Bimatoprost 155206-00-1

1 Kev Taw Qhia

Bimaprost yog ib qho tshuaj prostaglandin, uas yog thawj zaug siv los kho cov kab mob ophthalmic xws li glaucoma. Lub npe tshuaj yog Lumigan. Txawm li cas los xij, hauv kev kho mob, tus neeg mob tau npaj txhij pom tias txoj kab uas hla, qhov ntev thiab qhov ntom ntawm nws cov plaub muag tau nce ntau. Tom qab ntawd, bimalprost Chemicalbook tau siv rau hauv kev sim tshuaj xyuas ntawm cov plaub muag kev zoo nkauj, thiab nws cov txiaj ntsig loj ntawm cov plaub muag tuab thiab thickening ncaj qha coj mus rau lub hom phiaj ntawm Lattise los ntawm Lumigan lub tuam txhab tsim khoom, Erjian, uas tau pom zoo los ntawm US FDA thaum Lub Kaum Ob Hlis. 2008 thiab tau dhau los ua cov khoom lag luam rau kev ua kom cov plaub muag tsaus thiab tuab.

2 Muaj nuj nqi

ua tau zoo ntawm Brca1; P53 mis qog (intraperitoneal txhaj ntawm 50mg / kg ib hnub twg), tab sis Ecad nrog HR tsis txaus; P53 lub mis qog tsis muaj txiaj ntsig. tsis muaj tshuaj toxicity rau cov nas uas muaj qog nqaij hlav. OChemicalbooklaparib tau siv los kho cov qog nqaij hlav BRCA, xws li qog nqaij hlav zes qe menyuam, mob qog noj ntshav mis, thiab mob qog nqaij hlav prostate. Tsis tas li ntawd, Olaparib muaj kev xaiv hauv inhibiting ATM-tsis muaj cov qog hlwb, uas qhia tau tias tuaj yeem siv los ua tus neeg sawv cev rau kev kho mob ntawm ATM mutated lymph qog.

yog PARP inhibitor thiab tseem ua rau BRCA1 lossis BRCA2 kev hloov pauv. Olaparib muaj me ntsis cuam tshuam rau lub davhlau ya nyob twg thauj tog rau nkoj (polymerization) enzyme -1, thiab IC50 tus nqi ntau dua. Olaparib ntawm qhov concentration ntawm 30-100 nM ua rau SW620 hlwb thiab inactivated PARP-1. Piv nrog BRCA1 thiab BRCA2 cov kab ntawm tes txaus (Hs578T, MDA-MB-23Chemicalbook1, T47D), BRCA1 cov kab tsis muaj cell (MDA-MB-463 [1] thiab HCC1937) yog dhau-rhiab heev rau Olaparib inhibits PARP, thaiv kev kho lub hauv paus excision, thiab ua rau KB2P hlwb ua rau muaj kev nkag siab zoo rau Olaparib. Qhov tshwm sim yog tias ib txoj hlua tawg hloov pauv mus rau ob txoj hlua tawg thaum lub sij hawm DNA replication, yog li ua rau BRCA2 nyob ntawm kev sib txuas ua ke.

3 Daim ntawv thov

Bimaprost yog ib qho hluavtaws prostaglandin F2 Derivative, uas tuaj yeem xaiv simulate cov nyhuv ntawm prostaglandin tsim hauv lub cev, nce tus nqi ntawm aqueous lom zem ntau lawm, txo qhov tsis kam ntawm aqueous lom zem outflow, thiab txo intraocular siab (IOP) los ntawm kev ua kom cov dej ntws tawm. chemicalbook los ntawm trabecular meshwork channel thiab uveoscleral channel. Nws raug suav hais tias yog cov tshuaj tiv thaiv kab mob glaucoma hauv zos zoo tshaj plaws rau kev txo qis intraocular siab tam sim no. Nws yog qhov tsim nyog rau kev kho mob ntawm cov neeg mob uas muaj qhov qhib-angle glaucoma (POAG) lossis siab intraocular siab (OHT) uas tsis muaj txiaj ntsig nrog lwm cov tshuaj siv tshuaj intraocular siab.

