Potent and selective 5-HT6 receptor antagonist (Ki = 1-2 nM). Displays >200-fold selectivity for 5-HT6 receptors (vs. other receptor binding sites and ion channels). Poor penetration of the blood-brain barrier. Nootropic effects in vivo.
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM and in ethanol to 5 mM (with heating)
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Da Silva Costa-Aze V et al. Serotonin 5-HT6 receptor blockade reverses the age-related deficits of recognition memory and working memory in mice. Behav Brain Res222:134-40 (2011).
Read more (PubMed: 21443908) »
Routledge C et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol130:1606-12 (2000).
Read more (PubMed: 10928964) »
Bromidge SM et al. 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J Med Chem42:202-5 (1999).
Read more (PubMed: 9925723) »