Carbetocin CAS 37025-55-1

Carbetocinyog dawb rau beige hmoov nrog lub zog zoo heev. Cov mis molecular c45h69n11o12s, cas 37025-55-1. Nws muaj qee qhov solubility hauv DMO (me me) thiab methanol (ib qho me me), thiab yog soluble nyob rau qee cov kuab tshuaj. Lub ISOELECTRIC PARCH yog li 9.5, qhia tias nws nqa tau tus nqi zoo nyob hauv ib puag ncig nrog ib puag ncig nrog ib puag ncig nrog cov pH hauv qab no 9.5. Nws yog peptide tshuaj nrog cov qauv tshuaj nyuaj thiab belongs rau qeb ntawm biochemistry. Nws muaj ntau cov siv hauv Chemistry, koom nrog nws cov ntawv thov hauv cov synthesis ntawm cov oxytocin analogues, kev tsim tshuaj, thiab kev tsim yeeb. Txawm li cas los xij, hauv cov ntawv thov kev siv, cov lus qhia kev nyab xeeb thiab cov txheej txheem kev ua haujlwm tseem ceeb tseem yuav tsum tau ua raws li kev nyab xeeb thiab ua haujlwm ntawm kev sim. Nyob rau yav tom ntej, nrog qhov tob ntawm kev tshawb fawb thiab kev txhim kho thev naus laus zis, daim ntawv thov hauv Chemistry yuav nthuav ntxiv ntxiv nthuav ntxiv.

Carbetocinyog cov khoom siv hluavtaws ntev-ua rau oxytocin {{1} peptide analogue nrog agonist cov yam ntxwv zoo ib yam li cov oxytocin zoo ib yam. Lub ntsiab siv suav nrog kev tiv thaiv thiab kev kho mob tom qab yug menyuam, thiab kev thov hauv kev tshawb fawb thiab kev lag luam muaj kev lag luam tshwj xeeb.

1. Ua ntej, nws lub hom phiaj tseem tiv thaiv thiab kho cov hemorrhatum. Tom qab hemorrhage yog ib qho kev ua piv txwv tsis zoo uas tuaj yeem ua rau muaj mob loj thiab tuag taus. Los ntawm kev txhawb nqa uterine kev cog lus thiab nce uterine nro, xa cov hemorrhage tuaj yeem tswj tau zoo. Kev tshawb fawb tau pom tias ib qho koob tshuajcarbetocin100 yog muab tshuaj tiv thaiv tau sai li sai tau tom qab phais nyuj hauv qab epidural lossis txha caj qaum μ g. Nws tuaj yeem txo qis qhov tshwm sim ntawm kev ua haujlwm ntawm tus menyuam mos, tiv thaiv kev pheej hmoo ntawm Uterine nruj, thiab txo qhov kev pheej hmoo ntawm kev cuam tshuam ntsig txog.

2. Thib ob, nws kuj tseem pab txhawb txoj kev rov qab ntawm lub tsev menyuam. Nyob rau hauv thaum ntxov qib ntawm kev xa menyuam tom qab pib, kev tswj hwm tuaj yeem txhawb cov kev mob siab ntseej thiab txhawb nqa uterine rov qab. Qhov no pab kom txo cov kev tshwm sim ntawm kev kawm tom qab yug menyuam thiab txhim kho kev noj qab haus huv theem ntawm tus poj niam tom qab yug menyuam.

Ntxiv nrog rau nws daim ntawv thov hauv thaj chaw ntawm cov leeg, nws tseem muaj qee cov kev siv hauv lwm qhov chaw. Hauv kev tshawb fawb ntawm kev tshawb fawb, ua kev tshawb fawb, nws yog siv los tshawb txog lub cev muaj sia thiab chaw muag tshuaj ntawm cov khoos phis tawm Oxytocin, nrog rau kev txhim kho cov tswv yim kho tshiab. Tsis tas li ntawd, nws tseem muaj qee qhov kev thov muaj nuj nqis hauv qee cov teb tshwj xeeb. Piv txwv li, nws tuaj yeem siv rau hauv kev lag luam xim, cov khoom siv sib txuas lus, cov ntaub qhwv ntsej muag, cov ntaub qhwv, cov roj hmab, tshuab, thiab lwm daim teb.

