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SB-271046

Chemical Structure : SB-271046

CAS No.: 209481-20-9

SB-271046 (SB271046)

Catalog No.: PC-21121Not For Human Use, Lab Use Only.

SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist, potently displaces [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT6 receptors recombinantly expressed in HeLa cells with pKi 8.92 and 9.09 respectively.

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Biological Activity

SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist, potently displaces [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT6 receptors recombinantly expressed in HeLa cells with pKi 8.92 and 9.09 respectively.
SB-271046 also displaces [(125)I]-SB-258585 from human caudate putamen and rat and pig striatum membranes (pK(i) 8.81, 9.02 and 8.55 respectively).
SB-271046 is >200 fold selective for the 5-HT(6) receptor vs. 55 other receptors, binding sites and ion channels.
SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA(2) of 8.71 in functional studies on human 5-HT(6) receptors.
SB-271046 (10 mg/kg) demonstrates anticonvulsant activity in the rat MEST test.

Physicochemical Properties

M.Wt 488.44
Formula C20H23Cl2N3O3S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-Chloro-3-methyl-benzo[b]thiophene-2-sulphonic acid (4-methoxy-3-piperazin-1-yl-phenyl)-amide monohydrochloride

References

1. C Routledge, et al. Br J Pharmacol. 2000 Aug;130(7):1606-12.

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