Agomelatine hmoov CAS 138112-76-2

Agomelatine hmoovCov mis mos molecular yog C15H17NO2 thiab txheeb ze molecular loj yog 243.3 g / mol. Nws yog dawb los yog yuav luag dawb crystalline hmoov nrog tshuaj tsw qab. Nws tuaj yeem soluble me ntsis hauv dej thiab yooj yim soluble hauv cov kuab tshuaj organic xws li ethanol, chloroform, dimethyl sulfoxide thiab ethyl acetate. Qhov ze-infrared spectrum qhia tau hais tias nws muaj qhov pom tseeb nqus qhov siab ntawm li 7500 cm-1. Lub melting point yog 106-109 degree C, thiab cov txheej txheem melting yuav raug kuaj los ntawm txawv scanning calorimeter (DSC ). Cov qauv tshuaj zoo feem ntau xav kom cov ntsiab lus impurity tsis pub tshaj 1 feem pua, suav nrog impurities A, B, C, thiab lwm yam, qee qhov yuav muaj kev cuam tshuam tsis zoo rau kev siv tshuaj thiab kev noj qab haus huv ntawm tib neeg. Yog li ntawd, nws cov ntsiab lus purity thiab impurity kuj yog ib qho tseem ceeb ntsuas ntsuas nws qhov zoo. Nws yog ib hom tshuaj antidepressant tshiab. Nws cov txheej txheem ntawm kev ua yog txawv ntawm cov tshuaj serotonin reuptake inhibitor (SSRI) thiab tricyclic antidepressants. Nws txhim kho cov haujlwm ntawm melatonin thiab 5-HT los ntawm kev ua raws li melatonin receptor agonist thiab 5-HT 2C receptor antagonist, yog li ua rau nws cov tshuaj tiv thaiv kev nyuaj siab. Thov nco ntsoov tias cov khoom tsim los ntawm Shaanxi Achieve chem-tech Co., Ltd yog thawj cov khoom siv tshuaj thiab tsuas yog siv rau hauv kev sim.

Agomelatine hmoovmuaj cov kev siv tseem ceeb hauv qab no:

1. Antidepressant nyhuv:

AGOMELATINE, raws li ib qho tshuaj tiv thaiv kev nyuaj siab nrog ob qho tib si tshuaj tiv thaiv kev ntxhov siab thiab kev pw tsaug zog, tau lees paub nws cov tshuaj tiv thaiv kev ntxhov siab tseem ceeb hauv ntau qhov kev sim tshuaj. Txoj kev tshawb no tau pom tias kev kho qhov ncauj nrog AGOMELATINE tau txhim kho cov tsos mob ntawm kev nyuaj siab hauv cov neeg mob piv nrog cov placebo hauv qhov ncauj thiab muaj txiaj ntsig zoo rau cov tshuaj SSRI cov tshuaj tiv thaiv kev ntxhov siab. Tsis tas li ntawd, AGOMELATINE tuaj yeem txhim kho kev pw tsaug zog zoo ntawm cov neeg mob yam tsis muaj kev phiv loj.

2. Txhim kho txoj kev xav tsis zoo:

Inverted mus ob peb vas yog ib qho kev puas siab puas ntsws muaj feem xyuam nrog kev xav ntawm kev xav, uas yog cov tsos mob ntawm kev nyuaj siab thiab hypomania ntawm lub sijhawm sib txawv. AGOMELATINE tau raug pov thawj los txhim kho cov tsos mob ntawm flipped mus ob peb vas thiab yog dav siv nyob rau hauv kev kho mob.

3. Tswj kev pw tsaug zog:

AGOMELATINE kuj tau pom tias muaj kev pw tsaug zog zoo. Thaum kho kev nyuaj siab, AGOMELATINE tuaj yeem txhim kho kev pw tsaug zog zoo thiab txo cov tsos mob ntawm insomnia. Qhov no yog vim nws cov melatonin receptor agonist ua, uas tuaj yeem tswj hwm lub moos lom neeg thiab txhim kho kev pw tsaug zog zoo.

