| Description | IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors. |
| In vitro | BBAC或选择性 OX2R 拮抗剂 IPSU 在结合和/或功能测定中迅速结合并迅速达到平衡[1]。 |
| In vivo | IPSU具有可接受的绝对口服生物可用性，其脑/血浓度比表明了良好的脑部渗透能力。IPSU在小鼠活动期间（熄灯后）给药，能显著增加睡眠时间，主要通过增加非快速眼动(NREM)睡眠来诱导睡眠。IPSU作用发生快速，给药后首小时内总睡眠时间明显增加。此效应持续4-5小时，之后每小时的总睡眠时间与给予车辆日[2]相同。 |
| Target activity | OX2:7.85 (pKi) , OX1:6.29 (pKi) |
| molecular weight | 405.49 |
| Molecular formula | C23H27N5O2 |
| CAS | 1373765-19-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 30 mg/mL (73.98 mM) |
| References | 1. Callander GE, et al. Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. 2. Betschart C, et al. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleeparchitecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607. |