货号 | 4317/50 |
别名 | N-(2,4-Dibromophenyl)-N'-[(4S,5S)-2, |
供应商 | Tocris |
生物活性 | Selective OX2 receptor antagonist (pIC50 = 7.4 for chimeric OX2 receptors; pKB values are 5.9 and 8.5 for OX1 and OX2 receptors respectively). Shows no significant activity in a panel of over 50 other neurotransmitters and neuropeptide receptors. Achieves high level of OX2 receptor occupancy in the rat brain; exhibits sleep-promoting effects in rats. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 484.18 |
分子式 | C19H20Br2N2< |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
参考文献 | Gozziet al (2011) Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists. PLoS ONE 6 e16406. PMID: 21307957. Tranet al (2011) Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. Eur.J.Pharmacol. 667 120. PMID: 21679703. Dugovicet al (2009) Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J.Pharmacol.Exp.Ther. 330 142. PMID: 19363060. |