3-Hydroxy agomelatine

SKU: orb2901847

Description

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.

Key Properties

• CAS Number: 166526-99-4
• MW: 259.3
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₇NO₃
• SMILES: COc1ccc2cc(O)cc(CCNC(C)=O)c2c1
• Target: 5-HT Receptor
• Solubility: In Vitro: DMSO : 250 mg/mL (964.13 mM; Ultrasonic )

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor