SB 271046 hydrochloride

Biological Activity

SB 271046 hydrochloride is a selective, orally active 5-HT₆ antagonist (pK_i 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-HT_1D, 5-HT_1A, D₃, 5-HT_1B, 5-HT_1F, α_1B, 5-HT_2C, 5-HT_2A, D₂, 5-HT_2B, 5-HT₇, 5-HT₄ and 5-HT_1E 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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

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, DA, 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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