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- 5-HT Receptor
- 3-Hydroxy agomelatine
3-Hydroxy agomelatine
3-Hydroxyagomelatine是Agomelatine的代谢产物。3-Hydroxyagomelatine是5-HT2C受体拮抗剂，IC50为3.2μM，Ki为1.8μM。
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包装价格促销价数量
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5mg￥1850.001480.00- +
- 货号: ajcx29996
- CAS: 166526-99-4
- 别名: 阿戈美拉汀杂质
- 分子式: C15H17NO3
- 分子量: 259.3
- 纯度: ＞98%
- 溶解度:
- 储存: Store at -20°C
- 库存: 现货
Background
3-Hydroxy agomelatine is a metabolite of Agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM[1].
Agomelatine and S 21517 have moderately high affinities for 5-HT2C receptors (Ki = 0.21 μM and 0.13 μM, respectively). The metabolite 3-Hydroxy agomelatine (S 21540) has a 10-fold lower affinity (Ki = 1.8 μM). Agomelatine, S 21517 and 3-Hydroxy agomelatine (10-7-10-4 M) are antagonists at 5-HT2C receptors, with a rank order of efficacy as follows: S 21517>Agomelatine>3-Hydroxy agomelatine[1].
Increasing doses (from 1.25 to 40 mg/kg, intraperitoneal injection) of 3-Hydroxy agomelatine (S 21540) does not affect the penile erections induced by mCPP and Ro 60-0175 in Wistar rat[1].
[1]. Chagraoui A, et al. Agomelatine(S 20098) antagonizes the penile erections induced by the stimulation of 5-HT2C receptors in Wistar rats. Psychopharmacology (Berl). 2003 Oct;170(1):17-22.
