Agomelatine

A melatonin receptor agonist and 5-HT2B and 5-HT2C antagonist

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥437.00

350.00

- +
10mg

￥650.00

520.00

- +
50mg

￥1912.00

1530.00

- +
100mg

￥2787.00

2230.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

Background

Agomelatine is an agonist of melatonin receptors and an antagonist of the serotonin 5-HT2C receptor with Ki values of 0.062nM and 0.268nM and IC50 value of 0.27μM, respectively for MT1, MT2 and 5-HT2C [1].

Agomelatine is a unique antidepressant and is developed for treatment of major depressive disorder (MDD). Agomelatine is selective against 5-HT2C. It shows low affinities to cloned human 5-HT2A and 5-HT1A. For melatonin receptors, agomelatine shows similar affinities to cloned human MT1 and MT2 with Ki values of 0.09nM and 0.263nM, respectively. In the in vivo studies, agomelatine causes increase of dopamine and noradrenaline levels via blocking the inhibitory input of 5-HT2C. Moreover, the administration of agomelatine counteractes the stress-induced decrease in sucrose consumption in a rat model of depression. Besides that, agomelatine exerts alleviated anxiety efficacy in a rodent model of anxiety [1].

参考文献:
[1] Zupancic M, Guilleminault C. Agomelatine. CNS drugs, 2006, 20(12): 981-992.