Buserelin CAS 57982-77-1

Buserelin, GNRH Analogue. Feem ntau nthuav tawm raws li dawb los yog tawm cov hmoov tawv dawb, cov molecular formula ntawm lub zog ntawm Busherelin yog 1239.424-1, thiab muaj qhov tseeb ntawm 1238.656006. Qes solubility hauv dej, manifested li me ntsis soluble hauv dej. Qhov no txhais tau tias thaum ua cov tshuaj lom neeg siv tshuaj, nws yog qhov tsim nyog los xav txog kev xaiv ntawm cov kuab tshuaj thiab cov tshuaj tiv thaiv kev ua kom pom tau tias koom nrog cov tshuaj tiv thaiv. Ib qho ntxiv, cov solubility ntawm buscherelin nyob rau hauv dilute acids kuj tsawg, uas txuas ntxiv txwv nws daim ntawv thov hauv qee cov tshuaj tiv thaiv. Qhov kev kwv yees acidity coefficient (PKA) yog 9.82 ± 0.15. Cov acidernity coefficient yog ib qho tseem ceeb uas piav qhia cov acidity thiab alkalinity ntawm cov tshuaj, pom tias nws muaj peev xwm cuam tshuam hydrogen ions hauv kev daws teeb meem. Buscherin muaj tus nqi PKA siab, qhia txog nws txoj kev ruaj khov los yog Alkaline tej yam kev mob, thaum nws yuav nquag faib lossis tsis muaj kev cuam tshuam hauv acidic tej yam kev mob. Nws muaj ntau txoj haujlwm thiab cov txiaj ntsig tseem ceeb thiab ua lub luag haujlwm tseem ceeb hauv kev kho mob. Nws cov tshuab ntawm kev nqis tes ua hauv kev kho cov txha epleoporosis, txiv neej lub cev mob cancer, mob cancer thiab tswj cov tshuaj ntawm kev txhawj xeeb ntawm kev txhawj xeeb. Nws kuj yuav tsum tau kawm ntxiv thiab tshawb nrhiav cov ntawv thov cov txiaj ntsig ntawm busherelin hauv lwm liaj teb kom ua rau muaj kev pab ntau dua rau kev txhim kho tshuaj.

Buserelinyog ib qho tshuaj nrog ntau daim ntawv thov kho mob, thiab nws cov haujlwm yog ntau yam thiab tseem ceeb.

Kho cov osteoporosis

 

Ua ib qho tshuaj tseem ceeb, nws muaj qhov kho tau muaj nuj nqis kho rau cov kabmob caj qaum. Osteoporosis yog tus kab mob pob txha uas muaj tus mob pob txha los ntawm thinning thiab tsis muaj zog ntawm cov pob txha, ua rau nws kis tau. Busherelin zoo txhim kho cov tsos mob ntawm cov neeg mob oseoporosis los ntawm kev txhawb nqa pob txha kev loj hlob thiab nce pob txha ceev. Nws lub ntsiab tivthaiv, Estradiol, yog qhov tseem ceeb hauv tib neeg lub cev uas ua lub luag haujlwm tseem ceeb hauv kev ua niam txiv thiab muaj peev xwm. Estradiol tuaj yeem txhawb cov kev coj ua kom zoo nkauj Rau cov neeg muaj txha txha caj qaum, cov tsheb thauj mus los zoo kev loj hlob, nce pob txha ceev, thiab yog li txhim kho pob txha kev noj qab haus huv.

Kev Kho Mob ntawm Txiv Neej Kev Loj Hlob Rau Lub Cev & Kho Prostate thiab Cancer Cancer Mob Cancer

 

Ib qho ntxiv rau kev kho cov txha epteoporosis, nws kuj tuaj yeem siv los kho txiv neej mis. Txiv neej lub mis txoj kev loj hlob yog ib tus txiv neej tus kab mob uas coj tau cov tsos mob los ntawm cov tsos mob xws li lub mis o thiab mob. Busherelin tau txhim kho cov tsos mob ntawm txiv neej kev loj hlob ntawm cov txiv neej mis los ntawm kev tswj hwm qib tshuaj hormones ntawm lub mis thiab cov kua mis. Estradiol, raws li lub ntsiab tivthaiv ntawm busherelin, muaj cov nyhuv inhibities ntawm txoj kev loj hlob thiab zais ntawm lub mis zom mov thiab tuaj yeem pab txhawb cov qauv nqaij lub mis.