4. Txhim kho vaginitis cov tsos mob:

Cov kev tshawb fawb tsis ntev los no tau pom tias AGOMELATINE tuaj yeem txhim kho cov poj niam leucorrhea, qhov chaw mos noo noo, mob thiab lwm yam tsos mob. AGOMELATINE tuaj yeem ua rau vascular endothelial hlwb, txhim khu kev ua haujlwm ntawm vascular endothelial hlwb, yog li ua kom ntshav txaus thiab txhim kho cov tsos mob ntawm vaginitis.

Ntxiv rau cov kev siv tseem ceeb uas tau hais los saum no, AGOMELATINE kuj tau siv dav hauv qee qhov chaw. Piv txwv li, nws kuj muaj cov txiaj ntsig zoo hauv kev kho mob ntawm kev phobia thiab kev ntxhov siab. Tsis tas li ntawd, AGOMELATINE kuj tseem siv los txhim kho cov tawv nqaij laus, tswj cov ntshav qab zib thiab lipid metabolism, thiab lwm yam, tab sis kev tshawb fawb thiab kev siv hauv cov haujlwm no tseem txuas ntxiv mus.

Hauv cov ntsiab lus, AGOMELATINE, ua ib hom tshuaj tiv thaiv kev ntxhov siab tshiab, tau siv dav hauv kev kho mob, thiab nws cov tshuaj tiv thaiv kev ntxhov siab tseem ceeb thiab kev tswj kev pw tsaug zog tau lees paub. Nws kuj muaj peev xwm txhim kho flipping mus ob peb vas, cov tsos mob ntawm poj niam vaginitis, thiab kev phobia. Nws yog ib qho tseem ceeb heev tshuaj rau nws cov nyhuv curative.

Lub synthesis ntawmAgomelatine hmoovFeem ntau suav nrog plaub theem:

Kauj ruam 1: Synthesis ntawm ethyl 7-hydroxy-6-methoxy-2-phenylpropionate

Qhov no yog ib tug precursor compound rau lub synthesis ntawm AGOMELATINE. Nws txoj kev siv hluavtaws feem ntau yog Barr-Finkler rearrangement cov tshuaj tiv thaiv tau piav qhia hauv kev siv (1). Ua ntej, p-methoxyphenylacetonitrile thiab acetone yog condensed nyob rau hauv lub xub ntiag ntawm catalysts xws li sulfuric acid, glacial acetic acid thiab cuprous chloride kom tau propiophenone. Tom qab ntawd propiophenone yog esterified nrog catalysts xws li benzoic acid thiab methyl diethylthioacetate los npaj ethyl 7-hydroxy-6-methoxy-2-phenylpropionate.

Qhov thib ob theem: Synthesis ntawm 5-bromo-2-nitrophenol

Dissolve 3, 5-dinitrophenol nyob rau hauv hydrochloric acid, thiab ntxiv cov concentrated hydrochloric acid kom yaj tag. Tom qab ntawd, ntawm 0 degree, concentrated sodium bromide aqueous tov tau ntxiv dropwise los tsim 5-bromo-2-nitrophenol.

Kauj ruam 3: Synthesis of AGOMELATINE intermediate

Condensation cov tshuaj tiv thaiv ntawm ethyl 7-hydroxy-6-methoxy-2-phenylpropionate thiab 5-bromo-2-nitrophenol hauv benzene muab compound (1). Tom qab ntawd compound (1) thiab 3-methoxyphenol tau raug rau ntau cov tshuaj tiv thaiv hauv iodobenzene kom thaum kawg tau txais qhov nruab nrab ntawm AGOMELATINE, uas tau hu ua compound (2) ntawm no.

Kauj Ruam 4: Synthesis ntawm AGOMELATINE

Qhov nruab nrab (2) ntawm AGOMELATINE yog cyclized nyob rau hauv catalysis ntawm sulfuryl chloride thiab DMF kom tau AGOMELATINE. Cov kauj ruam no tseem tuaj yeem siv lwm txoj hauv kev, xws li cov txheej txheem npaj tau piav qhia hauv kev siv (2).

