Scopolamine butylbromideyog cov organic compound nrog cov tshuaj formula C21H30BrNO4 thiab molecular hnyav 440.3804 g/mol. Cov compound yog cov hmoov dawb crystalline, yuav luag insoluble hauv dej, nws tuaj yeem tsim cov kev daws teeb meem hauv qee cov organic solvents, thiab yooj yim soluble hauv ethanol, chloroform thiab benzene. yog ib qho ionic compound uas muaj qhov sib txawv ionization tas li hauv dej. Ntawm lawv, ionization tas li ntawm N (CH3) 3 pawg ntawm acetylcholine receptor yog 9.4 × 10-5; thiab ionization tas li ntawm Br-ion yog 7.3 × 10-17. Nws yog nyob rau hauv chav kawm ntawm acetylcholine receptor antagonists, thiab tuaj yeem so cov leeg du thiab txo qis kev zais cia los ntawm kev thaiv cov kev ua ntawm M1-M5 acetylcholine receptors.
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Tshuaj Formula |
C21H30BrNO4 |
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Exact Mass |
439 |
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Molecular Luj |
440 |
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m/z |
439 (100.0%), 441 (97.3%), 442 (22.1%), 440 (16.2%), 440 (6.5%), 441 (1.2%), 443 (1.2%), 443 (1.2%), 441 (1.1%) |
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Elemental Analysis |
C, 57,28; H, 6,87; Saib, 18.14; N, 3.18; 14.53 Nws |
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Scopolamine butylbromide(feem ntau hu ua Buscopan) yog ib qho tshuaj siv los kho cov tsos mob ntawm plab hnyuv thiab belongs rau ib chav kawm ntawm cov tshuaj anticholinergic. Cov tshuaj no tsuas yog ua kom cov leeg du thiab txo qis kev zais cia los ntawm kev thaiv qhov kev txiav txim ntawm acetylcholine, thiaj li ua tiav lub hom phiaj ntawm kev kho thiab txo cov teeb meem hauv plab. Tam sim no, nws tau siv dav hauv kev kho mob, thiab nws cov kev siv yuav raug qhia kom ntxaws hauv qab no.
Nws tsuas yog ua rau cov leeg du ntawm lub plab zom mov, thiab tuaj yeem txo cov tsos mob xws li mob plab los ntawm spasms thiab contractions ntawm txoj hnyuv. Yog li ntawd, nws yog feem ntau siv los kho ntau yam kab mob ntsig txog kab mob plab, xws li mob plab, plab hnyuv ulcers, biliary ascariasis (kab tom), colitis, cholecystitis, plab hnyuv, thiab lwm yam.
1.1 Mob plab:
Lub plab cramping yog ib qho mob ntawm qhov mob thiab qhov tsis xis nyob uas tshwm sim los ntawm qhov txawv txav ntawm lub plab zom mov. Nws muaj cov nyhuv ntawm kev so cov leeg du ntawm lub plab zom mov, uas tuaj yeem txo qhov mob thiab tsis xis nyob.
1.2 Cov kab mob hauv plab:
Gastrointestinal ulcer yog ib qho kev raug mob ntawm lub plab hnyuv mucosa, feem ntau tshwm sim los ntawm cov kua qaub ntau dhau. Nws tuaj yeem ua lub luag haujlwm hauv kev kho mob plab hnyuv los ntawm kev txo qis ntawm cov kua qaub los txo qis kev ua xua thiab cov tsos mob ntawm lub plab zom mov.
1.3 Biliary ascariasis:
Biliary ascariasis yog ib yam kab mob ntawm biliary obstruction los ntawm roundworms parasitizing nyob rau hauv lub kua tsib duct. Nws txo cov tsos mob los ntawm kev so / txo cov leeg nqaij hauv daim siab, pancreas, duodenum, thiab gallbladder.
1.4 Colitis:
Colitis yog ib qho mob ntawm phab ntsa ntawm cov hnyuv, cov tsos mob tseem ceeb ntawm cov mob plab thiab raws plab. nws relieves cov tsos mob no los ntawm kev txo cov contractions thiab spasms ntawm lub plab.
