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  • 5HT6-ligand-1
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5HT6-ligand-1

5HT6-ligand-1是有效的5-HT6受体配体,与其结合的Ki值为1.43nM。

原价
¥2150-12712
价格
1720-10170
5HT6-ligand-1的二维码

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  • 货号: ajce46834
  • CAS: 1038988-11-2
  • 别名:
  • 分子式: C20H22BrN3O2S
  • 分子量: 448.38
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM.


5HT6-ligand-1 is extensively metabolized in rat liver microsomes whereas in human liver microsomes, 5HT6-ligand-1 is extensively metabolized (90%). The IC50 values for 5HT6-ligand-1 at CYP 3A4 is 35.97%, whereas the IC50 values at CYP 2D6 enzymes is less than 20 μM. 5HT6-ligand-1 at an oral dose of 10 mg/kg is rapidly absorbed in rats with a good oral half-life of 3.17±0.49 h with an oral bioavailability of 29±5%. The observed oral Cmax is 60±44 ng/mL and occurs at 1.83 h. 5HT6-ligand-1 displays an oral exposure of 217±92 ng h/mL. It has a clearance of 220±92 mL/min/kg with a volume of distribution of 32.6±10.7 L/kg for iv dose. Extensive rat metabolism coupled with high clearance could be the possible reason for moderate oral bioavailability showed by 5HT6-ligand-1. Oral administration of 5HT6-ligand-1 reverses the time delay induced memory deficit and statistically significant effect is observed at a dose of 10 mg/kg indicating cognitive improvement potential of the compound 6a[1].


[1]. Nirogi RVS, et al. Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands. Bioorg Med Chem Lett 22 (2012) 7431-7435

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