货号 | 10096-1mg |
描述 | Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.1,2In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.1 SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.3,4,5 |
供应商 | Cayman |
应用文献 | |
1.Kennett, G.A.,Wood, M.D.,Bright, F., et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology 36(4/5), 609-620 (1997). 2.Bromidge, S.M.,Duckworth, M.,Forbes, I.T., et al. 6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-indoline (SB-242084): The first selective and brain penetrant 5-HT2C receptor antagonist. Journal of Medicinal Chemistry 40, 3494-3496 (1997). 3.Fletcher, P.J.,Tampakeras, M.,Sinyard, J., et al. Characterizing the effects of 5-HT2C receptor ligands on motor activity and feeding behaviour in 5-HT2C receptor knockout mice. Neuropharmacology 57, 259-267 (2009). 4.Fletcher, P.J.,Sinyard, J. and Higgins, G.A. The effects of the 5-HT2C receptor antagonist SB242084 on locomotor activity induced by selective, or mixed, indirect serotonergic and dopaminergic agonists. Psychopharmacology 187, 515-525 (2006). 5.Dalton, G.L.,Lee, M.D.,Kennett, G.A., et al. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology 185, 45-47 (2006). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 467.8 |
分子式 | C21H19ClN4O2 • 2HCl |
CAS号 | 1049747-87-6 |
稳定性 | ≥ 2 years |
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