Agomelatine

Tlhaloso e Khutšoanyane:

Agomelatine ke mofuta o mocha oa antidepressant. Mokhoa oa eona oa ts'ebetso o phunyeha ka mokhoa o tloaelehileng oa monoamine transmitter system.Agomelatine ke melatoninergic agonist le mohanyetsi ea khethiloeng oa li-receptor tsa 5-HT2C, 'me e bontšitsoe hore e sebetsa ka mafolofolo liphoofolong tse ngata tsa ho tepella maikutlong. Agomelatine (S20098) e bonts'itse litekanyetso tsa pKi tsa 6.4 le 6.2 ho li-receptor tsa tlhaho (porcine) le tse entsoeng ka batho (h) 5-hydroxytryptamine (5-HT)2C receptors, ka ho latellana.

Agomelatine ke mofuta o le mong oa phofo e tšoeu kapa e tšoeu ea kristale kapa e tiileng e tšoeu. Lebitso la IUPAC la k'hemik'hale ena ke N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide. K'hemik'hale ena ke ea Aromatics Compounds;Aromatics;Neurochemicals;APIS. E lokela ho bolokoa ho -20°C Freezer.


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  • Matla a Phepelo:10000 KG/Kgwedi
  • Boema-kepe:Shanghai / Beijing
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  • Lintlha tsa Sehlahisoa

    Li-tag tsa Sehlahisoa

    Lebitso la Sehlahisoa:Agomelatine

    Lebitso le Leng:N-[2-(7-Methoxy-1-naphthyl)ethyl]acetamide;N-[2-(7methoxynaphthalen-1-yl)ethyl]acetamide

    Nomoro ea CAS:138112-76-2

    Litlhaloso: 99.0%

    'Mala: Phofo e tšoeu e nang le monko le tatso e ikhethang

    Boemo ba GMO:GMO Mahala

    Ho paka: ka meqomo ea fiber ea 25kgs

    Polokelo: Boloka setshelo se sa buloa sebakeng se phodileng, se omileng, Qoba hole le leseli le matla

    Shelf Life: Likhoeli tse 24 ho tloha ka letsatsi la tlhahiso

    AgomelatineTlhaloso ea Sehlahisoa

    1. Tlhaloso ea Sehlahisoa
    Agomelatine ke novel antidepressant e nang le mekhoa e 'meli e ikhethang ea ketso: e sebetsa e le melatonin receptor agonist (MT1/MT2) le mohanyetsi oa 5-HT2C receptor**. Lebitso la eona la lik'hemik'hale keN-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, ka foromo ea molek'hule C₁₅H₁₇NO₂ le nomoro ea CAS138112-76-2. E fumaneha ka mokhoa oa phofo kapa oa letlapa (25 mg letlapa ka leng), e hloekile haholo (≥98% ka HPLC) 'me e qhibiliha ka har'a metsoako ea tlhaho e kang DMSO le ethanol.

    2. Lipontšo
    Agomelatine e bontšoa bakeng sa phekolo ea boloetse bo tebileng ba ho tepella maikutlo (MDD) ho batho ba baholo, haholo-holo ho bakuli ba sa mamelleng li-antidepressants tse tloaelehileng kapa ba nang le ho tšoenyeha ho bakoang ke ho sithabela maikutlong kapa ho robala. Liteko tsa bongaka li bonts'a katleho ea ho ntlafatsa matšoao a tepeletseng maikutlo, taolo ea morethetho oa circadian, le ts'ebetso ea mots'eare.

    3. Mokhoa oa ho Etsa

    • MT1/MT2 Agonism: E khutlisetsa morethetho oa circadian ka ho etsisa melatonin, ho ntlafatsa boleng ba boroko le ho falimeha ha motšehare**.
    • 5-HT2C Antagonism: E eketsa tokollo ea dopamine le norepinephrine ka har'a prefrontal cortex, e fokotsa matšoao a khatello ea maikutlo.
      Ketso ena e habeli e khetholla Agomelatine ho SSRIs/SNRIs, e fana ka boemo bo botle ba mamello.

    4. Tekanyo le Tsamaiso

    • Tekanyetso e khothalletsoang: 25-50 mg hang ka letsatsi pele ho robala **.
    • Pharmacokinetics: ho kenngoa ka potlako (sehlohlolong sa plasma nakong ea lihora tse 2), metabolized ka CYP1A2, 'me e ntšoa ka renal **.

    5. Katleho ea Bongaka

    • Bokaholimo ho Taolo ea Circadian: Agomelatine e ntlafatsa haholo latency ea boroko le katleho ha e bapisoa le sertraline, e nang le litlamorao tse bonoang pele ho Beke ea 1 **.
    • Melemo ea nako e telele: E boloka tšoarelo ho MDD ho feta selemo sa 1, ka litekanyetso tse fokolang tsa ho khutlela morao le ho khaotsa ho fokolang ka lebaka la liphello tse mpe **.
    • Matšoenyeho le Mosebetsi: E fokotsa matšoao a ho tšoenyeha le ho ntlafatsa mosebetsi, boiketlo ba sechaba, le ts'ebetso ea lelapa**.

    6. Polokeho le Mamello

    • Litla-morao tse Tloaelehileng: Ho opeloa ke hlooho, nasopharyngitis, le tšitiso e fokolang ea mala **.
    • Boemo ba Polokeho: Ha ho na boima ba 'mele, ho se sebetse hantle ka thobalano, kapa matšoao a ho tlohela, a ikamahanyang le khetho ea eona ea ho amohela**.
    • Tlhokomeliso ea Tikoloho: E khethiloe e le chefo ea metsing (WGK 3); qoba ho pepesehela tikoloho ka kotloloho**.

    7. Ho boloka le ho Tšoara

    • Polokelo: Boloka ho 2–8°C (phofo) kapa mocheso oa kamore (matlapa a ka har’a sephutheloana sa pele)**.
    • Botsitso: E tsitsitse ka lilemo tse ≥2 ha e sirelelitsoe leseli le mongobo **.

    8. Boemo ba Taolo

    • E amohetsoe ho EU, Australia, le limmarakeng tse ling tlasa mabitso a marang-rang joalo kaValdoxan®**.
    • E thathamisitsoe ho WHO International Nonproprietary Names (INN) le FDA Preferred Term databases**.

    9. Likopo tsa Lipatlisiso
    Agomelatine e boetse e sebelisoa lithutong tsa preclinical bakeng sa neuroprotection, tau protein phosphorylation, le pontšo ea calcium ho li-neurone. Litekanyetso tsa litšupiso (mohlala, litšila, metabolites) li teng bakeng sa nts'etsopele ea meriana le taolo ea boleng.

    Mantsoe a sehlooho :Agmelatine, MT1/MT2 agonist, mohanyetsi oa 5-HT2C, bothata bo boholo ba ho tepella maikutlo, morethetho oa circadian, Valdoxan, katleho ea ho imeloa kelellong, serotonin receptor, melatonin analog.


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