SB 271046 Hydrochloride

An orally-available 5-HT6 antagonist

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10mg

￥1175.00

940.00

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50mg

￥4412.00

3530.00

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100mg

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200mg

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货号: ajce59436
CAS: 209481-24-3
别名: 5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[B]噻吩-2-磺酰胺盐酸盐,SB 271046A
分子式: C20H23Cl2N3O3S2
分子量: 488.45
纯度: >98%
溶解度: DMSO: 50 mg/mL (102.36 mM)
储存: Store at -20°C
库存: 现货

Background

SB-271046 is an orally-available antagonist of the serotonin receptor 5-HT₆ (pK_i = 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)