Bioactivity | 5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs[1]. |
In Vivo | 5-HT1AR agonist 1 (2.5 MG/ KG, I.V. and 10 MG / KG, P.O.) 在小鼠中表现出优秀的口服生物利用度和低清除率[1]。5-HT1AR agonist 1 (30 MG/KG, i.p., 30 min) 在小鼠强迫游泳测试中展示了强大的抗抑郁潜力,类似于 Vilazodone (HY-14262) 的效果[1]。5-HT1AR agonist 1在ICR小鼠体内药动学参数[1]药代动力学分析[1]Route |
Formula | C24H26N4O3 |
Molar Mass | 418.49 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zheng J, et al. Synthesis and biological evaluation of multimodal monoaminergic arylpiperazine derivatives with potential antidepressant profile[J]. Eur J Med Chem. 2024 Jun 3;275:116564. |