Catalog Number: 3368
Chemical Name: 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophen-2-sulfonamide hydrochloride
Biological Activity
Selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).
Technical Data
  • M.Wt:
    488.45
  • Formula:
    C20H22ClN3O3S2.HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    209481-24-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
Background References
  1. 5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
    Bromidge et al.
    J.Med.Chem., 1999;42:202
  2. In vivo effects of the 5-HT6 antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartate.
    Dawson et al.
    Br.J.Pharmacol., 2000;130:23
  3. Characterization of SB-271046: a potent, selective and orally active 5-HT6 receptor antagonist.
    Routledge et al.
    Br.J.Pharmacol., 2000;130:1606
  4. Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat.
    Marcos et al.
    Br.J.Pharmacol., 2008;155:434

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