3. Nws yog cov khoom siv hluavtaws ntev ntev oxytocin analogue nrog anti los ntshav thiab uterine evelical teebmeem. Nws cov qauv tshuaj yog zoo ib yam li tib neeg oxytocin, tab sis tau ua tiav rau kev txhim kho nws cov ruaj khov thiab kev ua tau zoo. Vim nws cov tshuaj tiv thaiv thiab cov neeg pab cog lus uterine, feem ntau nws siv los ua cov tshuaj lom neeg rau kev kawm cov roj pleev roj Oxytocin. Los ntawm kev khi rau Oxytocin cov khoom plig, nws tuaj yeem siv los tshawb txog cov chaw muag tshuaj thiab teeb liab Transduction txoj hauv kev ntawm Oxytocin receptors. Qhov no pab kom tau txais kev nkag siab tob txog lub luag haujlwm ntawm Oxytocin cov recitors hauv kev tswj cov kev cog lus uterine thiab tiv thaiv tus ncej tom qab.

4. Nws kuj tseem siv los tsim cov tshuaj tshiab lossis cov tswv yim kev kho mob. Raws li nws kev sib cuam tshuam nrog Oxytocin cov khoom plig, nws tuaj yeem ua cov tshuaj txhuas ua kom muaj kev ua haujlwm thiab kev xaiv los ntawm kev ua kom zoo dua thiab kev ua tshuaj ntsuam xyuas. Cov tshuaj no yuav siv tau los kho cov kab mob ntsig txog Oxytocin cov khoom plig, xws li tom qab yug menyuam yaus, Uterine atony, thiab lwm yam.

5. Hauv kev lag luam tsim khoom, nws tseem muaj qee yam tus nqi. Vim nws lub peev xwm los txhawb kev mob siab rau uterine, nws tuaj yeem siv los ua ke lwm cov tshuaj lossis cov khoom siv roj ntsha muaj feem cuam tshuam nrog cov kev cog lus uterine. Cov tshuaj lossis cov khoom lag luam no tuaj yeem siv los kho uterine cov kab mob uas muaj feem xyuam, xws li tom qab yug menyuam yaus, uterine fibroids, thiab lwm yam.

Ib txoj kev npaj rauCarbetocin, tus cwj pwm hauv uas nws muaj cov kauj ruam hauv qab no:

(1) Siv cov fmoc khoom-theem kev sibtsoo, Leu, thiab Tyr (R2), ASN (CHR2CH2CE2R1), ASN (CHR2CH2CH2R1) CYS (CH2CH2CH2CU2CO2R1) - PRO NEU GLY AMINO RESIN;

(2) Tshem cov pab pawg tiv thaiv FMOC

(3) Condensing Reside Resin tau txais hauv Kauj Ruam (2) kom tau txais cyclized carbetoxin peptide resin;

(4) tawg cov cyclized carboplatin peptide resin siv txiav cov tshuaj txiav, thiab terkipitating nws hauv etyl metyl ether kom tau txais carboplatin nyoos peptide;

(5) Siv cov npaj npaj npaj npaj cov tshuaj chromatography ua kua kom cais thiab ntxuav cov carbetoxin, khov-kom qhuav tau ua kom tau txais carbetoxin.

Hom qauv no cuam tshuam rau tom teb ntawm peptide synthesis, tshwj xeeb rau ib txoj kev rau npaj carbetoxin. Cov kauj ruam kev npaj muaj cov kauj ruam hauv qab no: Leu, Pro, Ch2ch2Ch2R1), ile (r2), ile (ch2ch), ile (ch2ch) Tshem cov pab pawg tiv thaiv FMOC tiv thaiv thiab R1, thiab condense lub peptide resin kom tau txais cyclized carbetoxin peptide resin; Kev tawg thiab nag lossis daus kom tau txais cov heev peptides; Cais thiab huv si lub ntsej muag nyoos pepudide, thiab khov qhuav nws. R1 pab pawg ntawm cov kev tsim muaj tam sim no tuaj yeem raug tshem tawm nyob rau hauv cov xwm txheej me me, kom tias peptide saw yuav tsis tshem tawm ntawm lub resin thaum tshem tawm ntawm R1. Tam sim no tsim muaj cov nplhaib ua kom tau ib lub nplhaib los ntawm kev tsim cov ntawv cog lus mus rau kuv Muaj txiaj ntsig zoo rau kev tsim khoom loj.

