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SB 271046 hydrochloride

Cat No. 3368

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Chemical Name: 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl -benzo[b]thiophen-2-sulfonamide hydrochloride

Biological Activity

Orally active, selective 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).

Licensing Information

Sold with the permission of GlaxoSmithKline.

Technical Data

M.Wt:

488.45

Formula:

C₂₀H₂₂CIN₃O₃S₂.HCl

Solubility:

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Purity:

>99 %

Storage:

Desiccate at RT

CAS No:

[209481-20-9]

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

Bromidge et al (1999) 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. J.Med.Chem. 42 202. Dawson et al (2000) 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. Br.J.Pharmacol. 130 23. Routledge et al (2000) Characterization of SB-271046: a potent, selective and orally active 5-HT₆ receptor antagonist. Br.J.Pharmacol. 130 1606. Marcos et al (2008) Effects of 5-HT₆ receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br.J.Pharmacol. 155 434.

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Keywords: SB 271046 hydrochloride, Orally, active, selective, 5-HT6, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB271046, hydrochloride, GlaxoSmithKline

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