Nws tseem muaj qee qhov kev thov muaj nuj nqis rau hauv kev kho mob kheesxaws mob prostate thiab mob cancer mis. Raws li gonadotropin - tso cov yam ntxwv, nws ua rau muaj cov tshuaj tiv thaiv kab mob antes Lub tshuab no ua nws cov tshuaj zoo rau kev kho mob kheesxaws mob prostate thiab mob cancer mis. Nyob rau hauv kev kho mob ntawm prostate cancer, Busherelincan txo cov ntsuas tes taw titorosterone, yog li inhibit cov qog kev loj hlob thiab kis tau. Nyob rau hauv kev kho mob cancer mis, nws tuaj yeem tiv thaiv kev rov ua mob cancer mis hauv cov poj niam postmenopausal thiab txhim kho cov kev kho mob.

Kev kho mob ntawm Envometriosis & tswj cov haujlwm endocrine

 

 

Ntxiv rau, nws kuj tseem siv tau los kho endometriosis. Endometriosis yog ib hom mob gynecological uas muaj tus cwj pwm los ntawm kev loj hlob ntawm cov ntaub so ntswg sab nraud sab nraum lub terine kab noj hniav. Busherelin inition ntawm Lutioninizing hormone thiab follicle stimulating hormone primenary caj dab, thiab yog li intabits txoj kev loj hlob thiab muaj ectopic endometrium. Qhov kev siv tshuab ntawm kev ua ua rau cov tshuaj tiv thaiv busherelin rau kev kho cov tsos mob endometrisosis, uas tuaj yeem ua rau lawv lub neej zoo li no, thiab txhim kho lawv lub neej zoo.

Ntxiv rau cov ntawv thov tshwj xeeb tau hais los saum toj no, nws tseem muaj txoj haujlwm ntawm kev tswj hwm endocrine ua haujlwm. Raws li cov tshuaj hormonal, cov tsheb thauj hluav taws tuaj yeem cuam tshuam rau cov kev zais thiab cov tshuaj khib nyiab ntawm ntau cov tshuaj hormones hauv tib neeg lub cev, yog li tswj qhov sib npaug ntawm cov endocrine system. Piv txwv li, Buardinin tuaj yeem cuam tshuam rau txoj haujlwm ntawm cov qog endocrine xws li cov qog ua yeeb yaj kiab xws li cov qog ua suab paj nruag, thiab tswj cov txheej txheem zais ntawm cov tshuaj hormones cuam tshuam. Qhov kev tswj hwm cov nyhuv ntawm no yog qhov tseem ceeb tshaj plaws rau kev tswj hwm qhov sib npaug thiab kev ruaj ntseg ntawm tib neeg endocrine system.

Buserelinyog ib qho tseem ceeb kws tshuaj hauv paus nruab nrab tsuas yog siv hauv kev tsim khoom ntawm qee yam tshuaj tua kab mob. Nws belongs rau peptide cov tshuaj hormones thiab muaj cov yam ntxwv xws li muaj kuab lom muaj zog thiab ntev- ntev kev ua tau zoo. Synthesis ntawm Buscherelin cuam tshuam nrog ntau cov kauj ruam, suav nrog kev hws, hydroxylation, methylation, thiab lwm yam kev tawm tsam.

Cov kauj ruam synthesis

1. Synthesis ntawm Aminophenol

Firstly, cov kev tawm tsam hws ntawm Aniline thiab Acetaldehyde nqa tawm hauv qab cov acidic tej yam kev txwv los tsim aminophenol. Kev siv tshuaj rau cov kauj ruam no yog raws li hauv qab no:

C₆H₅Naj₂+ Ch₃Cho → c₆H₅Tus niam₂Huag (nyob rau hauv cov xwm txheej acidic)

Qhov kev tawm tsam no feem ntau tau nqa tawm hauv kev siv hluav taws xob hydrochloric ntawm hydrochloric acid lossis sulfuric acid, thiab cov tshuaj tiv thaiv kub yog tswj tau ntawm chav tsev kub thiab npau npau. Tom qab cov tshuaj tiv thaiv tau ua tiav, Aminophenol yog sib cais los ntawm distillation lossis cov txheej txheem extraction.