Carbetocin yog cov hluavtaws ntev-ua rau oxytocin analog feem ntau siv rau kev tiv thaiv thiab kho cov hemorrhatum (ppph). Raws li kev teeb tsa kev hloov kho ntawm Oxytocin, Carbetocin sib txuas ua ke cov kev ua haujlwm roj ntsha thiab ntev ib nrab ntawm Oxytocin, ua rau nws tseem ceeb hauv cov chaw kuaj mob. Oxytocin yog cuaj lub tshuaj tua hluav taws xob peptideized los ntawm hypothalamus thiab tso tawm los ntawm lub tom qab caj dab, uas txhawb nqa uterine zais cia. Thaum pib ntawm lub xyoo pua 20, Askiv Kws Kho Mob Henry Dale (1910) Thawj zaug tshaj tawm cov dej num pituitary, tso lub hauv paus extract ntawm Oxytocin. Xyoo 1953, pab neeg ntawm Asmeskas Biochemist Vincent du Vignages tau daws cov khoom siv Oxytocin (CYS tiav rau cov khoom siv Peptide thawj zaug los ua kev lom zem. Qhov kev tshawb fawb hauv ntiaj teb no tau txais Du Vigneasud lub Nobel khoom plig hauv 1955 thiab 1960, Oxytocin tau siv dav rau kev ncaj ncees. Txawm li cas los xij, nws lub neej luv-lub neej (txog 3-12 feeb) yuav tsum tau txais kev pab cuam intravenous tas mus li kev lis ntshav, uas txwv nws daim ntawv thov kho mob. Vim yog cov kws kho mob ua haujlwm tsis xws luag Txhim kho cov xaiv receptor: txhim kho uterine kev cog lus thiab txo cov kev mob plawv. Thaum xyoo 1960 thiab 1970s, ntau pab pawg tshawb fawb tau sim hloov cov qauv ntawm Oxytocin: Demoxytocin, synthesized hauv xyoo 1964, yog qhov ua tau zoo tab sis muaj kev ua haujlwm qis dua. Carboprost: Ib qho Prostaglandin Analogue siv rau Refractory Partpartum hemorrhage, tab sis nrog cov kev mob tshwm sim tseem ceeb. Nyob rau xyoo 1980, cov kws tshawb fawb los ntawm Swiss Ferring cov tshuaj uas pom tau tias C-Terminal hloov kho acid) tuaj yeem txhim kho kev ruaj khov. Methylation ntawm {19}} Txoj Haujlwm Cysteine ​​tuaj yeem txo cov oxididative degree. Cov kev tshawb pom no muab cov tswv yim tseem ceeb rau kev tsim cov carbetocin.

Cov qauv kev coj ua ntawm carbetocin (lub npe tshuaj: {{}}}}}} methyltyrosin-otocin):

• {{0 {0}}} Kev Damination: Txo aminopeptidase Defadation.
• {{0 {0}} Tyrosine Methylation: Txhim Kho Receptor Binding.
• C-Terminal - mercaptopropionic acid hloov chaw: ntev ntev-lub neej.
• Cov pab pawg ua kom tiav txoj kev xav tau-theem-theem peptide synthesis (SPPS) lub tswv yim:
• FMOC tiv thaiv pab pawg chemical: maj mam tsim cuaj peptide caj qaum.
• Sab Saw Kev Hloov Kho: Ib Theem Me Me Me Methylation.
• Oxidative Folding: Tsim ntawm Disulfide Bonds (CYS 1- Cys6).
• Hauv cov kev ua si vitro: zoo ib yam kev sib txawv rau Oxytocin receptor (Oxtr) (ec ₅₀ ~ 1 nm).
• Hauv vivo ib nrab-lub neej: cov qauv nas pom tau ib nrab-lub neej mus rau 40 feeb (vs Oxytocin 10 feeb).
• Kev sim uterine monsaction: ntev dua li oxytocin nyhuv.
• Kev Nyab Xeeb Kev Nyab Xeeb: Tsis muaj cov ntshav siab hloov pauv tau pom.
• Ib txoj kev tswj hwm ib zaug: Ib koob tshuaj ntawm 100 μ G pom muaj peev xwm.
• Pharmaconinetics: Ib nrab lub neej ntawm kwv yees li 30-45 feeb (thiab 5-10 feeb rau oxytocin).
• Kev tiv thaiv ntawm PPH: carbetocin (100 μ g iv) vs oxytocin (10 iu iv).

Nws tau pom zoo thawj zaug hauv Canada hauv 1997 nyob rau hauv lub lag luam npe duratocin. Tom qab 2000, European Union (Pabal) thiab ntau lub teb chaws Asian tau pom zoo zoo nws. Nyob rau hauv 2018, leej twg suav nrog carbetocin nyob rau hauv cov tshuaj tseem ceeb (rau pph kev tiv thaiv). Txo qhov xwm txheej ntawm PPH: los ntawm 5% rau 2% (cov ntaub ntawv thoob ntiaj teb). Tus nqi ua tau zoo: Ib qho koob tshuaj ib koob VS kev lis kev lis kev lis kev lis kev lis ntshav ntawm oxytocin, txuag cov peev txheej kho mob. Txais rov qab cov phiajcim rau kev taug kev:
Oxtr Kev → GQ Protein Coupling → Pospholipase C (PLC) ua kom → → uterine du cov leeg consaction.
 

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