SB 271046 hydrochloride

Short Summary : Selective 5-HT6 antagonist

Category : Neuroscience|5-HT Receptor

Purity : 0.98

CAS Number : 209481-24-3

Formula : C20H23Cl2N3O3S2

Molecular Weight : 488.45

SMILE : CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4.Cl

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : SB 271046 hydrochloride is a potent, selective and orally active antagonist of 5-HT6 receptor (pKi = 8.9 in HeLa cell in vitro). SB 271046 hydrochloride is a hydrochloride salt form of SB 271046. 5-HT receptor is a G-protein coupled receptor for 5-hydroxytryptamine (serotonin) that found in nerve systems. It also functions as receptor for various alkaloids and psychoactive substances. In native brain tissue, SB-271046 exhibits high affinity for human recombinant 5-HT6 receptors and 5-HT6 receptors. SB-271046 has a 200 fold greater selectivity over all other 5-HT receptors subtypes tested. [1] In rat MEST (maximal electroshock seizure threshold) test, SB-271046 increases the seizure threshold over a wide range of dose with a minimum effective dose of 40.1 mg kg71 p.o. and maximum effect at 4 h post-dose. [1] In rat Morris water maze that measuring behavior acquisition and retention, galanthamine and SB-271046 combined treatment reverses the scopolamine- or MK-801-induced learning impairments. [2]References: 1. Routledge C, Bromidge SM, Moss SF et al. Characterization of SB-271046: a potent, selective and orally active 5-HT (6) receptor antagonist. Br J Pharmacol. 2000 Aug; 130(7):1606-12.2. Marcos B, Chuang TT, Gil-Bea FJ, Ramirez MJ. Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br J Pharmacol. 2008 Oct;155(3):434-40.

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