2. Khoom cua ntawm 2-hydroxiline

Tom ntej no, hydroxylation cov tshuaj ntawm aminophenol thiab formaldehyde yog nqa tawm nyob rau hauv Alkaline tej yam kev mob los tsim 2-hydroxyaniline. Kev siv tshuaj rau cov kauj ruam no yog raws li hauv qab no:

C₆H₅Tus niam₂Oh + hcho → c₆H₆(Oh) nhch₂Oh (nyob rau hauv ib tug alkaline tej yam kev mob)

Qhov kev tawm tsam no feem ntau tau nqa tawm hauv kev daws teeb meem alkaline ntawm sodium hydroxide, thiab cov tshuaj tiv thaiv kub yog tswj tau ntawm chav tsev kub thiab 60 degree. Tom qab cov tshuaj tiv thaiv tiav, 2-hydroxiline tau sib cais los ntawm acidification, extraction thiab lwm txoj kev.

3. Khoom cua ntawm 2-methyl-4-nitroaniline

Tom qab ntawd, 2-hydroxyaniline yog methylated nrog depethyl sulfate nyob rau hauv Alkaline tej yam kev mob los tsim 2-methyl-4-nitroaniline. Kev siv tshuaj rau cov kauj ruam no yog raws li hauv qab no:

C₆H₆(Oh) nhch₂Oh + (ch₃)₂Yog li₄ → C₆H₇N (ch₃)+H₂O + li ntawd₂(nyob rau hauv cov xwm txheej alkaline)

Qhov kev tawm tsam no feem ntau tau nqa tawm hauv kev daws teeb meem alkaline ntawm sodium hydroxide, thiab cov tshuaj tiv thaiv kub yog tswj tau ntawm chav tsev kub thiab 80 degree. Tom qab cov tshuaj tiv thaiv tiav, 2-methyl-4-nitroaniline tau sib cais los ntawm kev rho tawm, crystallization thiab lwm txoj kev.

4. Khoom cua ntawm Busscherin

Thaum kawg, 2-methyl-4-nitroaniline tau raug cov tshuaj tiv thaiv diazotization nrog sodium nitrite nyob rau hauv acidic tej yam kev mob los tsim busscherin. Kev siv tshuaj rau cov kauj ruam no yog raws li hauv qab no:

C₆H₇N (ch₃) + Nano₂+ Hc → c₆H₇N (ch₃) TSIS TAU + NACL + H₂O (nyob rau hauv acidic tej yam kev mob)

Qhov kev tawm tsam no feem ntau tau nqa tawm hauv cov kua qaub ntawm hydrochloric acid lossis sulfuric acid lossis cov tshuaj tiv thaiv kub yog tswj tau ntawm 0-5 degree. Tom qab cov tshuaj tiv thaiv tau ua tiav, busnerelin tau sib cais los ntawm kev rho tawm, crystallization, thiab lwm txoj kev.

Los ntawm cov theem saum toj no, peb tuaj yeem suav nrog cov tshuaj tseem ceeb ntawm kev caij tsheb. Txhua kauj ruam ib kauj ruam muaj cov tshuaj lom neeg thiab cov xwm txheej uas xav tau kev tswj nruj kom ntseeg tau tias yog qhov zoo thiab huv ntawm covBuserelinCov. Lub caij no, vim muaj kev sib koom tes ntawm qee cov tshuaj lom thiab kev tiv thaiv kev nyab xeeb thiab ib puag ncig kev nyab xeeb thiab ib puag ncig kev nyab xeeb ntawm cov neeg sim thiab cov kev ruaj khov ntawm ib puag ncig.

