Kāpae

ʻO Agomelatine kahi agonist o nā melatonin receptors a me kahi antagonist o ka serotonin 5-HT2C receptor me nā helu Ki o 0.062nM a me 0.268nM a me IC50 waiwai o 0.27μM, kēlā me kēia no MT1, MT2 a me 5-HT2C [1].

He antidepressant kū hoʻokahi ʻo Agomelatine a ua hoʻomohala ʻia no ka mālama ʻana i ka maʻi depressive nui (MDD). Ua koho ʻo Agomelatine i ka 5-HT2C. Hōʻike ia i nā haʻahaʻa haʻahaʻa i ka cloned kanaka 5-HT2A a me 5-HT1A. No nā mea loaʻa melatonin, hōʻike ʻo agomelatine i nā pilina like me ka cloned kanaka MT1 a me MT2 me nā helu Ki o 0.09nM a me 0.263nM, kēlā me kēia. Ma nā haʻawina in vivo, ʻo agomelatine ka mea e hoʻonui ai i nā pae dopamine a me nā noradrenaline ma o ka pale ʻana i ka hoʻokomo inhibitory o 5-HT2C. Eia kekahi, ʻo ka hoʻokele ʻana o agomelatine e kūʻē i ka emi ʻana o ke koʻikoʻi i ka hoʻohana ʻana i ka sucrose i kahi ʻano ʻiole o ke kaumaha. Ma waho aʻe o kēlā, hoʻohana ʻo agomelatine i ka hoʻohaʻahaʻa ʻana i ka manaʻo hopohopo i kahi hoʻohālike rodent o ka hopohopo [1].

Kuhikuhi:
[1] Zupancic M, Guilleminault C. Agomelatine. Nā lāʻau lapaʻau CNS, 2006, 20 (12): 981-992.

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