SB271046

Names

[ CAS No. ]:
209481-20-9

[ Name ]:
SB271046

[Synonym ]:
5-Chloro-N-[4-methoxy-3-(piperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride (1:1)
Benzo[b]thiophene-2-sulfonamide, 5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-, hydrochloride (1:1)
5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride (1:1)
Benzo[b]thiophene-2-sulfonamide (5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl
SB271046

Biological Activity

[Description]:

SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT6 Receptor:8.92-9.09 (pKi)

[In Vitro]

In functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71[1].

[In Vivo]

SB 271046 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. 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 Cmax[1].

[References]

[1]. C Routledge, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000 Aug;130(7):1606-12.

Chemical & Physical Properties

[ Density]:
1.400

[ Boiling Point ]:
664.3ºC at 760 mmHg

[ Melting Point ]:
240-241℃ (DEC.)

[ Molecular Formula ]:
C₂₀H₂₃Cl₂N₃O₃S₂

[ Molecular Weight ]:
488.45100

[ Flash Point ]:
355.5ºC

[ Exact Mass ]:
487.05600

[ PSA ]:
107.29000

[ LogP ]:
6.43170

[ Storage condition ]:
Desiccate at RT

Related Compounds

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