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

Product Name5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride
CAS209481-24-3
MFC20H23Cl2N3O3S2
MW488.44
EINECS
MOL File209481-24-3.mol

Chemical Properties

storage temp.	2-8°C
solubility	DMSO: >20mg/mL
form	powder
color	White to light brown

Safety Information

WGK Germany

nwg

Usage And Synthesis

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

SB 271046 Hydrochloride (10?mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ?0.1?mg/kg p.o. and maximum effect at 4?h post-dose^[1].

Animal Model:	Male Sprague Dawley rats^[1]
Dosage:	10?mg/kg
Administration:	P.o.
Result:	Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ?0.1?mg?kg?1 p.o. and maximum effect at 4?h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC₅₀ of 0.16?μM) and brain concentrations of 0.01-0.04?μM at C_max.

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

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