An orally-available 5-HT6 antagonist
SB-271046 is an orally-available antagonist of the serotonin receptor 5-HT6 (pKi = 9.02-8.92).1,2 It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.2 While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.3 It has been used to evaluate the role of 5-HT6 in learning and memory.4
1.Bromidge, S.M., Brown, A.M., Clarke, S.E., 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 antagonistJ. Med. Chem.42(2)202-205(1999) 2.Routledge, C., Bromidge, S.M., Moss, S.F., et al.Characterization of SB-271046: A potent, selective and orally active 5-HT6 receptor antagonistBr. J. Pharmacol.1301606-1612(2000) 3.Dawson, L.A., Nguyen, H.Q., and Li, P.In vivo effects of the 5-HT(6) antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartateBr. J. Pharmacol.13023-26(2000) 4.Woods, S., Clarke, N.N., Layfield, R., et al.5-HT(6) receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanismsBr. J. Pharmacol.167436-449(2012)
动态评分
0.0