Hauv cov ntsiab lus, AGOMELATINE ua tiav los ntawm kev sib txuas 4 intermediates. Qhov twg, 7-hydroxyl-6-methoxyl-2-phenylpropionic acid ethyl ester thiab 5-bromo-2-nitrophenol yog thawj ob intermediates, thiab thib peb intermediate compound (2) , thiab thaum kawg tau AGOMELATINE. Txawm hais tias cov txheej txheem synthesis yog qhov nyuaj, AGOMELATINE tau dhau los ua ib qho ntawm cov tshuaj tseem ceeb rau kev kho kev nyuaj siab vim nws cov tshuaj tiv thaiv kev ntxhov siab tseem ceeb thiab kev tswj kev pw tsaug zog.

Cov qauv molecular ntawmAgomelatine hmoovyog tus cwj pwm los ntawm nws lub peev xwm los ua ib txhij ua ntawm 5-hydroxytryptamine 2C receptors (5-HT2C) thiab melatonin receptors MT1/MT2, nrog rau kev xaiv siab thiab kev sib raug zoo.

Cov tshuaj formula ntawm AGOMELATINE yog C15H17NO2, thiab nws cov qauv muaj ib pab pawg neeg zoo li amphetamine thiab ib tug alkoxy-hloov benzene nplhaib. Qhov hnyav molecular yog 243.3 g / mol. Lub cev thiab tshuaj lom neeg cov khoom ntawm cov tshuaj qhia tias AGOMELATINE tsis yooj yim soluble hauv dej thiab ethanol, tab sis yog yooj yim soluble nyob rau hauv organic solvents xws li dimethyl sulfoxide thiab dichloromethane.

Pharmacologically, AGOMELATINE tuaj yeem ua rau ob qho 5-HT2C thiab MT1 / MT2 receptors. Lub 5-HT2C receptor yog G protein-coupled receptor dav dav nyob rau hauv lub hauv nruab nrab lub paj hlwb thiab yog ze ze rau txoj kev xav thiab kev noj qab haus huv tswj; thaum lub MT1 / MT2 receptor yog lub ntsiab receptor rau melatonin, Nws plays lub luag haujlwm tseem ceeb hauv kev tswj lub moos lom neeg thiab lub voj voog pw tsaug zog, thiab lwm yam.

Hauv cov qauv molecular ntawm AGOMELATINE, pawg amphetamine feem ntau ua rau ntawm 5-HT2C receptor, thiab nws cov nyhuv antagonistic ntawm cov receptor tuaj yeem txo qhov ua kom ntawm 5-HT2C receptor, yog li txhim kho kev xav thiab kev coj cwj pwm txawv txav. Lub alkoxy-hloov benzene nplhaib feem ntau ua rau MT1 / MT2 receptors, uas tuaj yeem khi rau cov receptors thiab simulate cov teebmeem lom ntawm melatonin, yog li tswj kev pw tsaug zog thiab cov moos lom neeg.

Tsis tas li ntawd, cov qauv molecular ntawm AGOMELATINE kuj muaj binary bonds ntawm benzene rings. Cov qauv no ua rau nws muaj kev sib raug zoo rau oxidases, yog li txhim kho kev ruaj ntseg thiab bioavailability ntawm cov tshuaj. Piv nrog rau lwm cov tshuaj tiv thaiv kev nyuaj siab, AGOMELATINE muaj kev xaiv ntau dua thiab muaj kev sib raug zoo, uas tuaj yeem txo qhov cuam tshuam rau lwm cov neurotransmitter receptors, yog li txo cov kev mob tshwm sim thiab kev nyab xeeb.

Hauv kev xaus, cov qauv molecular ntawm AGOMELATINE suav nrog cov pab pawg zoo li amphetamine thiab alkoxy-hloov benzene nplhaib, uas tuaj yeem ua rau tib lub sijhawm ntawm 5-HT2C thiab MT1 / MT2 receptors, nrog kev xaiv siab thiab kev sib raug zoo, thiab muaj zog heev. cuam ​​tshuam rau oxidases. Muaj zog affinity, thiab tuaj yeem txo cov kev mob tshwm sim thiab kev nyab xeeb.

Ntawm no yog cov highlights ntawmAgomelatine hmoov's discovery keeb kwm:

AGOMELATINE yog thawj zaug tsim los ntawm Fabkis lub tuam txhab tshuaj Servier Laboratories hauv xyoo 2001 thiab tau pom zoo rau kev lag luam hauv xyoo 2009. Cov tshuaj no yog lub npe hu ua S-20098, thiab hauv kev tshawb fawb thiab kev loj hlob ntxiv, lub npe lag luam AGOMELATINE tau txiav txim siab thaum kawg.

Qhov kev tshawb pom ntawm AGOMELATINE yog ze ze rau nws cov txheej txheem ntawm kev ua. Hauv xyoo 1980s, melatonin, uas yog ib qho tseem ceeb ntawm cov tshuaj lom neeg endogenous, tau nyiam cov kws tshawb fawb. Cov kev tshawb fawb tau pom tias melatonin tuaj yeem tswj tsis tau tsuas yog tswj lub cev lub moos lom neeg thiab lub voj voog pw tsaug zog, tab sis kuj muaj qee yam cuam tshuam rau kev xav thiab qhov tshwm sim ntawm kev nyuaj siab. Qhov no txhawb cov kws tshawb fawb los nrhiav cov hom phiaj molecular uas muaj ob qho tib si tshuaj tiv thaiv kev ntxhov siab thiab txhim kho kev pw tsaug zog zoo rau kev kho mob antidepressant.

Nyob rau hauv cov ntsiab lus no, Servier Laboratories pib kawm melatonin mimics nyob rau hauv 1990 thiab nrhiav tau lub molecule AGOMELATINE nyob rau hauv 1999. Cov qauv ntawm AGOMELATINE muaj ob qho tib si 5-hydroxytryptamine 2C receptor (5-HT2C) antagonist thiab melatonin, thiab receptors. muaj siab selectivity. Cov qauv no tseem txhim kho nws cov kev ua tau zoo hauv kev txhim kho kev xav thiab kev pw tsaug zog zoo, ua rau nws yog ib hom tshuaj tshiab rau kev kho kev nyuaj siab.

Cov kev sim tshuaj ntsuam xyuas ntawm AGOMELATINE kuj tau lees paub nws cov tshuaj tiv thaiv kev ntxhov siab tseem ceeb. Hauv kev sib piv ntau qhov sib piv ntawm 520 cov neeg mob uas muaj kev nyuaj siab, AGOMELATINE tau muab piv rau cov tshuaj tiv thaiv kev ntxhov siab SSRI hauv kev txhim kho cov tsos mob kev nyuaj siab yam tsis muaj kev phiv loj. Cov txiaj ntsig zoo li no ua rau AGOMELATINE yog ib qho ntawm cov tshuaj tseem ceeb rau kev kho kev nyuaj siab.

Nyob rau hauv kev kho mob daim ntawv thov ntawm AGOMELATINE, ntxiv rau nws cov nyhuv antidepressant, nws kuj tau raug pov thawj los txhim kho flipping mus ob peb vas, kev phobia, poj niam vaginitis tsos mob, thiab lwm yam., thiab nws muaj peev xwm tswj lub sij hawm lom, txhim kho daim tawv nqaij laus, tswj cov ntshav qab zib thiab lipid metabolism, thiab lwm yam. Ob leeg muaj peev xwm zoo. Yog li ntawd, qhov kev tshawb pom ntawm AGOMELATINE tsis tsuas yog txhawb txoj kev loj hlob ntawm cov tshuaj tiv thaiv kev ntxhov siab, tab sis kuj muab cov tswv yim tshiab rau kev tshawb fawb hauv lwm qhov chaw.

Hauv cov ntsiab lus, AGOMELATINE yog cov tshuaj tiv thaiv kev ntxhov siab tshiab tsim los ntawm Servier Laboratories hauv xyoo 2001. Nws cov txheej txheem tshawb pom tau tshwm sim los ntawm kev tshawb fawb ntawm melatonin, ua ke nrog cov yam ntxwv ntawm 5-HT2C receptor antagonist thiab melatonin receptor agonist, nws muaj cov tshuaj tiv thaiv kev ntxhov siab tseem ceeb thiab Kev tswj kev pw tsaug zog, thiab tau dhau los ua ib qho tshuaj tseem ceeb rau kev kho mob antidepressant ib qho.

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