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SB-271046 is a potent, selective and orally active antagonist of 5-HT6 receptor (pKi = 8.9 in HeLa cell in vitro)

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]

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