1.5 Cholecystitis:
Cholecystitis yog ib qho mob ntawm lub gallbladder, cov tsos mob tseem ceeb uas yog mob plab thiab kub taub hau. Nws txo cov tsos mob no los ntawm kev ua kom cov leeg du ntawm lub gallbladder thiab txo cov zais zis.
1.6 Kev mob plab hnyuv:
Txoj hnyuv plab yog ib yam mob tshwm sim los ntawm kev txhaws hauv plab hnyuv. Cov tsos mob muaj xws li mob plab, ntuav, thiab cem quav. Nws tuaj yeem txo cov tsos mob no los ntawm kev ua kom cov leeg du ntawm lub plab zom mov.
2. So uterine du nqaij:
Ntxiv nrog rau kev siv los kho cov kab mob hauv plab hnyuv, nws tseem tuaj yeem siv los ua cov tshuaj ua ntej rau kev phais gynecological kom so cov leeg nqaij uterine. Nws tuaj yeem txo qhov nro thiab siab ntawm lub tsev menyuam sai sai, ua rau kev ua haujlwm smoother thiab nyab xeeb.
3. Cov nyhuv tiv thaiv neuronal:
Ntxiv nrog rau cov kev kho mob saum toj no, nws kuj muaj qee yam kev siv hauv thaj tsam ntawm neurology. Cov kev tshawb fawb tau pom tias cov tshuaj muaj peev xwm tiv thaiv cov neurons los ntawm kev tswj cov neuronal membrane permeability thiab sodium tam sim no thiab lwm yam mechanisms, thiab txo cov tsos mob los ntawm cov kab mob thiab kev raug mob ntawm lub paj hlwb thiab cov leeg nqaij.
4. Relax airway smooth nqaij:
Nws tseem tuaj yeem txo cov tsos mob tshwm sim los ntawm cov kab mob ua pa xws li mob hawb pob thiab mob ntsws ntsws rau qee yam los ntawm kev so cov leeg nqaij ntawm txoj hlab ntsws. Lub mechanism ntawm kev txiav txim ntawm cov tshuaj tseem nyob rau hauv kev tshawb fawb thiab kev tshawb fawb ntxiv.
5. Inhibit qaub qaub secretion:
Nws kuj inhibits qaub ncaug ntau lawm nyob rau hauv lub qhov ncauj thiab larynx, yog li pab nyob rau hauv tej yam kev phais thiab kho cov txheej txheem. Tsis tas li ntawd, nws tuaj yeem txo cov tsos mob tsis xis nyob xws li qhov ncauj qhuav los ntawm salivation.
Hauv kev xaus, nws tau dhau los ua ib qho ntawm cov tshuaj tseem ceeb hauv kev lag luam kho mob, thiab tau siv dav hauv ntau qhov chaw xws li kab mob hauv plab, gynecology, neurology, thiab ua pa. Txawm hais tias cov tshuaj muaj qee qhov kev pheej hmoo thiab cov tsos mob tsis xis nyob thaum lub sijhawm kho, nws txoj kev kho mob yog qhov tseem ceeb heev thiab tsim nyog nyob rau hauv kev siv kom raug thiab saib xyuas.
Scopolamine butylbromide(feem ntau hu ua Buscopan) yog ib qho tshuaj siv los kho cov tsos mob ntawm plab hnyuv, thiab nws cov qauv tshuaj zoo ib yam li Scopolamine hydrobromide. Rau cov tuam txhab xws li Shaanxi Chuzhan Chemical Co., Ltd., nrhiav tau txoj kev sib xyaw ua tau zoo thiab ua tau tsis tau tsuas yog txo cov nqi tsim khoom, tab sis kuj ua kom cov khoom zoo thiab cov khoom tsim tawm.
