| 货号 | 18513-50mg |
| 描述 | SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) 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 |
| 供应商 | Cayman |
| 应用文献 | |
| 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 antagonist. Journal of Medicinal Chemistry 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 antagonist. British Journal of Pharmacology 130, 1606-1612 (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 aspartate. Brit.J.Pharmacol. 130, 23-26 (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 mechanisms. Brit.J.Pharmacol. 167, 436-449 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 488.4 |
| 分子式 | C20H22CIN3O3S2 • HCl |
| CAS号 | 209481-24-3 |
| 稳定性 | ≥ 2 years |
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