209481-20-9

209481-20-9 structure

Name: SB271046
Chemical Name: SB 271046 hydrochloride
CAS Number: 209481-20-9
Molecular Formula: C₂₀H₂₃Cl₂N₃O₃S₂
Molecular Weight: 488.45100
Catalog: Biochemical Inhibitor Neuronal Signaling 5-HT Receptor Antagonist
Create Date: 2019-01-01 13:21:06
Modify Date: 2024-01-12 00:02:32
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].

Name	SB 271046 hydrochloride
Synonyms	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

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.