov Kho: nws cov pab pawg hydrazide tuaj yeem hnov nrog polyurethane Prepolymers los npaj cov kev hnav khaub ncaws zoo nrog biocompatibility zoo heev.
Muaj cov txheej txheem hluav taws xob thiab txoj kev ua kom zoo
Tsoos ib txwm-qib synthesis txoj kev
Txheej txheem thev naus laus zis:
Alkylation Reaction:
Pib ntawm 4-phenyl-2-pyrrolidone, nws reacts nrog Ethyl Bromoacetate nyob rau hauv anhydrodrolidine-1-acetic acid Ether);
Cov tsis tseem ceeb:
Cov tshuaj tiv thaiv kub -20 degree, lub sijhawm tiv thaiv lub sijhawm 8 teev, sodium hydride (nah) raws li puag, kev tiv thaiv nitrogen;
Hydrolysis thiab Decarboxylation:
Nruab nrab a yog hydrolyzed hauv sodium hydroxide tov thiab ces rhuab mus rau qhov nruab nrab b (2-oxo-4-phenylprodrolidine-1-acetic acid);
HYZAZINYURATIONSE:
Nruab nrab b thiab hydrazine hydrate tau refluxed nyob rau hauv ethanol rau 6 teev, thiab tom qab ntawd recrystallized kom tau txais phenylpirine.
Technical bottleneck:
Sodium hydride reacts ua nruj ua tsiv nrog dej, xav tau nruj ua haujlwm tsis muaj nqis, uas nce ntau lawm cov nqi;
Cov tshuaj tiv thaiv tag nrho ntawm ntau kauj ruam cov tshuaj tiv thaiv tsuas yog 45% -50 -50 -50 -50-50%, thiab cov kua khib nyiab yog tsim ib phaus ntawm cov khoom).
Ntsuab catalytic synthesis txoj kev (cov txheej txheem tshiab)
Txhim Kho Cov Txheej Txheem:
Alkylation hloov: poov tshuaj
Ib lub lauj kaub hydrolysis hydrazide kev tawm tsam: hydriav teb ib qho yog hydrolyzed thiab ncaj qha ntxiv rau lub npib tsib xee chlooride (sodium borohydride (nicl ₂ / nabh ₄) txo cov txheej txheem. Cov tshuaj tiv thaiv yog nqa tawm ntawm 60℃hauv ethanol rau 4 teev kom tiav decarboxylation thiab hydrazide cov tshuaj tiv thaiv nyob rau hauv ib kauj ruam, nrog rau tag nrho cov txiaj ntsig ntawm 75%.
Pharmacical mechanism ntawm kev ua thiab chaw kuaj mob zoo
1. Kev ua kom haum kev txhim kho mechanism
Kev tswj hwm dopaminergic system: los ntawm kev hais tawm ntawm Dopamine D1 receptors hauv qhov prefronte cortex, nrog 40% txo qis hauv cov qauv sib xws);
Acetylcholine synthesis kev tshaj tawm: Ua kom muaj ChopporTylTs (sib tham), nce happocampal acetylcholine qib li 25%, thiab txhim kho kev muaj peev xwm spatial mementic;
Kev tiv thaiv kab mob antioxidant: Muaj peev xwm tshem tawm dawb radicals yog 1.8 zaug txo qis Apoptosis (kev muaj sia nyob ntawm 60% mus rau 85%).
2. Kev ua haujlwm txhim kho hauv kev ua kis las
Lub zog metabolism optimization: nce leeg leeg mitochondrial atp li cas los ntawm 15%, txuas ntxiv mus ua luam dej ntev ntev los ntawm 30%;
Anti Latasge nyhuv: Los ntawm inhibiting lactate kev vam meej, theem ntshav lactate qib txo qis dua li ntawm 22% tom qab qoj ib ce, ncua qhov tshwm sim ntawm kev qaug zog.
3. Kev nyab xeeb thiab thev taus
Toxicological data: LD ₅₀ (oral administration to rats)>5000 mg / kg, cais raws li kev coj ua tsis muaj kuab lom;
Cov kev mob kho mob tshwm sim: muaj qee kis tau qhia me ntsis insomnia (qhov xwm txheej<2%) and gastrointestinal discomfort (incidence<1%), with no dependence or withdrawal reactions.
Notropic Fonturacetam Hydazide, raws li ib tiam tshiab ntawm kev nkag siab, yog ua rau muaj kev tshawb fawb boom thoob ntiaj teb vim nws cov qauv tshuaj tshwj xeeb, thiab kev nyab xeeb ntau. Nrog rau cov neeg muaj kev pom zoo ntawm cov khoom siv ntsuab ntawm cov ntaub ntawv pov thawj hauv chaw kuaj mob, kev txhim kho kev ua kom muaj kev ua haujlwm, thiab tawm tsam kev laus.
Cim npe nrov: Notropic Fonturacetam Hydrazide, cov chaw muag khoom, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqi, loj, rau muag