货号 | 4020/50 |
别名 | 1-[3-[4-(1-Piperidinylmethyl)phenox |
供应商 | Tocris |
生物活性 | High affinity histamine H3 receptor neutral antagonist (pKi values are 8.9 and 9.2 in rat and human respectively). Brain penetrant and orally active. Has 3- and 100-fold higher affinity than thioperamide (Cat. No. 0644) for rat and human H3 receptors respectively. Suppresses slow-wave sleep; exhibits wake-promoting effects in rodent arousal models. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >99 % |
计算分子量 | 389.4 |
分子式 | C20H32N2O.2HCl |
可溶性/溶解性 | Soluble to 50 mM in water and to 20 mM in DMSO with gentle warming |
参考文献 | Leet al (2008) Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists. J.Pharmacol.Exp.Ther. 325 902. PMID: 18305012. Jiaet al (2005) Effects of histamine H3 antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice. Neuropharmacology 50 404. PMID: 16310812. Barbieret al (2004) Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br.J.Pharmacol. 143 649. PMID: 15466448. |