Traditional chemical synthesis method:
1. Synthetic route ib:
Txoj kev hluavtaws los ntawm kev tshawb fawb qhia ("Synthesis of buscopan derivatives"), cov kauj ruam tseem ceeb yog raws li hauv qab no:
Kauj Ruam 1: Cov tshuaj tiv thaiv ntawm 2-bromoisopropylacetophenone nrog N-methyl-2-pyridinecarboxamide:
Sib tov 2-bromoisopropylacetophenone nrog N-methyl-2-pyridinecarboxamide thiab hnov mob ntawm 85 degree rau ob peb teev nyob rau hauv lub xub ntiag ntawm cesium chloride kom tau cov khoom.
Kauj Ruam 2: Cov tshuaj tiv thaiv ntawm 2-bromoisopropyl-N-methyl-2-pyridinecarboxamide nrog propylene oxide:
Cov khoom saum toj no yog tov nrog propylene oxide thiab nplawm ntawm chav tsev kub nyob rau hauv lub xub ntiag ntawm sodium hydroxide rau ob peb teev kom tau cov khoom.
Qhov zoo ntawm txoj kev siv hluavtaws no yog cov tshuaj tiv thaiv me me, thiab tsis tas yuav siv ntau cov kuab tshuaj lom thiab teeb meem thiab cov tshuaj reagents. Txawm li cas los xij, kev sib cais thiab kev ua kom huv ntawm cov txheej txheem no yog qhov nyuaj, thiab cov txiaj ntsig tsis zoo.
2. Synthetic txoj kev ob:
Txoj kev hluavtaws yog muab los ntawm cov ntaub ntawv patent (US Patent 4418109 A), thiab cov kauj ruam tseem ceeb yog raws li hauv qab no:
Kauj Ruam 1: Cov tshuaj tiv thaiv cis-4-hydroxy-3-methoxyphenylacetic acid nrog 2,3-dibromopropionyl bromide:
cis-4-hydroxy-3-methoxyphenylacetic acid yog tov nrog 2,3-dibromopropionyl bromide thiab reacted rau ob peb teev ntawm chav tsev kub nyob rau hauv lub xub ntiag ntawm ethanol muab 2-({{5 }}hydroxy-3-methoxy phenylacetic acid)-2, 3-dibromopropyl ester.
Kauj Ruam 2: Recrystallization ntawm 2-(4-hydroxy-3-methoxyphenylacetic acid)-2, 3-dibromopropyl ester:
Cov khoom saum toj no tau recrystallized kom tau txais cov khoom lag luam nrog ntau dua purity.
Kauj Ruam 3: Cov tshuaj tiv thaiv ntawm 2-(4-hydroxy-3-methoxyphenylacetic acid) propionamidine nrog metabromic acid:
Sib tov 2-(4-hydroxy-3-methoxyphenylacetic acid) propionamidine nrog metabromide thiab ua rau ntau xuab moos ntawm chav tsev kub hauv qhov muaj ethanol kom tau txais cov khoom.
Qhov kom zoo dua ntawm txoj kev siv hluavtaws no yog qhov kev sib cais thiab kev ua kom huv huv yog qhov ua tau zoo, cov khoom muaj purity siab, thiab cov yield yog qhov zoo tagnrho. Txawm li cas los xij, cov kev mob tshwm sim kuj hnyav heev thiab yuav tsum muaj qee yam kev sim tshuaj lom neeg.
Melting point 142-1440c, Kev sib hloov tshwj xeeb D20 - 20.8 degree (C=3 hauv dej), Cia txias txias 2-8 degree C, Solubility H2O: 50 mg / ml, Morphological hmoov, Xim dawb, Kev ua haujlwm kho qhov muag[ ] 25/D 20.8 degree , c=3 hauv H2O(lit.), Kev ceeb toom qhia, Kev piav qhia txog H302, Kev Ceeb Toom P301 + p312 + p330, Dangerous goods sign xn, Hazard category code 22, WGK Germany 3, RTECS No. ym350000, Toxicity LD50 in nas (mg/kg): 15.6 iv; 74 ib;. 5 70s;ua. 3000 qhov ncauj (Stockhaus, Wick)
Scopolamine butylbromideyog ib tug complex organic compound nrog molecular mis C21H30BrNO4. Nws belongs rau cov chav kawm dimethyloxymuscarinic ntawm cov tshuaj, zoo ib yam li atropine, tab sis piv nrog atropine, nws bromide ion hloov cov pab pawg hydroxyl.
