Agomelatine

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Agomelatine jẹ agonist ti awọn olugba melatonin ati antagonist ti olugba 5-HT2C serotonin pẹlu awọn iye Ki ti 0.062nM ati 0.268nM ati iye IC50 ti 0.27μM, lẹsẹsẹ fun MT1, MT2 ati 5-HT2C [1].

Agomelatine jẹ oogun apakokoro alailẹgbẹ ati pe o ni idagbasoke fun itọju ailera aibalẹ nla (MDD).Agomelatine jẹ yiyan lodi si 5-HT2C.O ṣe afihan awọn ibatan kekere si ẹda oniye 5-HT2A ati 5-HT1A.Fun awọn olugba melatonin, agomelatine ṣe afihan awọn ibatan ti o jọra si MT1 eniyan ti o ni ẹda ati MT2 pẹlu awọn iye Ki ti 0.09nM ati 0.263nM, lẹsẹsẹ.Ninu awọn ẹkọ in vivo, agomelatine fa ilosoke ti dopamine ati awọn ipele noradrenaline nipasẹ didi igbewọle inhibitory ti 5-HT2C.Pẹlupẹlu, iṣakoso ti agomelatine ṣe ilodisi idinku ti aapọn ti o fa ni agbara sucrose ni awoṣe eku ti ibanujẹ.Yato si iyẹn, agomelatine n ṣiṣẹ idinku ipa aibalẹ ni awoṣe rodent ti aibalẹ [1].

Awọn itọkasi:
[1] Zupancic M, Guilleminault C. Agomelatine.CNS oloro, 2006, 20 (12): 981-992.

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Agomelatine

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2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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