IPSU是可口服和脑渗透性的选择性OX2R拮抗剂,pKi值为7.85。
产品描述
IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors.
体外活性
BBAC or the selective OX2R antagonist IPSU bind rapidly and reach equilibrium very quickly in binding and/or functional assays[1].
体内活性
IPSU?exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration.?IPSU increases sleep when dosed during the mouse active phase (lights off);?IPSU induces sleep primarily by increasing NREM sleep.?IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing.?The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day[2]
Cas No.
1373765-19-5
分子式
C23H27N5O2
分子量
405.502
储存和溶解度
DMSO:30 mg/mL (73.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years