Cov qauv molecular ntawm peoduct muaj cov qauv carboxylic acid monoester (COOCH2CH2CH2CH3) thiab cov qauv benzyloxycarbonyl (C6H5CH2OCO) uas muaj bromine atom. Ntawm lawv, pawg benzyl thiab pawg methyl txuas nrog rau carbonyl los ua ib lub nplhaib rau-tus tswv cuab, thiab lub nplhaib rau lub nplhaib txuas nrog rau lwm tsib lub nplhaib. Muaj ib pawg txiv neej nrog peb hydrogen atoms, ib pawg amino thiab ib lub pa oxygen atom ntawm tsib lub nplhaib. Nyob rau hauv cov qauv imine, cov atoms nyob rau hauv plaub txoj haujlwm sib txawv ntawm tsib lub nplhaib yog txuas nrog ntau pawg, raws li qhia hauv daim duab:
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Cov qauv molecular no ua rau cov khoom lag luam muaj cov nyhuv anticholinergic zoo ib yam li ntawm atropine, thiab tib lub sijhawm, kev hloov pauv ntawm bromine atoms txo cov teebmeem hauv nruab nrab ntawm cov tshuaj atropine. Tsis tas li ntawd, cov qauv ntawm tsib-ntiv nplhaib ib feem kuj endows nws nrog tej yam stability.
Nws yog ib qho tshuaj anticholinergic, thiab nws cov nyhuv feem ntau yog ua kom tsis muaj zog ntawm acetylcholine los ntawm kev sib tw antagonizing qhov kev txiav txim ntawm acetylcholine ntawm M1-M5 receptors. Nyob rau hauv lub plab zom mov, nws tuaj yeem so cov leeg du, txo cov dej tso tawm, thiab muaj kev kho mob ntawm kev zom zaub mov, plab tsis xis nyob thiab lwm yam kab mob. Nyob rau hauv lub cev muaj zog, nws muaj peev xwm txo tau cov leeg nqaij spasm, thiab muaj ib co nyhuv ntawm alleviating lub cev muaj zog kab mob xws li spastic torticollis. Tsis tas li ntawd, hauv kev ua pa, nws tuaj yeem siv los ua bronchodilator.
Nws tuaj yeem nkag mus rau hauv lub cev los ntawm txoj hnyuv thiab cov hlab ntsha-hlwb barrier tom qab tswj qhov ncauj lossis txhaj tshuaj. Hauv lub plab hnyuv, nws nqus tau sai heev, mus txog qib ntshav siab tshaj plaws hauv li 1-2 teev, thiab nce qib ntshav siab tshaj plaws hauv 0.5-1 teev tom qab txhaj tshuaj. Qhov ncauj nws yog metabolized los ntawm daim siab, qhov twg nws yog acylated los yog hydroxylated los tsim cov metabolites sib xws, uas tom qab ntawd tawm hauv lub cev los ntawm ob lub raum los yog kua tsib. Kev txhaj tshuaj ntawm cov khoom yog yooj yim dua metabolized thiab tawm los ntawm lub raum. Feem ntau, cov metabolism thiab tshem tawm cov khoom hauv lub cev yog qhov nrawm, thiab nws ib nrab-lub neej yog nyob nruab nrab ntawm 2-4 teev.
Hauv cov ntsiab lus,Scopolamine butylbromideyog ib qho organic compound nrog cov qauv complex thiab muaj zog biological kev ua si, uas muaj ntau yam anticholinergic teebmeem. Nws cov qauv molecular muaj cov qauv benzyloxycarbonyl thiab carboxylic acid monoester qauv, uas yog lub hauv paus tseem ceeb rau nws cov tshuaj anticholinergic. Nyob rau hauv cov nqe lus ntawm pharmacokinetics, nws muaj zoo bioavailability thiab metabolic teebmeem, thiab yog dav siv nyob rau hauv kev kho mob xyaum.
Cim npe nrov: scopolamine butylbromide cas 149-64-4, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom