1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-
- Product Name
- 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-
- CAS No.
- 1038988-11-2
- Chemical Name
- 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-
- Synonyms
- 5HT6-ligand-1;5HT6 ligand 1,5HT-6-ligand-1,5HT6ligand1;1-(2-bromobenzenesulfonyl)-4-(4-methylpiperazin-1-ylmethyl)-1H-indole;1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-
- CBNumber
- CB73339548
- Molecular Formula
- C20H22BrN3O2S
- Formula Weight
- 448.38
- MOL File
- 1038988-11-2.mol
1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Property
- Boiling point:
- 587.1±60.0 °C(Predicted)
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 7.57±0.10(Predicted)
1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Chemical Properties,Usage,Production
Uses
5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM.
in vivo
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].
IC 50
5-HT6 Receptor: 1.43 nM (Ki)
References
[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
1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Suppliers
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