Buserelinyog ib qho kev ua yeeb yam zoo nkauj gonadotropin - tso cov tshuaj hormones (GNRH, tseem hu ua LHRH) Analogue, yog thawj tiam ntawm GNRH agonists. Txij li thaum nws pib hauv xyoo 1970, nws tau dhau los ua kev kho mob qog noj ntshav (endometriosomy, thiab tswj kav dej number cas), thiab muaj mob qog nqaij hlav inclarbululation hauv pab kev pab thev naus laus zis (kos duab). Thaum xyoo 1960, cov kws tshawb fawb tau nthuav tawm cov tshuab uas cov hypothalamus regonizing hormone (lH) los ntawm kev zais gonadotropin {}} tso cov hormone (gnrh). GNRH yog tus lej peptide uas nws cov qauv tau txheeb xyuas nws tus kheej ntawm cov kws tshaj lij ntawm xyoo 1971, nws tau muab tsub rau 1977 Nobel nqi zog hauv physiology lossis tshuaj. Ib nrab - lub neej ntawm ntuj gnrh (pgllu nws txoj kev sib cav sib ceg ntawm cov enzymes, uas txwv nws cov ntawv thov. Yog li no, cov kws tshawb fawb pib tshawb nrhiav kom muaj cov analog zoo li GNRH analogs los txhim kho lawv txoj kev ua tau zoo thiab ntev ntev ntawm kev nqis tes ua. Thaum xyoo 1970, ib pab neeg ntawm Heechst AG (tam sim no ib feem ntawm Sanofi) hauv Tebchaws Askiv tau pib ua haujlwm ntawm GNRH analogs. Lawv pom tias 6 lub glycine (gly ⁶) thiab 10 glycinamide (gly-nh ₂) ntawm GNRH yog qhov tseem ceeb rau enzyme degradation. Los ntawm cov amino acid hloov thiab hloov kho, pab pawg tshawb fawb pom tias:

• Lub 6 Gly → d - amino acid (xws li d {}} Trp) tuaj yeem txhim kho enzyme ruaj khov.
• Gly-NH ₂ → ethylamide (- NH Et) at position 10 can enhance receptor affinity.

Tom qab ntau cov puag ncig ntawm kev ua kom zoo, lub hoove pab pawg synthes buserelin (Amesly Codenamed Hoe-766) xyoo 1975, nrog cov qauv hauv qab no:
[PDLU - nws-}}}}}} {} {9} - nhet]
Embellishments:

• Lub 6 d- sine (d -}}}} {{{} lub neej.
• Tert Butyl hloov kho (TBU): Txawj siv hydrophobicity thiab txhim kho cov membrane nkag.
• C -} Terminal Ethylamide (Pro NHET): Txhim Kho Gnrh Receptor Binding.

Cov kev hloov pauv no nce kev ua haujlwm ntawm buserelin los ntawm 50- kub 1 zaug piv rau ib nrab-lub neej mus txog 1 teev (subcutaneous txhaj tshuaj).

Buserelin yog cov khoom siv hluavtaws Gnrh analog nrog cov ntawv thov hluav taws xob tseem ceeb hauv kev tswj hwm ntawm ntau yam me nyuam thiab tsis muaj me nyuam sib deev. Nws cov txheej txheem tshwj xeeb ntawm kev nqis tes ua, uas koom nrog kev pib ua raws li los ntawm kev ua kom muaj txiaj ntsig ntawm cov pa yeeb yaj kiab ntawm HPG Axis thiab cov kev cai ntawm kev sib deev Hormone ntau lawm. Buserelin tau ua pov thawj kom ua tau zoo hauv kev kho mob ntawm endometrisosis, hauv kev pab cuam tus mob probuctive thev naus laus zis. Txawm li cas los xij, zoo li txhua hom tshuaj, nws muaj kev nyab xeeb profile nrog cov tshwm sim kev tshwm sim thiab siv tshuaj yeeb. Tus kws kho mob yuav tsum ua tib zoo xav txog cov txiaj ntsig thiab kev pheej hmoo ntawm cov neeg mob busterelin thiab soj ntsuam cov neeg mob kom ntseeg tau cov txiaj ntsig zoo. Kev tshawb fawb ntxiv yog txuas ntxiv mus tshawb cov ntawv thov tshiab ntawm cov busterelin thiab txhawm rau txhim kho nws txoj kev nyab xeeb thiab kev ua tau zoo hauv chaw kuaj mob.

Cim npe nrov: Buserelin CAS 57982-77-1, Cov chaw tsim khoom, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, rau muag