5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride

Uses

5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophene-2-sulfonamide Hydrochloride is a 5-Hydroxytryptamine6 receptor antagonist.

Biological Activity

The first potent and selective 5-HT6 antagonist. Training in cognitive tasks, as well as administration SB-271046, induces an increase in pERK1/2 and pCREB1 levels, while CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2, not pCREB1/2. SB-271046 reverses MK-801-induced, but not scopolamine-induced, learning impairments. However, with coadministration of galanthamine, both types of learning impairments were ameliorated.

in vivo

IC 50

5-HT₆ Receptor: 8.92-9.02 (pKi); 5-HT_1D Receptor: 6.55 (pKi); 5-HT_1A Receptor: 6.35 (pKi); 5-HT_1B Receptor: 6.05 (pKi); 5-HT_1F Receptor: 5.95 (pKi); 5-HT_2A Receptor: 5.62 (pKi); 5-HT_2B Receptor: 5.41 (pKi); 5-HT₇ Receptor: 5.39 (pKi); 5-HT₄ Receptor: 5.27 (pKi); 5-HT_1E Receptor: <4.99 (pKi); Human 5-HT_2C Receptor: 5.73 (pKi)

storage

Desiccate at RT