3-Hydroxy agomelatine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

3-Hydroxy agomelatine 是 Agomelatine 的代谢产物。3-Hydroxy agomelatine 是 5-HT2C 受体拮抗剂，IC50 为 3.2 μM，Ki 为 1.8 μM。

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.

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.

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.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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166526-99-4

259.3

C15H17NO3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (964.13 mM; 超声助溶 )

COc1ccc2cc(O)cc(CCNC(C)=O)c2c1

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(-20℃)

With Ice Pack

≥ 2 years