2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Vortioxetine Hcl (Lu AA21004 Hcl) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.in vitro: Compound 5m (Lu AA21004) was the lead compound, displaying high affinity for recombinant human 5-HT(1A) (K(i) = 15 nM), 5-HT(1B) (K(i) = 33 nM), 5-HT(3A) (K(i) = 3.7 nM), 5-HT(7) (K(i) = 19 nM), and noradrenergic β(1) (K(i) = 46 nM) receptors, and SERT (K(i) = 1.6 nM). Compound 5m displayed antagonistic properties at 5-HT(3A) and 5-HT(7) receptors, partial agonist properties at 5-HT(1B) receptors, agonistic properties at 5-HT(1A) receptors, and potent inhibition of SERT. Lu AA21004 is a partial h5-HT1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Lu AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay.
in vivo: Lu AA21004 occupies the r5-HT(1B) receptor and rSERT (ED(50) = 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT(3) receptor antagonist in the Bezold-Jarisch reflex assay (ED(50) = 0.11 mg/kg s.c.). Vortioxetine significantly increased cell proliferation and cell survival and stimulated maturation of immature granule cells in the subgranular zone of the dentate gyrus of the hippocampus after 21 days of treatment. Vortioxetine did not cause cognitive or psychomotor impairment. Subjects were randomized (1:1) to receive vortioxetine 5mg (n=152) or placebo (n=152) for 8 weeks. Efficacy was assessed using change from baseline in HAM-A total scores after 8 weeks of treatment compared with placebo, using mixed-model repeated measures (MMRM) analyses. For the detailed information of Vortioxetine hydrobromide, the solubility of Vortioxetine hydrobromide in water, the solubility of Vortioxetine hydrobromide in DMSO, the solubility of Vortioxetine hydrobromide in PBS buffer, the animal experiment (test) of Vortioxetine hydrobromide, the cell expriment (test) of Vortioxetine hydrobromide, the in vivo, in vitro and clinical trial test of Vortioxetine hydrobromide, the EC50, IC50,and affinity,of Vortioxetine hydrobromide, For the detailed information of Vortioxetine hydrobromide, the solubility of Vortioxetine hydrobromide in water, the solubility of Vortioxetine hydrobromide in DMSO, the solubility of Vortioxetine hydrobromide in PBS buffer, the animal experiment (test) of Vortioxetine hydrobromide, the cell expriment (test) of Vortioxetine hydrobromide, the in vivo, in vitro and clinical trial test of Vortioxetine hydrobromide, the EC50, IC50,and affinity,of Vortioxetine hydrobromide, Please contact DC Chemicals.