1. Cov prostaglandin derivative latanoprost, xws li (Xalatan), tsub kom lub outflow ntawm aqueous humor uveoscleral piv nrog marprost (lub npe lag luam Lumigan) thiab travoprost (Travatan). Bimaprost kuj nce trabecular outflow. 2. Hauv zos - Adrenaline tuaj yeem txo qhov tsim ntawm receptor antagonists hauv ciliary aqueous lom zem, xws li thiazide, levobunol (Betagan) thiab betalol. 3. Cov txheej txheem dual ntawm Alpha2-adrenoceptor agonists xws li bromonidine (Alphagan) txo cov dej ntau lawm thiab ua rau cov kab mob trabecular nce ntxiv. 4. Ib rooj plaub uas zoo ib yam li epinephrine thiab dipiveChemicalbookfrin (Propine) tau nce cov dej ntws tawm ntawm kev lom zem los ntawm trabecular meshwork, thiab tej zaum los ntawm txoj kev uveoscleral outflow, uas tej zaum yuav tshwm sim los ntawm Kev Ua ntawm 2-receptor agonists. 5. Parasymopathics, xws li kev ua haujlwm ntawm ciliary nqaij contraction Roca, zawm lub trabecula thiab tso cai rau lub outflow ntawm aqueous lom zem nce. Ecotropiopate yog siv rau mob glaucoma. 6. Piv txwv li, Trusopt thiab Azopt txo qhov tso tawm ntawm carbonic anhydrase inhibitors hauv aqueous lom zem los ntawm inhibiting cov carbonic anhydrase acetylazolamide hauv lub cev ciliary. 7. physostigmine kuj tseem siv los kho mob glaucoma thiab ncua lub plab khoob.

Bimaprost - timolol maleate compound qhov muag tee tau raug pom zoo los ntawm EU kev tswj hwm tshuaj kom txo qis qhov tsis zoo ntawm kev siv ib leeg Intraocular siab lossis ocular hypertension hauv cov neeg mob uas muaj qhov qhib-angle glaucoma uas tsis teb txaus rau kev kho mob nrog receptor blockers lossis prostaglandin analogues. Qhov kev sib xyaw qhov muag no muaj 0.03 feem pua ​​​​ntawm bimalprost thiab 0.5 feem pua ​​​​ntawm timolol maleate hauv Chemicalbook. Nws muaj peev xwm muab tau zoo heev kev kho mob intraocular siab tswj cov nyhuv ib zaug ib hnub twg, thiab nws cov nyhuv yog superior rau cov bimalprost los yog timolol maleate ib leeg. Cov kev sim tshuaj ntsuam xyuas tau lees paub tias cov tshuaj muaj qhov ua tau zoo heev, suav nrog qhov tshwm sim ntawm qhov muag qhov muag yog 40 feem pua ​​qis dua li ntawm bisoprostol ib leeg.

4 Tus Qauv Zoo

5 Flow Chart

S1: bisoprostol, anhydrous tetrahydrofuran, benzalkamine, ethyl phenylpropionate, penetration enhancer thiab activator

Raws li cov khoom siv raw;

S2: Muab bisoprostol thiab anhydrous tetrahydrofuran tso rau hauv lub tov khoom thiab sib tov ntawm 10-20 degree -

20min, ces txav mus rau lub pulverizer, zuaj nws los tsim ib tug sib tov;

S3: Lim sib tov a hauv s2, thiab lim txoj kab uas hla tsis ntau tshaj 30 meshes, kom tshem tawm cov dej ntau hauv cov dej sib tov.

Cov khoom me me;

S4: Muab qhov sib tov ib zaug rau hauv ib qho agitator ntawm 30-40 degree C, thiab muab phenylpropionate Z ester thiab nkag mus rau hauv nws

Ntxiv tus neeg sawv cev, sib tov thiab do nws tusyees, thiab tom qab ntawd ntxiv benzalkamine rau nws dua tom qab 60-90s ntawm cov tshuaj tiv thaiv, thiab

Sib tov sib xyaw thiab nplawm kom tsim cov khoom sib xyaw b;

S5: Tom qab cov saum toj no, maj mam ntxiv tus neeg sawv cev rau hauv kev sib xyaw b, thiab txuas ntxiv mus rau 3-6 min tom qab ntxiv,

6 NMR

7.MOA

Tsib yam ntawm bisoprostol feem ntau yog siv los kho qhov muag kab mob. Vim li cas thiaj yuav tsum tau FDA tshwj xeeb [] tso rau pem hauv ntej kev tshuaj xyuas cov tshuaj pleev ib ce

Yuav ua li cas txog txoj kev ntsuas tsib yam no? Yog vim li cas yog tias ob peb xyoos dhau los, ib lub tuam txhab ua lag luam hauv Tebchaws Meskas tau pom tias bisoprostol tau siv los kho qhov muag

Thaum lub sij hawm tus kab mob no, txoj kab uas hla, ntev thiab ceev ntawm cov plaub muag ntawm cov neeg mob tau ho nce.

Tom qab ntawd, ntau qhov kev sim tau pom tias marprost tuaj yeem txhawb kev loj hlob ntawm cov plaub hau xim, yog li ntau lub tuam txhab tshuaj pleev ib ce pib.

Tsom ntsoov rau kev kho mob ntawm qhov muag kab mob xws li bisoprostol, kawm txog nws cov nyhuv ntawm cov plaub hau poob, cov plaub muag dub, thickening thiab loj hlob.

Lub sij hawm no, txoj kev tso tawm los ntawm Food and Drug Administration yog tsuas yog siv hauv qab zib, kua, gel, siv quav ciab thiab hmoov tshuaj pleev ib ce.

Kev txiav txim siab zoo thiab ntau yam ntawm tsib yam xws li prostaglandin feem ntau yog ua los ntawm kev ua haujlwm siab ua kua chromatography thiab huab hwm coj spectrometry.

Lub hauv paus ntsiab lus tshwj xeeb yog vortex tus qauv nrog saturated sodium chloride tov, disperse thiab sib tov nws tusyees, thiab ces muab rho tawm los ntawm Z nitrile ultrasound, centrifuge, thiab coj lub supernatant.

Cov tshuaj yog diluted nrog dej, thiab thaum kawg sib cais los ntawm kev ua haujlwm siab ua kua chromatography thiab kuaj pom los ntawm huab hwm coj spectrometry detector. Cov txiaj ntsig Raws li lub sijhawm khaws cia thiab cov yam ntxwv ion khub

Tus txheeb ze abundance piv yog qualitative, lub quantitative ion yog quantitative rau lub ncov cheeb tsam, thiab cov ntsiab lus yog xam los ntawm tus qauv nkhaus txoj kev.

8 Kev Tsim Nyog

Tom qab xyoo ntawm kev tsim khoom, peb lub tuam txhab tau txais cov ntawv tso cai tsim khoom tsim nyog.

9 Tus khub

Peb muaj ntau tus neeg koom tes mus sij hawm ntev thoob plaws ntiaj teb.

10 Cov neeg siv khoom xyuas

Peb tau txais kev qhuas ntau ntawm lwm lub platform, thiab peb cov neeg siv khoom tau zoo siab heev ntawm cov khoom tsim los ntawm peb lub tuam txhab.

11 Exhibition

Peb lub tuam txhab koom nrog ntau yam kev nthuav qhia hauv tsev thiab txawv teb chaws txhua xyoo, thiab sib txuas lus nrog cov neeg siv khoom ntsej muag.

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