SB 271046 hydrochloride

Product Description

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).

Licensing Information

Sold with the permission of GlaxoSmithKline

Solubility

Preparing Stock Solutions for SB 271046 hydrochloride

The following data is based on the product molecular weight 488.45

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.05 mL	10.24 mL	20.47 mL
5 mM	0.41 mL	2.05 mL	4.09 mL
10 mM	0.20 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Marcos Effects of 5-HT₆ receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br.J.Pharmacol. 2008 PMID: 18622410
• Dawson 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. Br.J.Pharmacol. 2000 PMID: 10780993
• Routledge Characterization of SB-271046: a potent, selective and orally active 5-HT₆ receptor antagonist. Br.J.Pharmacol. 2000 PMID: 10928964
• Bromidge 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. 1999 PMID: 9925723